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Match drugs and receptor types to function

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Question
Answer
What are the 3 main types of classical ntm?   Monoamines (catecholamines, 5HT), Acetylcholine, Amino acids (GABA, glutamate)  
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What are the 5 types of non-classical ntm?   Neuropeptides, lipids, gases, D-amino acids, purines  
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What are the 4 characteristics of classical neuromodulatory systems?   subcortical, long projections to cortex, excitatory or inhibitory, for arousal/attention/motivation  
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What are the 2 metabolites of NE when broken down? For DA?   MHPG, VMA for NE; HVA for DA  
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Dopa --> Dopamine needs which enzyme?   AADC  
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Dopamine --> NE needs which enz?   DBH (marker of NE cells)  
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NE --> EPIN needs which enz?   phenylethanolamine-N-methyltransferase  
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The substantia nigra is a region in which ntm system and what does it control?   DA. movement  
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The ventral tegmental area (VTA) is a region in which ntm system and what does it control?   DA. reward/reinforcement, mood, concentration  
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What is the region of the DA system that controls olfaction?   periglomerular cells  
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The tuberophypophysialincertohypothalamic is a region in which ntm system and what does it control?   DA. hormones  
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In the DA system, how does D1-like receptors act? Which 2 receptors are they? Where are they?   increase cAMP. D1, D5. Caudate-putamen, nucleus accumbens, olf, hippocampus, hypothalamus  
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In the DA system, how does D2-like receptors act? Which 3 receptors are they?   decrease cAMP, open K+ channels, increase AA, decrease Ca++. D2, D3, D4  
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SKF38393. ntm system? receptor? fxn?   DA. D1. agonist  
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fenoldopam. what else is it called? ntm system? receptor? fxn?   SKF 82526. DA. D1. agonist  
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clozapine. ntm system? receptor? fxn?   DA. D4. agonist... inhibitory since reduce cAMP  
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quinpirole. ntm system? receptor? fxn?   DA. D2, D3. agonist.  
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pergolide. ntm system? receptor? fxn?   DA. D2, D3. agonist.  
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apomorphine. ntm system? receptor? fxn?   DA. D1, D2. agonist.  
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bromocriptine. ntm system? receptor? fxn?   DA. D2. agonist  
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dihydrexidine. ntm system? receptor? fxn?   DA. D1. agonist.  
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haloperidol. ntm system? receptor? fxn?   DA, D2, antagonist  
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sulpiride. ntm system? receptor? fxn?   DA, D2, antagonist  
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spiperone. ntm system? receptor? fxn?   DA, D2, antagonist  
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YM-09151-2. ntm system? receptor? fxn?   DA, D2. antagonist  
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S 14297. ntm system? receptor? fxn?   DA, D3, antagonist  
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NNC-112. ntm system? receptor? fxn?   DA, D1. antagonist  
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SCH 23390, SCH 39166. ntm system? receptor? fxn?   DA, D1, antagonist  
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Describe the pathway after D1 and D2 receptors are bound by dopamine or a drug.   receptor-->G protein-->AC-->cAMP-->PKC-->open Na+ ch. note: in D2-receptors less cAMP results in more open K+ channels  
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How many DA receptors are metabotropic?   5 (all)  
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What are the 3 pathways for DA? Which one is for reward?   mesolimbic (reward), mesocortical, nigrostriatal  
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Where does VTA project to in the mesolimbic pathway for DA?   nucleus accumbens, amygdala, lateral septum, olfactory tubercule  
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Where does VTA project to in the mesocortical pathway that the mesolimbic pathway doesn't for DA?   prefrontal cortex, hippocampus  
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What 3 areas are involved in the reward pathway?   VTA --> nucleus accumbens --> prefrontal cortex  
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Parkinson's is due to the death of what area of which neurons?   substantia nigra, DA  
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What is the precursor for catecholamines? For 5HT? For glutamate? For GABA? For ACh?   tyrosine. tryptophan. glutamine. glutamate. acetyl coa and choline.  
