Pharmacology Exam 1

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Questions and Answers

What is the term used to describe the process of assembling small building block units into large complex molecules?

  • Monomerization
  • Hydrolysis
  • Depolymerization
  • Polymerization (correct)

Which of the following is NOT a monomer used in the building of biological macromolecules?

  • Glucose
  • Water (correct)
  • Oleic Acid
  • ATP

Which of these pairs correctly identifies a monomer and its corresponding polymer?

  • Amino Acid - Carbohydrate
  • Glucose - Protein
  • Nucleotide - DNA (correct)
  • Fatty Acid - Nucleic Acid

What is the general term for a molecule made up of three monomer units?

<p>Trimer (C)</p> Signup and view all the answers

Which of the following is NOT a function of biological macromolecules?

<p>Generating light energy (A)</p> Signup and view all the answers

Which of the following is an example of a monosaccharide?

<p>Fructose (B)</p> Signup and view all the answers

What is the difference between ATP and AMP?

<p>ATP has more phosphate groups than AMP (A)</p> Signup and view all the answers

Which of the following is a type of fatty acid?

<p>Oleic Acid (C)</p> Signup and view all the answers

Which of the following is an example of an amino acid?

<p>Tryptophan (A)</p> Signup and view all the answers

What is the primary function of proteins in cells?

<p>Catalyzing biochemical reactions (C)</p> Signup and view all the answers

What distinguishes an oligomer from a polymer?

<p>An oligomer consists of a few units. (D)</p> Signup and view all the answers

Which statement accurately describes the function of individual building block units?

<p>They have biological functions independent of polymerization. (A)</p> Signup and view all the answers

Which pair correctly links a monomer to its corresponding polymer?

<p>Fatty Acid - Triglyceride (A)</p> Signup and view all the answers

What role do protein domains play in protein structures?

<p>They provide repeating structural features. (B)</p> Signup and view all the answers

How does an agonist function in relation to a receptor?

<p>It initiates a physiological response. (D)</p> Signup and view all the answers

Which of the following statements about antagonists is true?

<p>Antagonists interfere with agonist-mediated receptor activation. (C)</p> Signup and view all the answers

What type of biomolecule includes proteins, carbohydrates, lipids, and nucleic acids?

<p>Biomolecules. (A)</p> Signup and view all the answers

What is a characteristic feature of polypeptides?

<p>They can fold into complex structures. (B)</p> Signup and view all the answers

Which hormone is involved in regulating blood pressure and is central to the peptide structure?

<p>Bradykinin (B)</p> Signup and view all the answers

What is the primary function of a receptor in biological systems?

<p>To initiate physiological functions. (D)</p> Signup and view all the answers

What is the central unifying principle of pharmacology?

<p>The lawful functional relationship between concentration of a chemical and a physiological response (C)</p> Signup and view all the answers

What are the independent and dependent variables in pharmacological studies?

<p>Independent: chemical concentration, Dependent: physiological response (A)</p> Signup and view all the answers

Which of the following is NOT a core concept in pharmacodynamics?

<p>Absorption, Distribution, Metabolism, Elimination (ADME) (B)</p> Signup and view all the answers

What is the primary focus of pharmacokinetics?

<p>How the body affects the drug (B)</p> Signup and view all the answers

Which of these is NOT a direct application of pharmacology?

<p>Medical imaging techniques (D)</p> Signup and view all the answers

What is the role of pharmacognosty in pharmacology?

<p>Studying the sources and properties of natural drugs (D)</p> Signup and view all the answers

What is the primary objective of experimental therapeutics?

<p>Testing the safety and efficacy of new drugs (D)</p> Signup and view all the answers

The concentration-response function can be used to determine which of the following properties of a drug?

<p>The optimal dosage for the drug (B)</p> Signup and view all the answers

Which of the following is NOT a core principle of pharmacology?

<p>The development of innovative drug delivery systems (A)</p> Signup and view all the answers

How is pharmacology a basic scientific discipline?

<p>It relies on basic concepts of chemistry, biology, and physics (A)</p> Signup and view all the answers

What is a primary function of nuclear receptors in cells?

<p>Directly bind to DNA to regulate gene expression (A)</p> Signup and view all the answers

What triggers the dissociation of the ligand-receptor complex from Heat Shock Protein (HSP)?

<p>The diffusion of the ligand across the membrane (A)</p> Signup and view all the answers

Which component is crucial for the recruitment of additional proteins to form a transcription initiation complex?

<p>Hormone Response Element (HRE) on DNA (D)</p> Signup and view all the answers

What distinguishes Class I nuclear receptors from Class II nuclear receptors?

<p>Their requirement for ligand binding to translocate to the nucleus (A)</p> Signup and view all the answers

Which hormone is NOT mentioned as an example of an agonist for nuclear receptors?

