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131 Cards in this Set
- Front
- Back
What are the ionotropic Glutamate receptors?
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AMPAR, KAR, NRs
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What are the metabotropic Glutamate receptors?
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mGluRs
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What are the ionotropic GABA receptors?
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GABAaR and GABAcR
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What is the metabotropic GABA receptor?
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GABAb
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AMPA receptor agonists
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AMPA, glutamate, quisqualate
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AMPA receptor antagonists
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NBQX
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KAR agonists
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kainate, glutamate, domoate
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What are the binding sites for NMDA receptors?
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glutamate, glycine, Mg, PCP, and polyamine
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What are the NR agonists for the glutamate binding site?
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NMDA and glutamate
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What are the NR antagonists for the glutamate binding site?
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APV, CPP
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What are the NR agonists for the glycine binding site?
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glycine and serine
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What are the NR antagonists for the glycine binding site?
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kynurenate
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What is a partial agonist for the glycine binding site?
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DCS
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What is a noncomp. antagonist for the Mg binding site?
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Mg and memantine
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What are the noncomp. antagonist for the PCP binding site?
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PCP, Angeldustin, dextromethorphan, ketamine, MK-801
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What are the noncomp. antagonist for the polyamine binding site?
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ifenprodil
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What are the mGluR class 1 agonists?
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glutamate, quisqualate, DHPG, ACPD
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What are the mGluR class 1 antagonists?
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CPG
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What are the ionotropic cholinergic receptors?
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nicotinic ACh receptors
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How many types of nicotinic receptors are on different neurons?
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3
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What are the mGluR class 2 agonists?
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Glutamate, NAAG, APDC, DCG
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What are the mGluR class 2 antagonists?
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EthylGlu, ADED
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What are the mGluR class 3 agonists?
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glutamate, AP-4
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What are the mGluR class 3 antagonists?
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MAP4
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What are the GlyR agonists?
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glycine, alanine, taurine
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What are the GlyR antagonists?
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strychnine
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What are the GlyR noncomp. antagonists?
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picrotoxin, picrotoxinin
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What are the GABAa agonists?
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GABA, muscimol, gabaxadol
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What are the GABAa antagonists?
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bicuculline, GABAzine, picrotoxin (noncomp.), flucybene (noncomp.)
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What are the GABAb agoinsts?
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GABA, baclofen
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What are the GABAb antagonists?
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phaclofen
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What are the GABAc agonists?
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GABA, isoguvacine (partial), CACA (partial)
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What are the GABAc antagonists?
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TPMPA, picrotoxin (noncomp.)
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What are the nAChR CNS bungarotoxin insensitive agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, epibatidine, labeline
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What are the nAChR CNS bungarotoxin insensitive antagonists?
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mecamylamine, PCP(noncomp), TEA (noncomp)
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What are the nAChR CNS bungarotoxin sensitive agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, anabasine
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What are the nAChR CNS bungarotoxin sensitive antagonists?
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bungarotoxin, PCP (noncomp), TEA (noncomp), buproprion (noncomp)
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What are the nAChR autonomic ganglion agonists?
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ACh, carbachol, MeCh, bethanecol, epibatidine, DMPP
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What are the nAChR autonomic ganglion antagonists?
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k-bungarotoxin, hexamethonium, PCP (noncomp), TEA (noncomp)
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What are the nACh muscle agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, epibatidine
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What are the GABAb antagonists?
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phaclofen
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What are the GABAc agonists?
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GABA, isoguvacine (partial), CACA (partial)
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What are the GABAc antagonists?
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TPMPA, picrotoxin (noncomp.)
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What are the nAChR CNS bungarotoxin insensitive agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, epibatidine, labeline
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What are the nAChR CNS bungarotoxin insensitive antagonists?
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mecamylamine, PCP(noncomp), TEA (noncomp)
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What are the nAChR CNS bungarotoxin sensitive agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, anabasine
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What are the nAChR CNS bungarotoxin sensitive antagonists?
