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</p> Signup and view all the answers

    Which of the following is NOT a second messenger?

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

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

    <p>Excitation</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.</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.</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.</p> Signup and view all the answers

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

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

    What is the main inhibitory neurotransmitter in the nervous system?

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

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

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

    Which neurotransmitter is also a hormone secreted by adrenal glands?

    <p>Noradrenaline</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

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

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

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

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

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

    <p>1</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</p> Signup and view all the answers

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

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

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

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

    When is the seminar scheduled for?

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

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

    <p>To provide additional information</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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