<p>Epinephrine (B)</p> Signup and view all the answers

Which class of G protein coupled receptors (GPCRs) is characterized by a short amino terminus and a binding site located in a lipophilic pocket?

<p>Class A (B)</p> Signup and view all the answers

What type of receptor mechanism is employed by PAR-1 (Protease Activated Receptor) for activation?

<p>Tethered ligand mechanism (A)</p> Signup and view all the answers

What distinguishes Class C GPCRs from Class A and Class B GPCRs?

<p>Larger size and functional heterodimers (B)</p> Signup and view all the answers

Which of the following correctly identifies a common feature of ion channels?

<p>Can be voltage-gated or ligand-gated (C)</p> Signup and view all the answers

In terms of drug targets, which molecular structure is primarily involved in the binding of small molecules?

<p>G protein coupled receptors (B)</p> Signup and view all the answers

What type of binding is predominantly found in Class B GPCRs?

<p>Binding to extracellular loops (B)</p> Signup and view all the answers

Which type of receptor primarily interacts with insulin as a target?

<p>Transporters (C)</p> Signup and view all the answers

Which class of GPCRs is the most diverse and numerous among the classifications?

<p>Class A (A)</p> Signup and view all the answers

What is the effect of IP3 microinjection on neuroepithelioma cells?

<p>It stimulates intracellular release of calcium. (C)</p> Signup and view all the answers

What is the primary role of adenylyl cyclase in cellular processes?

<p>It converts ATP to cAMP. (C)</p> Signup and view all the answers

What occurs following the activation of GRKs in the presence of an agonist?

<p>It promotes β-arrestin recruitment to the receptor. (A)</p> Signup and view all the answers

Which of the following represents a potential fate of internalized GPCRs?

<p>They may undergo degradation in lysosomes. (B)</p> Signup and view all the answers

What is the composition of a sweet taste receptor?

<p>A heterodimer of two full-length GPCR monomers (A)</p> Signup and view all the answers

What role do β-arrestins play in GPCR signaling?

<p>They facilitate receptor internalization. (C)</p> Signup and view all the answers

How does GTP affect G protein activation?

<p>GTP activates G proteins by facilitating their GDP conversion (B)</p> Signup and view all the answers

What is the primary role of phospholipase C in cellular signaling?

<p>To hydrolyze phospholipids and produce signaling molecules (B)</p> Signup and view all the answers

What is the action of caffeine on adenylyl cyclase?

<p>It supports the conversion of ATP to cAMP. (C)</p> Signup and view all the answers

What happens after IP3 binds to its receptor on the endoplasmic reticulum?

<p>Calcium is released into the cytoplasm (D)</p> Signup and view all the answers

What triggers the recruitment of clathrin during GPCR internalization?

<p>The phosphorylation of the receptor by GRKs. (B)</p> Signup and view all the answers

Which of the following components is generated from the cleavage of PIP by phospholipase C?

<p>IP3 and DAG (D)</p> Signup and view all the answers

Which molecule acts as an inhibitor by reversing cAMP back to AMP?

<p>Phosphodiesterase (D)</p> Signup and view all the answers

Which ion is primarily released from the endoplasmic reticulum due to the action of IP3?

<p>Calcium (B)</p> Signup and view all the answers

What is the primary consequence of receptor desensitization?

<p>Decreased receptor expression on the cell surface. (B)</p> Signup and view all the answers

What structural feature allows the sweet taste receptor to bind its tastants?

<p>A ‘venus flytrap’ binding pocket (D)</p> Signup and view all the answers

What cellular component is involved in stabilizing the receptor complex during internalization?

<p>Clathrin (C)</p> Signup and view all the answers

What is generated when a G protein is activated by GTP?

<p>Activated downstream signaling components (C)</p> Signup and view all the answers

Which cellular structure is associated with the release of calcium upon IP3 receptor activation?

<p>Endoplasmic reticulum (D)</p> Signup and view all the answers

What is the end result of the signal transduction cascade initiated by the activation of GPCRs?

<p>Physiological changes in the cell (B)</p> Signup and view all the answers

What is the role of kinases in biological processes?

<p>Kinases are proteins that regulate the activity of other proteins by adding a phosphate group. (C)</p> Signup and view all the answers

What does cAMP activate?

<p>Protein Kinase A (PKA) (A)</p> Signup and view all the answers

What is the function of acetylcholinesterase in nerve signaling?

<p>Acetylcholinesterase breaks down acetylcholine, terminating the signal. (A)</p> Signup and view all the answers

Which of the following statements about enzymes is TRUE?

<p>Enzymes reduce the activation energy of a reaction. (D)</p> Signup and view all the answers

What effect does a catalyst have on the rate of a chemical reaction?

<p>A catalyst increases the rate of the reaction by providing an alternative reaction pathway with a lower activation energy. (B)</p> Signup and view all the answers

What is the primary role of a catalyst in a chemical reaction?

