Target Validation in Disease

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Questions and Answers

Which neurotransmitter is synthesized from histidine?

  • Epinephrine
  • Histamine (correct)
  • Norepinephrine
  • Dopamine

Which type of receptors are D1 and D5 receptors?

  • G-coupled
  • Inhibitory
  • Excitatory (correct)
  • Autoreceptor

What is the main function of dopamine?

  • Learning
  • Reward (correct)
  • Motor function
  • Cognition

Which type of receptor triggers a second messenger system through G-proteins?

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

Which of the following is NOT a second messenger?

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

What is the net effect of EPSPs and IPSPs on the firing of a neuron?

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

Which one of these is the correct function of glial cells in the brain?

<p>Glia cells provide physical support and nutrients to neurons. (A)</p> Signup and view all the answers

What is the role of ionotropic receptors in neuronal communication?

<p>Ionotropic receptors bind to neurotransmitters and open ion channels. (A)</p> Signup and view all the answers

What is the difference between ionotropic and metabotropic receptors?

<p>Ionotropic receptors require the binding of a ligand to open ion channels, while metabotropic receptors do not. (D)</p> Signup and view all the answers

Which neurotransmitter is both ligand-gated and G-coupled?

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

What is the main inhibitory neurotransmitter in the nervous system?

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

Which neurotransmitter has 5 receptor subtypes, some of which are excitatory and some inhibitory?

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

Which of the following families of voltage-dependent channels allow the flow of Ca2+ into the neuron and have a role in neurotransmitter release?

<p>Cav1, Cav2, Cav3 (D)</p> Signup and view all the answers

Which of the following ligand-gated channels is activated by ATP and allows the flow of Na+ and Ca2+ into the neuron?

<p>P2X1-P2X7 (C)</p> Signup and view all the answers

Which of the following ligand-gated channels is activated by serotonin and allows the flow of Na+ and Ca2+ into the neuron?

<p>5-HT3 (C)</p> Signup and view all the answers

Which neurotransmitter is also a hormone secreted by adrenal glands?

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

Which neurotransmitter has inhibitory effects on both postsynaptic neurons and autoreceptors?

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

Which neurotransmitter is mainly produced by neurons in the tuberomammillary nucleus (TMN) in the posterior hypothalamus?

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

Which step in the drug development process involves screening compounds to identify the most promising hits?

<p>Step 4: Identifying early chemical matter (C)</p> Signup and view all the answers

What is the purpose of the 'Hit to Lead' (HTL) stage in drug development?

<p>To improve the potency, selectivity, and pharmacokinetics of the best compound (B)</p> Signup and view all the answers

Which phase of clinical testing involves testing the compound in a relatively small number of patients with the disease of interest?

<p>Phase 2 (B)</p> Signup and view all the answers

Which stage of drug development is known as the 'lead optimization' stage?

<p>2-4 years (C)</p> Signup and view all the answers

How many drugs out of 10 make it all the way through the clinic?

<p>1 (D)</p> Signup and view all the answers

What is the estimated cost of drug development, depending on the disease and number of failures?

<p>$3 billion (A)</p> Signup and view all the answers

What are the key components involved in the development of new drugs?

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

Which chapter(s) should be read for next week?

<p>Chapter 4 (A)</p> Signup and view all the answers

What is the title of the Journal Club paper by Pereira et al. that should be read?

<p>TRPA1 participation in behavioral impairment induced by chronic corticosterone administration (C)</p> Signup and view all the answers

What is the title of the Journal Club paper by Bagher et al. that should be read?

<p>Cannabinoid receptor 1 positive allosteric modulator (GAT229) attenuates cisplatin-induced neuropathic pain in mice (A)</p> Signup and view all the answers

When is the seminar scheduled for?

<p>Sept 7 (D)</p> Signup and view all the answers

What is the purpose of the 'Final thoughts' section?

<p>To provide additional information (B)</p> Signup and view all the answers

What are the two main types of receptors involved in neurotransmitter signaling?

<p>Ionotropic receptors and metabotropic receptors</p> Signup and view all the answers

What are the two ways that neurotransmitter communication is stopped?

<p>Reuptake and deactivation</p> Signup and view all the answers

What are the two possible outcomes of ion flow through ion channels on post-synaptic neurons?

<p>Excitation or inhibition</p> Signup and view all the answers

What are the two families of high/moderate voltage activated Cav channels?

<p>Cav1, Cav2, Cav3</p> Signup and view all the answers

How many subtypes of human Kv channels are there?

<p>38</p> Signup and view all the answers

What is the role of ligand-gated P2X receptors?