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bungarotoxin, PCP (noncomp), TEA (noncomp), buproprion (noncomp)
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What are the nAChR autonomic ganglion agonists?
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ACh, carbachol, MeCh, bethanecol, epibatidine, DMPP
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What are the nAChR autonomic ganglion antagonists?
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k-bungarotoxin, hexamethonium, PCP (noncomp), TEA (noncomp)
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What are the nACh muscle agonists?
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ACh, carbachol, MeCh, bethanecol, anatoxin A, epibatidine
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What are the nAChR muscle antagonists?
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decamethomium, succinylcholine, curare, PCP (noncomp), TEA (noncomp), bromoACh (suicide)
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What are the M1 mAChR agonists?
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muscarine, ACh, oxotremorine, carbachol, methacholine, pilocarpine
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What are the M1 mAChR antagonists?
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atropine, scopolamine, pirenzipine, telenzipine
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What are the M3 mAChR agonists?
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muscarine, ACh, oxotremorine, carbachol, methacholine
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What are teh M3 mAChR antagonists?
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atropine, scopolamine, DAMP
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What are the M4 mAChR agonists?
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muscarine, ACh, oxotremorine, carbachol, methacholine
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What are the M4 mAChR antagonists?
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atropine, scopolamine, tropicamide
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What are the M2 mAChR agonists?
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muscarine, Ach, oxotremorine, carbachol, methacholine, bethanecol
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What are the M2 mAChR antagonists?
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atropine, scopolamine, hensamine, penzamine, gallamine
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What are the M5 mAChR agonists?
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muscarine, ACh, oxotremorine, carbachol, methacholine
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What are the M5 mAChR antagonists?
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atropine, scopolamine
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What enzyme turns l-glutamine into l-glutamate?
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glutaminase
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What enzyme turns l-glutamate into alpha-ketoglutarate?
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aspartate aminotransferase (AA)
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What enzyme turns glutamate into GABA?
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glutamate decarboxylase (GAD)
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What enzyme turns glutamate into glutamine?
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glutamine synthase (GS)
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What NR subunit receives glycine/glutamate?
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NR1 - glycine, NR2 - glutamate
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What effect do NR agonists and antagonists have on learning and memory?
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agonists facilitate, antagonists impair.
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What are the uses/abuses of NR ligands?
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dissociative anesthesia, cough suppression, learning and memory enhancement, stroke or drowning neuroprotection, hallucinogenic induction
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What mGluRs make up class 1?
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mGluR1 and mGluR5
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Which mGluR class increases IP3 and Ca?
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Class one
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What class of mGluRs decreases cAMP?
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Class two and three
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What are mGluRs involved in?
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perception of pain, affect and mood, learning and memory, modulating activity of voltage dependent ion channels, calcium channels and ligand gated channels
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Which mGluR group uses the Gq pathway?
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group 1.
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Which mGluR group uses the Gi pathway?
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group two and three
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What is the subunit structure of GlyRs?
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pentameric, Cl channel
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Are GABAR IPSPs voltage dependent?
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yes
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What enzyme turns GABA into succinate semialdehyde?
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GABA-T
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What are the blockers of VGAT?
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nipecotate, vigabatrin
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What are the blockers of GAT-1?
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nipecotate, ACHC
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What are the blockers of GAT-2?
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nipecotate, guvacine
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What are the blockers of GAT-3?
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nipecotate
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What are the barbiturates?
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phenobarbital, pentobarbital
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What are the BDZ agonists?
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diazepam, flurazepam, bretazenil (partial), carboline (inverse)
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What are the BDZ antagonist?
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flumazenil
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What are the uses/abuses of GABAR ligands?
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sedatives, hypnotics, anxiolytics, seizure prevention, date rape
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GABAbR show an indirect activation of?
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VDKCs
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What are the organophosphate/nerve gas agent AChE antagonists?
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DFP, sarin, soman, tabun
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What are the organophosphate/insecticides?
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irreversible - DDT, long duration - diazinon, malathion, parathion
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What are the AChE inhibitors?