<p>To increase the rate of the reaction without being consumed. (A)</p> Signup and view all the answers

What is the relationship between cAMP and Protein Kinase A (PKA)?

<p>cAMP is a second messenger that activates PKA. (C)</p> Signup and view all the answers

How does acetylcholinesterase affect the transmission of nerve signals?

<p>It terminates the transmission of nerve signals by breaking down acetylcholine. (B)</p> Signup and view all the answers

What is the main function of phosphorylation in the context of kinases?

<p>Phosphorylation adds a phosphate group to a protein, which can activate or deactivate the protein. (C)</p> Signup and view all the answers

Which of the following statements accurately describes how enzymes catalyze reactions?

<p>Enzymes lower the activation energy required for the reaction to proceed. (D)</p> Signup and view all the answers

What is the primary function of Acetylcholinesterase?

<p>To break down acetylcholine into acetic acid and choline (B)</p> Signup and view all the answers

Which of the following is NOT a type of ion channel based on the provided text?

<p>Ligand-gated sodium channel (D)</p> Signup and view all the answers

Which of the following statements is TRUE about ion channels?

<p>Ion channels can be regulated by both voltage and ligand binding. (B)</p> Signup and view all the answers

What is a ‘patch clamp’ used for in the context of ion channels?

<p>To measure the conductance of a single ion channel (B)</p> Signup and view all the answers

How do agonists affect the activity of ion channels?

<p>Agonists can stabilize an open state and increase its frequency of opening. (C)</p> Signup and view all the answers

Which type of ion channel is the nicotinic acetylcholine receptor?

<p>Ligand-gated cation channel (B)</p> Signup and view all the answers

Where are nicotinic receptors primarily located?

<p>On the postsynaptic side of the neuromuscular junction (A)</p> Signup and view all the answers

What distinguishes transporters from ion channels?

<p>Transporters exhibit a high degree of selectivity for the molecules they transport, while ion channels are less selective. (A)</p> Signup and view all the answers

Based on the text, what is the primary role of transporters in biological systems?

<p>To move neurotransmitters and hormones across membrane barriers (C)</p> Signup and view all the answers

Which of the following is NOT an example of a ligand that binds to a ligand-gated ion channel, as mentioned in the text?

<p>Sodium (A)</p> Signup and view all the answers

Which of the following accurately describes the function of P-gp (P-glycoprotein, or mdr1)?

<p>P-gp functions as an efflux transporter, actively removing substances from cells. (A)</p> Signup and view all the answers

Which category of transporters is responsible for the movement of neurotransmitters like serotonin, norepinephrine, and dopamine?

<p>SLC Transporters (D)</p> Signup and view all the answers

What is a key difference between primary and secondary active transport?

<p>Primary active transport utilizes ATPases, while secondary active transport relies on symporters and antiporters. (C)</p> Signup and view all the answers

What is a primary characteristic of facilitated diffusion?

<p>It involves the binding of substrates to transporter proteins, leading to saturable transport. (B)</p> Signup and view all the answers

Which of the following statements accurately describes the directionality of SLC transporters?

<p>SLC transporters can operate in both directions, facilitating both influx and efflux of substrates. (A)</p> Signup and view all the answers

What is the primary mechanism by which P-gp (P-glycoprotein) facilitates the removal of substrates from cells?

<p>P-gp directly hydrolyzes ATP to power the movement of substrates out of cells. (D)</p> Signup and view all the answers

Which of the following is NOT a characteristic of secondary active transport?

<p>It utilizes ATP hydrolysis directly to move substrates across the membrane. (D)</p> Signup and view all the answers

In the context of transporter proteins, what is the meaning of the term "vectorial" transport?

<p>Transport that occurs along a specific direction, such as from the inside of a cell to the outside. (C)</p> Signup and view all the answers

What is the main purpose of the drug-binding pocket in a transporter protein?

<p>To provide a site for the binding of specific substrates, which are then transported across the membrane. (C)</p> Signup and view all the answers

Which of the following best describes the role of transporters in drug response?

<p>Transporters can influence the absorption, distribution, metabolism, and excretion (ADME) of drugs. (A)</p> Signup and view all the answers

What was Claude Bernard's primary contribution to the field of medicine?

<p>He introduced the scientific method to the study of medicine. (D)</p> Signup and view all the answers

How did Claude Bernard demonstrate that curare's effect was on the nerves and not the muscles?

<p>By showing that curare blocked muscle contraction when injected directly into the muscle but not when injected into the nerve innervating the muscle. (B)</p> Signup and view all the answers

What observation led Claude Bernard to conclude that curare must be carried by the blood to have an effect?

<p>Ingestion of curare had no effect on the animal. (A)</p> Signup and view all the answers

Which of the following statements accurately reflects Claude Bernard's findings about the effects of curare?