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increase catecholamine levels in brain by inhibiting MAO (MAOI)   phenelzine  
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inhibits tyrosine hydroxylase. what ntm system?   AMPT. DA  
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lowers catecholamine levels by inhibiting vMAT   reserpine  
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6-OHDA. fxn? what system?   lesions/kills catecholamine neurons (DA, NE)  
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what recreational drug causes more release of catecholamines?   amphetamine  
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what recreational drug inhibits reuptake of catecholamines?   cocaine  
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methylphenidate. fxn? what ntm system?   same as cocaine - stops reuptake of catecholamines  
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apomorphine   DA agonist, mainly D2 (DA)  
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agonists for D1 receptors (DA)   SKF 38393, fenoldam  
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SCH 23390, NCC-112   antagonist for D1 receptor (DA)  
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quinpirole   agonist for D2, D3 receptors (DA)  
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haloperidol   antagonist for D2 (DA)  
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Locus Coeruleus (A6): where is it (approx)? where does it project to? what ntm system? fxn?   pons. all of forebrain. NE. arousal (sleep/wake)  
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Which activates the locus coeruleus to increase vigilance: internal cues (grooming, sleep) or external cues?   external  
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Paraventricular neurons are in the hypothalamus and receives NE to trigger what type of behavior?   eating  
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NE receptors are called what? Are they metabotropic or ionotropic?   adrenoceptors. all metabotropic  
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NE alpha 1 receptors do what?   excitatory: phosphoinositide 2nd messenger system to increase Ca++  
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Describe NE alpha 2 receptor fxns.   autoreceptor and receptor. inhibitory: inhibit AC-->decrease cAMP; open K+ channels  
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Describe NE beta 1 and 2 receptors' fxn.   excitatory: stimulate AC-->increase cAMP  
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what drug selectively inhibit NE uptake?   Nisoxetine (not cocaine or methylphenidate since for all catecholamines)  
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phenylephrine   NE alpha 1 agonist  
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prazosin   NE alpha 1 antagonist  
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clonidine   NE alpha 2 agonist  
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Yohimbine   NE alpha 2 antagonist  
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albuterol   NE beta agonist, mainly beta 2  
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propanolol   NE beta antagonist  
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metoprolol   NE beta 1 antagonist  
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The raphe nucleus is for which ntm system? What are the 2 main nuclei (b7, b8)?   serotonin. b7 = dorsal RN, b8 = medial RN  
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5HT is inactivated by which enzyme? What is the metabolite?   MAO. 5-HIAA  
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Which 5HT receptor subtypes are autoreceptors?   1B, 1D  
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What does 5HT 1A receptor do? Where are 1A receptors found mostly?   inhibitory (opp from catecholamines where subtypes 1 are excitatory and 2 are inhibitory)! decrease cAMP, open K+ ch. Found in hippocampus, DORSAL raphe nucleus, amygdala, septal area.  
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What does 5HT 2A receptor do? Where are 2A receptors found mostly?   Excitatory: 2A receptor-->G protein-->PKC, increase Ca++. Found in cortex  
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Which ntm system uses PPI 2nd messenger system? which receptor subtype?   NE. alpha 1  
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para-chlorophenylalanine   5HT. (similar to AMPT in catecholamine) inhibits tryptophan hydroxylase.  
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What 2 drugs inhibit 5HT uptake?   SSRIs: fluoxetine, paroxetine  
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Paroxetine   SSRI (prevent 5HT reuptake). fluoxetine is also a SSRI.  