<p>Allow in-flow of Na+ and Ca2+ (depolarization), also allows flow of K+</p> Signup and view all the answers

Which neurotransmitter degrades dopamine in both the postsynaptic neuron and astrocytes?

<p>catechol-O-methyltransferase (COMT)</p> Signup and view all the answers

Which neurotransmitter is mainly produced by neurons in the tuberomammillary nucleus (TMN) in the posterior hypothalamus?

<p>histamine</p> Signup and view all the answers

Which neurotransmitter has inhibitory effects on both postsynaptic neurons and autoreceptors?

<p>serotonin</p> Signup and view all the answers

What is the function of glial cells in the brain?

<p>Glia cells in the brain have several functions including supplying nutrients, providing physical support and barrier, removing debris, and participating in functional interaction and neurotransmitter reuptake.</p> Signup and view all the answers

What are the two types of receptors that neurotransmitters can bind to?

<p>Neurotransmitters can bind to ionotropic receptors and metabotropic receptors.</p> Signup and view all the answers

What is the difference between ionotropic and metabotropic receptors?

<p>Ionotropic receptors have a binding site and ion channel combined, while metabotropic receptors trigger a second messenger system through G-proteins.</p> Signup and view all the answers

What are the three main pathways of dopamine?

<p>The three main pathways of dopamine are the nigrostriatal pathway, the mesolimbic pathway, and the mesocortical pathway.</p> Signup and view all the answers

What are the main functions of dopamine?

<p>The main functions of dopamine include motor function, reward, cognition, and learning.</p> Signup and view all the answers

What are the five most prevalent neurotransmitters?

<p>The five most prevalent neurotransmitters are dopamine, norepinephrine, serotonin, histamine, and acetylcholine.</p> Signup and view all the answers

Which Drug Development Stage tries to improve on 'best compound' for a specific disease by trying to fix things like potency, selectivity, and pharmacokinetics?

<p>Lead Optimization</p> Signup and view all the answers

What is the purpose of the 'Hit to Lead' (HTL) stage in drug development?

<p>To improve on screen 'hits' by improving potency, selectivity, and physiochemical properties</p> Signup and view all the answers

Which step in the drug development process involves screening compounds to identify the most promising hits?

<p>Identifying early chemical matter: A 'Hit'</p> Signup and view all the answers

What are the major classes of neurotransmitters in the central nervous system?

<p>Monoamines, GABA, glutamate, acetylcholine, various peptides, and lipids.</p> Signup and view all the answers

What is the role of peptides as neurotransmitters?

<p>Peptides can act as neuromodulators and neurotransmitters, and can act both through the synaptic cleft and diffusion to other neurons or cells.</p> Signup and view all the answers

What are some examples of lipids released as neurotransmitters?

<p>Examples of lipids released as neurotransmitters include endocannabinoids like anandamide (AEA) and 2-arachidonyl glycerol (2-AG).</p> Signup and view all the answers

What are the key components involved in the development of new drugs?

<p>The key components involved in the development of new drugs include the most basic understanding of biology for the disease and target, chemical science, and pre-clinical and clinical evaluation of the drug's efficacy and safety.</p> Signup and view all the answers

What is the estimated cost of drug development, depending on the disease and number of failures?

<p>The estimated cost of drug development ranges from $700 million to $3 billion, depending on the disease and number of failures.</p> Signup and view all the answers

When is the seminar scheduled for?

<p>The seminar is scheduled for September 7th.</p> Signup and view all the answers

What is the purpose of the 'Hit to Lead' (HTL) stage in drug development?

<p>The purpose of the 'Hit to Lead' (HTL) stage in drug development is to screen compounds and identify the most promising hits.</p> Signup and view all the answers

Which stage of drug development is known as the 'lead optimization' stage?

<p>The 'lead optimization' stage is a stage in drug development.</p> Signup and view all the answers

Which phase of clinical testing involves testing the compound in a relatively small number of patients with the disease of interest?

<p>Phase 2 clinical testing involves testing the compound in a relatively small number of patients with the disease of interest.</p> Signup and view all the answers

What is the purpose of the 'Final thoughts' section?

<p>The purpose of the 'Final thoughts' section is not specified in the given text.</p> Signup and view all the answers

Which chapter(s) should be read for next week?

<p>The chapters that should be read for next week are chapters 4 (LO 4.1, 4.3, 4.4, 4.6-4.9) on Pharmacodynamics and Types of Drug Modulation (agonist, antagonist interactions).</p> Signup and view all the answers

What is the title of the Journal Club paper by Pereira et al. that should be read?

<p>The title of the Journal Club paper by Pereira et al. that should be read is 'TRPA1 participation in behavioral impairment induced by chronic corticosterone administration'.</p> Signup and view all the answers

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