<p>Curare primarily affects motor nerves, leaving sensory nerves unaffected. (A)</p> Signup and view all the answers

What was Claude Bernard's key finding about the mechanism of curare's action?

<p>Curare acts on a specific site at the neuromuscular junction, interfering with the transmission of nerve impulses to the muscle. (C)</p> Signup and view all the answers

What is the significance of Claude Bernard's research on curare?

<p>It led to a deeper understanding of how drugs work at the molecular level. (C)</p> Signup and view all the answers

What is the mathematical relationship between the dissociation constant (KD) and the rate constants (k1 and k2)?

<p>KD = k2 / k1 (D)</p> Signup and view all the answers

If the value of k1 is 1 and the value of k2 is 0.5, what is the corresponding affinity of the interaction?

<p>Medium affinity (A)</p> Signup and view all the answers

What is the unit for the dissociation constant (KD)?

<p>Molar (M) (A)</p> Signup and view all the answers

What does a high dissociation constant (KD) generally suggest about the affinity of a ligand to its receptor?

<p>Lower affinity (B)</p> Signup and view all the answers

How does the rate of association (k1) compare to the rate of dissociation (k2) at equilibrium?

<p>k1 is equal to k2 (C)</p> Signup and view all the answers

What is the underlying principle behind the relationship between kinetics and affinity?

<p>Affinity is determined by the ratio of the rate constants (D)</p> Signup and view all the answers

What is the relationship between curare and nicotine, as described in the content?

<p>They are mutually antagonistic, meaning they have opposing effects on the same receptor. (D)</p> Signup and view all the answers

What does the content suggest about the nature of the "receptive substance" shared by curare and nicotine?

<p>It is a specific site on a protein, where both drugs can bind and elicit their respective effects. (A)</p> Signup and view all the answers

Why is the "receptive substance" described as "saturable"?

<p>Because it can only bind to a limited number of drug molecules at a time. (B)</p> Signup and view all the answers

Which of the following is TRUE about a system at equilibrium, as defined in the content?

<p>The rate of change in one direction is equal to the rate of change in the opposite direction. (B)</p> Signup and view all the answers

Which of the following best describes the relationship between the "biological tissue" and "receptors" in the provided illustration?

<p>The receptors are located within the biological tissue, and are accessible from the extracellular space. (A)</p> Signup and view all the answers

Based on the information provided, what is the nature of interactions between receptors and ligands?

<p>Reversible chemical reactions, allowing for dynamic binding and unbinding. (D)</p> Signup and view all the answers

In the Law of Mass Action, what does the association constant (KA) represent?

<p>The ratio of product to reactant concentrations at equilibrium. (D)</p> Signup and view all the answers

What is the primary assumption underlying the Law of Mass Action, as it applies to drug-receptor interactions?

<p>That the rate of reaction is directly proportional to the concentration of reactants. (B)</p> Signup and view all the answers

What is the main significance of the Hill-Langmuir Equation in pharmacology?

<p>It describes the relationship between drug concentration and the effects on the body. (D)</p> Signup and view all the answers

What is the primary concept Langley developed in his research, that was further expanded upon?

<p>Drugs work by binding to specific receptors on the surface of cells. (D)</p> Signup and view all the answers

How did Erlich's work contribute to Langley's concept of 'receptive substances'?

<p>Erlich demonstrated that drugs work by binding to specific chemical groups on the surface of cells. (D)</p> Signup and view all the answers

What principle does the observation of 'mutual antagonism' between curare and nicotine support?

<p>Drugs work by binding to specific receptors, and different drugs can compete for the same receptor site. (D)</p> Signup and view all the answers

How does Langley's concept of a 'receptive substance' address the issue of the effectiveness of small concentrations of agonist?

<p>Small concentrations can have a large effect because the agonists interact with specific receptors. (B)</p> Signup and view all the answers

What is the 'chemotherapeutic index' in the context of Erlich's work?

<p>The difference between the dose of a drug that is effective and the dose that is toxic. (A)</p> Signup and view all the answers

Which of the following is NOT a characteristic of a 'receptive substance' as described by Langley?

<p>It is independent of the concentration of the chemical. (B)</p> Signup and view all the answers

What is the main difference between Langley's 'receptive substance' and modern pharmacological concept of a receptor?

<p>Langley's 'receptive substance' is a hypothetical entity, while receptors are concrete structures confirmed scientifically. (D)</p> Signup and view all the answers

How did Claude Bernard's contribution help to refine the concept of a 'receptive substance'?

<p>Bernard provided a series of experiments that localized the action of curare to the neuromuscular junction. (C)</p> Signup and view all the answers

What is the primary factor that determines the selectivity of a drug for a specific receptor?

<p>The affinity of the drug for the receptor (A)</p> Signup and view all the answers

What is meant by the term "enantiomers" in the context of molecules?