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para-chloroamphetamine. can it be dangerous?   increase 5HT release. yes - can be neurotoxic just like MDMA  
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MDMA   increase 5HT release. neurotoxic  
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What drug increases 5HT release at nerve terminals but is NOT neurotoxic?   fenfluramine  
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5,7-dihydroxytryptamine   5HT neurotoxin for lesioning. (similar to 6-OHDA in catecholamine system)  
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buspirone (buspar)   5HT 1A agonist --> less 5HT released, inhibitory  
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ipsapirone   5HT 1A agonist  
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8-OH-DPAT   5HT 1A agonist  
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WAY 100635   5HT 1A antagonist  
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DOI   5HT 2A agonist  
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Ketanserin   5HT 2A antagonist  
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Ritanserin   5HT 2A antagonist  
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Sumatriptan   5HT 1B/1D (autoreceptors) agonist, increase negative feedback on 5HT release (inhibitory)  
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Zolmitriptan   5HT 1B/1D (autoreceptors) agonist, increase negative feedback on 5HT release (inhibitory)  
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Ondansetron   5HT 3 antagonist  
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Granisetron   5HT 3 antagonist  
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What is the only 5HT ionotropic receptor?   5HT 3  
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What 6 regions in the striatum of the brain can ACh neurons be found?   laterodorsal nuclei, pedunculopontine tegmental nucleus; nucleus basalis, substantia innominata; medial septum, diagonal band nuclei; caudate-putamen, nucleus accumbens  
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How do mAChR work?   Inhibitory: many different mechanisms ie. PPI 2nd messenger, decrease cAMP, open K+ channels  
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Vesamicol   inhibit vesicular loading (inhibit vAChT)  
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black widow spider venom. what is a drug that has the opposite effect?   more release of ACh. botox  
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HC-3   inhibit choline (ACh) reuptake  
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physostigmine, neostigmine, pyridostigmine   inhibit AChE reversibly, increases ACh in cleft  
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What 2 nerve gases irreversibly inhibit AChE?   sarin, soman  
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nicotine   nAChR agonist (duh...)  
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What is the other nAChR agonist besides nicotine? which is the stronger drug?   succinylcholine is stronger since it can cause depolarization block  
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mecamylamine   nAChR antagonist. same as D-tubocurarine  
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D-tubocurarine   nAChR antagonist. same as mecamylamine and curare  
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muscarine   mAChR agonist (duh...)  
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arecoline   mAChR agonist. same as pilocarpine  
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pilocarpine   mAChR agonist  
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Atropine   mAChR antagonist. same as scopolamine (can treat motion sickness)  
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Scopolamine   mAChR antagonist.  
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Where can glutamatergic neurons be found? Where do they project? Is it excit or inhib?   pyramidal neurons (hippocampus), parallel fibers of cerebellum. project to striatum, brainstem, limbic system, thalamus. Excitatory  
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Glutamine-->glutamate needs what enzyme and reagents?   glutaminase. water, ATP (the only ntm synthesis that needs energy so far!)  
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What are good markers for glutamate neurons?   VGLUT1,2,3  
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How is glutamate inactivated?   By reuptake via EAAT1,2,3 into neurons (3) or astrocytes (1,2)  
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Glutamine synthetase   in astrocytes. glutmate-->glutamine  
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Do metabotropic glutamate receptors exist? If so, what mechanism(s) do they use?   Yes, mGluR1-8. PPI 2nd messenger; inhibit cAMP; autoreceptors; but note - no mention of opening K+ channels  
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What enzyme converts glutamate to GABA? What is lost (fxnal group)?   glutamic acid decarboxylase (GAD). CO2 is lost from backbone end.  
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What are GABA transporters called? What do they do? Are they also on glia?   GAT1,2,3. Reuptake GABA from cleft. Yes they are on glia and on neurons.  
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What enzyme inactivates/break down GABA? What are the final breakdown pdts? Where can this enzyme be found?   GABA-T = GABA aminotransferase. succinate, glutamate. Found in neurons and glia.  
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Glutamate and ____ neurons can be found in cerebellar cortex   Gaba  
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Where do GABA neurons in the striatum project to?   substantia nigra and globus pallidus  
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Where can GABA interneurons be found?   cortex, hippocampus  
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What are the 2 types of GABA receptors? Which one is inhibitory?   GABA a, GABA b. Both are inhibitory! B by inhibiting cAMP and opening K+ channels. A by letting in Cl- ions  
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Phenylcyclidine (PCP)   NMDA (glutamate) noncompetitive antagonist. same as ketamine  
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What are 2 noncompetitive antagonists of NMDA (glutamate)?   ketamine, pcp  
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How many subunits do GABA A receptors have? Where does BDZ bind? What about barbiturates?   5. on gamma or delta subunit. barbiturates on beta  
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What is the endogenous ligand for cannabinoid receptors?   anandamide  
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What are the endogenous ligands for opiate receptors?   endorphins, enkephalins  
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