<p>Molecules that are mirror images of each other and cannot be superimposed (A)</p> Signup and view all the answers

What is the relationship between drug concentration and receptor selectivity?

<p>Higher drug concentration generally leads to lower selectivity for the target receptor (A)</p> Signup and view all the answers

Which of the following statements accurately describes the concept of "affinity" in the context of drug-receptor interactions?

<p>Affinity refers to the strength of the bond between a drug and its receptor (D)</p> Signup and view all the answers

How does the "potency rank-order" of different drugs help in identifying receptor subtypes?

<p>By comparing the relative concentrations of drugs required to produce a specific effect, different receptor subtypes can be identified. (A)</p> Signup and view all the answers

What does the KD value represent in the context of drug-receptor interactions?

<p>The concentration of drug required to achieve 50% of the maximum response (C)</p> Signup and view all the answers

What is the relationship between "affinity" and "selectivity" in drug-receptor interactions?

<p>Higher affinity generally leads to higher selectivity (A)</p> Signup and view all the answers

Which of the following is a key difference between agonists and antagonists in terms of their effects on receptors?

<p>Agonists activate receptors, while antagonists block receptor activation (A)</p> Signup and view all the answers

Which of the following statements accurately describes the impact of enantiomers on pharmacological activity?

<p>Enantiomers often have different pharmacological activities (A)</p> Signup and view all the answers

What is the primary reason for the development of different drug subtypes for the same receptor family?

<p>To target specific tissues or functions more effectively (D)</p> Signup and view all the answers

What is the relationship between the EC50 and the KD?

<p>EC50 is the concentration causing 50% of the maximum response, while KD is the measure of a drug's affinity for its receptor. (C)</p> Signup and view all the answers

What differentiates a full agonist from a partial agonist?

<p>Full agonists are capable of producing their maximum response while binding to 100% of the receptors, while partial agonists can only achieve a partial response even when all receptors are occupied, regardless of concentration. (B)</p> Signup and view all the answers

What is the defining characteristic of an inverse agonist?

<p>It stabilizes the receptor in a conformation that cannot couple to G-proteins, leading to a reduction in basal activity. (D)</p> Signup and view all the answers

How do competitive antagonists affect the concentration-response curve of an agonist?

<p>They shift the curve to the right, indicating that a higher concentration of the agonist is needed to reach the same level of response. (B)</p> Signup and view all the answers

What is the mechanism of action for a biased agonist?

<p>Biased agonists bind to different regions of the receptor, leading to different conformational changes and activation of only specific signaling pathways. (B)</p> Signup and view all the answers

Which of the following statements about receptor conformations is TRUE?

<p>Receptors are dynamically evolving structures, and their conformation is influenced by the binding of ligands. (B)</p> Signup and view all the answers

What is the key difference between a competitive antagonist and a noncompetitive antagonist?

<p>Competitive antagonists bind to the same site as the agonist, while noncompetitive antagonists bind to a different site. (D)</p> Signup and view all the answers

What is the most likely outcome of increasing the concentration of an agonist in the presence of a noncompetitive antagonist?

<p>The response will not increase significantly beyond a certain point, even at very high concentrations. (B)</p> Signup and view all the answers

What is the primary mechanism by which a noncompetitive antagonist exerts its effect?

<p>It induces a conformational change in the receptor, making it less likely to bind the agonist. (C)</p> Signup and view all the answers

Flashcards

Pharmacology

The experimental study of the chemical control of physiology.

Independent Variable

The variable that is manipulated, such as chemical concentration.

Dependent Variable

The outcome measured in response to the independent variable, like physiological response.

Concentration-Response Function

The relationship between chemical concentration and physiological response, central to pharmacology.

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Pharmacodynamics

Study of what drugs do to the body, including ligand/receptor interactions.

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Pharmacokinetics

Study of what the body does to a drug, including absorption, distribution, metabolism, and elimination (ADME).

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ADME

Acronym for Absorption, Distribution, Metabolism, and Elimination, key processes in pharmacokinetics.

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Ligand

A chemical that binds to a receptor to produce a physiological response.

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Pharmacognosy

The study of medicinal drugs derived from plants and other natural sources.

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Modern Therapeutics

The application of pharmacology principles in treating diseases with drugs.

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Oligomer

A molecule made of a few monomer units.

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Polymer

A large molecule formed from many monomers.

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Monomer

A single building block unit of a polymer.

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Glucose

A simple sugar and key energy source for cells.

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Amino Acids

Building blocks of peptides and proteins.

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Peptide

Short chains of amino acids linked together.

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Agonist

A ligand that activates a receptor to induce a response.

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Antagonist

A ligand that blocks or inhibits receptor activation.

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Biomolecule

A molecule produced by a living organism (e.g., proteins).

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Monosaccharides

Simple sugars like glucose and fructose that are building blocks of carbohydrates.

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Fructose

A monosaccharide found in fruits; sweetener.

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Nucleotides

Building blocks of nucleic acids; includes ATP, AMP, GTP.

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ATP

A nucleotide that serves as the primary energy carrier in cells.

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Fatty Acids

Building blocks of lipids, essential for energy storage and membranes.

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Polymerization

The process of combining small units (monomers) to form large molecules (polymers).

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Emergent Properties

New traits that arise when monomers combine into polymers, essential for life.

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Sweet Taste Receptor

A heterodimer formed by two GPCR monomers that detects sweet taste.

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Venus Flytrap Binding Pocket

A structure in the sweet receptor that traps and binds tastants.

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G Protein Activation Cycle

The cycle where GTP activates G proteins, while GDP inactivates them.

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Phospholipase C (PLC)

An enzyme that cleaves phospholipids to produce IP3 and DAG.

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IP3 (Inositol trisphosphate)

A molecule generated by PLC that triggers calcium release from the ER.

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Calcium Release

The process where calcium ions exit the ER into the cytoplasm, triggered by IP3.

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Endoplasmic Reticulum (ER)

An organelle where calcium is stored and released into the cytoplasm.

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Sarcoplasmic Reticulum (SR)

Specialized form of ER found in muscle cells that stores calcium ions.

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Signal Transduction Cascade

A series of molecular events initiated by a receptor leading to a cellular response.

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Guanosine Tri- and Diphosphates

Nucleotides involved in the G protein activation cycle; GTP activates, GDP inactivates.

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Nuclear Receptors

Transcription factors that bind to DNA to regulate gene expression.

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Class I Nuclear Receptors

Receptors found in the cytosol that translocate to the nucleus upon ligand binding.

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Class II Nuclear Receptors

Receptors that reside in the nucleus and recruit coactivators upon ligand binding.

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Hormone Response Element (HRE)

DNA sequence that binds the ligand-receptor complex for transcription initiation.

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Agonists for Nuclear Receptors

Substances that activate nuclear receptors, such as steroid hormones.

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Microinjection of IP3

Technique used to introduce IP3 into cells, triggering calcium release.

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Calcium Signaling

A crucial process where calcium ions act as a signal in cells.

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Adenylyl Cyclase

An enzyme that converts ATP into cAMP, a secondary messenger.

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Receptor Down-regulation

Process where receptors are internalized or degraded after prolonged stimulation.

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β-Arrestins

Proteins that mediate the internalization of G protein-coupled receptors (GPCRs).

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GPCR internalization

The process where GPCRs are engulfed by the cell membrane into vesicles.

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Clathrin-coated pits

Areas in the cell membrane that help in endocytosis of receptors.

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GRKs

G protein-coupled receptor kinases that phosphorylate active receptors.

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Endocytic vesicle

Membrane-bound compartment where engulfed receptors are stored.

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G Protein Coupled Receptors (GPCRs)

A large family of cell surface receptors that respond to various ligands.

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Ion Channels

Proteins that allow ions to pass through cell membranes, crucial for cell signaling.

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Enzyme Linked Receptors

Receptors that are associated with enzymes, which can activate responses upon ligand binding.

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Class A GPCRs

The most common GPCR class, typically with small molecule binding sites.

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Class B GPCRs

GPCRs with longer aminotermini involved in binding ligands, often peptides.

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Class C GPCRs

This class has large amino termini and often forms heterodimers with other receptors.

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Voltage Gated Channels

Ion channels that open or close in response to changes in membrane potential.

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Ligand Gated Channels

Ion channels that open in response to the binding of a chemical messenger.

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Cleavage of Acetylcholine

Acetylcholinesterase cleaves acetylcholine into acetic acid and choline.

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Conductance

The rate of ion flow through an open ion channel.

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Nicotinic Acetylcholine Receptor

A ligand-gated cation channel activated by acetylcholine, crucial at neuromuscular junctions.

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Agonists in Ion Channels

Substances that stabilize an open state of ion channels, increasing ion flow frequency.

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Functional States of Ion Channels

Ion channels can exist in closed, open, or various conductive states.

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Patch Clamp Technique

A method to measure the ion conductance of individual ion channels.

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Transporters

Integral membrane proteins that move neurotransmitters and hormones across membranes.

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Active Transport

Process requiring energy (ATP) to move substances across membranes against their gradient.

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Facilitated Diffusion

Passive movement of molecules across membranes through transport proteins, driven by concentration gradients.

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ABC Transporters

ATP-binding cassette transporters that use ATP to move molecules, often uni-directionally (efflux).

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P-glycoprotein (P-gp)

A specific ABC transporter that reduces drug concentration in cells by ejecting them.

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SLC Transporters

Solute carrier transporters that facilitate or actively transport molecules, allowing both influx and efflux.

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Symporters

Transporters that move two different substances in the same direction across a membrane.

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Antiporters

Transporters that move one substance in while moving another out of the cell.

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Secondary Active Transport

Transport that indirectly relies on primary active transport (ATP); often involves symporters and antiporters.

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Uniporters

Transporters that move a single substrate down its concentration gradient without energy usage.

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Enzymes

Proteins that act as catalysts to speed up chemical reactions without being consumed.

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Catalysts

Substances that increase the rate of a chemical reaction without being consumed in the process.

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Kinases

Proteins that regulate the activity of other proteins by adding phosphate groups, a process called phosphorylation.

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Phosphorylation

The addition of a phosphate group to a molecule, often used to activate or deactivate proteins.

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Protein Kinase A (PKA)

An enzyme activated by cAMP that phosphorylates target proteins to regulate their function.

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Acetylcholinesterase

An enzyme that breaks down the neurotransmitter acetylcholine, thus terminating the signal transmission.

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Neurotransmitter signaling

Chemical signals that transmit messages across a synapse from one neuron to another.

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Regulation of Cellular Events

The control of various processes within a cell, often mediated by enzymes and signaling molecules.

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Cellular Responses

The outcomes or actions that result from signal transduction pathways in cells.

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Receptive Substance

A hypothetical site in cell membranes where drugs and chemicals bind to elicit effects.

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Mutual Antagonism

The phenomenon where two substances interfere with each other's effects at a common site.

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Saturable Effects

A concept where the biological response to a drug reaches a maximum beyond which no effect increases.

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Antimicrobials

Drugs specifically designed to target and kill microorganisms like bacteria.

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Chemical Side Chain Haptophores

Chemical functional groups on cell surfaces that interact with antibodies and drugs.

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Curare

A traditional antineurotoxin that blocks nerve impulses to muscles, illustrating mutual antagonism.

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Bioreactive Chemicals

Chemicals that can interact with biological systems to elicit a response.

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Claude Bernard

Father of Modern Physiology; first chair of physiology at the Sorbonne.

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Pharmacologic Action

Curare blocks nerve signals but not muscle stimulation; affects motor nerves only.

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Neuromuscular Junction

The synapse where nerve cells connect with muscles; crucial for muscle contraction.

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Blood Carrying Effect

Curare must be transported by blood to exert its effects; ingestion does not work.

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Reflex Contraction Experiment

Stimulation of the paralyzed leg produces contraction in the other leg, showing reflex pathways are intact despite paralysis.

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Equilibrium

A state where net changes cease, though individual reactions continue to occur.

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Reversible Reactions

Chemical reactions where reactants can form products and vice versa, signaling a dynamic balance.

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Hill-Langmuir Equation

Describes the relationship between drug concentration and receptor binding affinity at equilibrium.

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Law of Mass Action

Rules explaining how reaction rates relate to concentrations of reactants and products.

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Association Constant (KA)

A measure of how tightly a ligand binds to its receptor, calculated at equilibrium.

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Dissociation Constant (KD)

The inverse of KA; a measure of how easily a ligand detaches from its receptor.

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Binding and Dissociation Rates

Rates of how quickly ligands attach to and detach from receptors, dictated by constants k1 and k2.

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Extracellular Space

The area outside cells where receptors are located and ligands can bind.

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Equilibrium in Binding

A state where the rate of association equals the rate of dissociation of a ligand-receptor complex.

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Rate Constants (k1, k2)

k1 is the rate constant for association; k2 is for dissociation; they help define KD.

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Units of k1 and k2

k1 has units of min-1 M-1, whereas k2 has units of min-1, showing their roles in reaction speed.

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Affinity Relationship with KD

KD represents how strongly a ligand binds to a receptor; it is directly linked to binding affinity.

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Equilibrium Expression

At equilibrium, the expression [R][D] = k2[RD] illustrates the relationship between free and bound states.

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Enantiomers

Molecules that are non-superimposable mirror images of each other.

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Chiral Center

A carbon atom bonded to four different groups, leading to enantiomer formation.

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SERT Inhibition

The ability of a drug to inhibit the serotonin transporter, affecting serotonin reuptake.

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Affinity

A measure of how strongly a drug binds to its target receptor.

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Potency

The amount of drug needed to produce a desired effect at a target receptor.

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Alpha Adrenergic Subtypes

Six identified subtypes of receptors that respond to catecholamines, like epinephrine.

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Beta Adrenergic Subtypes

Three identified subtypes of receptors primarily involved in cardiovascular responses.

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Drug Concentration

The amount of drug present affects its selectivity and potential side effects.

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EC50

The concentration of an agonist that produces half-maximal response.

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KD

Dissociation constant indicating receptor affinity; lower KD means higher affinity.

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Intrinsic Efficacy

The ability of an agonist to produce a response when binding to a receptor.

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Full Agonist

An agonist that produces the maximum biological response possible.

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Partial Agonist

An agonist that activates a receptor but with less efficacy than a full agonist.

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Inverse Agonist

A ligand that stabilizes a receptor in an inactive form, reducing signaling.

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Competitive Antagonist

Substance that binds to the same site as the agonist but does not activate the receptor.

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Noncompetitive Antagonist

Binds to a different site and changes the receptor's shape to prevent agonist binding.

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Spare Receptors

Receptors that are not occupied by agonists but can contribute to efficacy.

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Biased Agonist

An agonist that preferentially activates certain signaling pathways over others.

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Study Notes

Important Organic "Building Block" Molecules

  • Monosaccharides are used by cells
  • Glucose and fructose are examples of monosaccharides
  • Nucleotides are another important building block
  • Adenosine triphosphate (ATP), adenosine monophosphate (AMP), and guanosine triphosphate (GTP) are examples
  • Fatty acids are a type of lipid
  • Oleic acid and Omega-3 fatty acids are examples
  • Amino acids are also crucial building blocks
  • Glutamate (glutamic acid), tryptophan, serine, and threonine are examples

Biological Macromolecules

  • Macromolecules have the ability to polymerize
  • Polymerization efficiently assembles building blocks to create complex molecules
  • The act of joining building blocks is called polymerization
  • Each building block is a monomer
  • Combining two monomers makes a dimer, three monomers a trimer, and so on
  • An oligomer is a few monomers, and a polymer is many monomers
  • Each building block has a function independently of polymerization
  • Examples of functions include energy currency (ATP), neurotransmitter/hormone (ATP), nutrient/neurotransmitter (glutamic acid), and nutrient (glucose)

Examples of Monomers and Polymers

  • Glucose is a carbohydrate monomer
  • Amylose (starch) is a carbohydrate polymer
  • Adenosine monophosphate (AMP) is a nucleotide monomer
  • Ribonucleic acid (RNA) is a nucleotide polymer

Examples of Lipid Monomers/Polymers

  • Lipids are also important building blocks
  • A general type of lipid monomer is shown
  • Palmitic acid is an example of a fatty acid
  • A triglyceride is a polymer of fatty acids
  • Examples of fatty acids found in triglycerides include palmitic, oleic, and linolenic acid
  • A phospholipid is also a polymer. They have both a hydrophilic ("water-loving") head and hydrophobic ("water-fearing") tails.
  • Glycerol is a part of the phospholipid molecule

Peptides and Proteins

  • Peptides and proteins are polymers of amino acid monomers
  • Amino acids have an amine group, a carboxyl group, a central carbon, and a variable R group
  • Combining amino acids through peptide bonds forms oligopeptides and proteins
  • Arg-Pro-Gly-Phe-Ser-Pro-Phe-Arg is an example of an oligopeptide, also known as bradykinin
  • Proteins have different levels of structure, including primary, secondary, tertiary, and quaternary structures
  • The primary structure is the sequence of amino acids
  • Secondary structures include alpha helices and beta pleated sheets
  • Tertiary structure is the overall three-dimensional shape
  • Quaternary structure occurs when multiple polypeptide chains combine

Protein Multimerization

  • Proteins can combine to form more complex structures called multimers
  • An example is the heterotetrameric voltage-gated potassium channel

Protein Domains

  • Proteins have repeating structural units called domains, contributing to more intricate structures

Versatility of Protein Chemistry

  • Proteins' diverse structures result in a wide array of functions.
  • Bradykinin, a peptide hormone, is involved in blood pressure regulation.

Definitions

  • A ligand is a molecule that forms a complex with a biomolecule
  • A biomolecule is a molecule produced by a living organism (proteins, carbohydrates, lipids, nucleic acids)
  • An agonist is a ligand that causes a response by binding to a receptor. It's essentially an external stimulus (chemical).
  • A receptor is a biomolecule that starts a physiological function by forming a complex with an agonist.
  • An antagonist is a ligand that interferes with, or blocks, an agonist's response.

Pharmacology

  • Pharmacology studies how chemicals control physiology.
  • To gain knowledge about physiology, pharmacology uses precise exogenous application of chemicals
  • The chemical concentration is the independent variable
  • The physiological response is the dependent variable
  • The relationship between the concentration of a chemical and its response is the core of pharmacology (concentration-response relationship).
  • Pharmacology is both a basic science and applicable to modern therapeutics, pharmacy, and drug discovery.
  • Pharmacodynamics describes the ligand-receptor interactions
  • Pharmacokinectics describes what happens to a drug on its way to a receptor (ADME: absorption, distribution, metabolism, elimination)

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Related Documents

Lec 1 PDF - Organic Molecules & Biological Macromolecules
Drug Targets PDF
Enzymes and Ion Channels PDF
Lec 4.pdf - Father of Modern Physiology
Lecture 5: Receptor Pharmacology (PDF)

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