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long duration: donepezil, tacrine
short acting: neostigmine, physostigmine, metrifanate regenerator: obidoximine |
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What are the uses/abuses of nAChR ligands?
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treatment of motor disfunction, cognitive impairments, memory impairments, weaning from tobacco addiction, regulation of autonomic functions, induction of surgical paralysis, recreational smoking, chewing, snuff, insecticides, neurotoxins, paralytic hunting, assassination poisionings
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Uses/abuses of mAChR ligands
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salivary secretion, adjunct therapy for parkinsons, treatment for autonomic disorders, dilation of pupils, treatment of severe diarrhea, slowing of heart rate, treatment of mushroom/anti-AChE poisoning
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If a GluR2 is present, what type of glutamate receptor is seen?
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AMPA, Na channel
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What type of channel is NMDAR?
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Ca channel
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What is the QR site at the GluR2 subunit?
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Q-glutamine, NMDAR
R-aspartate, AMPA |
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What is recorded when measuring an EPSP?
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voltage
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What is the equivalent to inactivation in ligand gated channels?
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desensitization
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What type of subunit is typically seen in NRs?
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2NR1 and 2NR2 subunits
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What is the coagonist site for NRs?
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NR1- glycine site
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What is the ratio of Mg to Ca in CSF?
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3:7mM
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What is the shape of an IV curve for NRs in the presence of Mg?
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fishhook shaped
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What happens when the NR is phosphorylated?
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see a larger current flow
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What effect do mGluR group 1 agonists have on AHP?
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reduces AHP, increases neuron excitability
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What happens when PLA enzymes are activated?
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PLA acts on PI to produce arachidonic acid which is acted upon by cox enzymes to produce prostanoids that dilate blood vessels (head ache)
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What slows the rundown/desensitization of GABAaRs?
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ATP
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GABAaR mediated Cl currents are ______________ dependent.
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ligand and voltage
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Where do zolpidem and eszopiclone bind?
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omega selective ligands, on alpha subunit of GABAaR
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What are the BDZ metabolites?
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1st pass - nordazepam
2nd pass - oxazepam |
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What is unique to GABAcRs?
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found in retinal cells, rare in NS, long and sustained response to GABA, insensitive to GABA modulators, rho subunits
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How many transmembrane segments does the GABAbR have?
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14, GABAb1 and GABAb2 expressed together, obligate heterodimer
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Where is the g-protein binding site/GABA binding site on GABAbRs?
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GABAb1 - GABA binding site
GABAb2 - g-protein binding site |
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Which pathway is activated by GABAbRs?
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Gi or Go; can inhibit AC or activate PLC
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What do GABAbR agonists do to Ca channels?
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suppresses VDCC activity, p-type Ca channels
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How does phosphorylation effect GABAbRs?
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enhances beta gamma coupling to GIRKS (Slow outward K currents)
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What ion channel does the nAChR open?
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Na channel
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What does the enzyme ChAT do?
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uses acetyl CoA and choline to produce ACh and CoA
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What does the enzyme AChE do?
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breaksdown ACh into acetate and choline
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Where is the major cholinergic input to the hippocampus?
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the septum
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What is the biggest source of ACh?
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habenula
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What ion has to be present in the vesicle for the ACh transporter to work?
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H
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For every ACh molecule taken into a vesicle, how many H ions are taken out?
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2
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What ligand blocks the ACh vesicular transporter?
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vesamical
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What do GABAbR agonists do to Ca channels?
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suppresses VDCC activity, p-type Ca channels
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How does phosphorylation effect GABAbRs?
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enhances beta gamma coupling to GIRKS (Slow outward K currents)
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What ion channel does the nAChR open?
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Na channel
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What does the enzyme ChAT do?
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uses acetyl CoA and choline to produce ACh and CoA
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What does the enzyme AChE do?
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breaksdown ACh into acetate and choline
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Where is the major cholinergic input to the hippocampus?
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the septum
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What is the biggest source of ACh?
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habenula
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What ion has to be present in the vesicle for the ACh transporter to work?
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H
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For every ACh molecule taken into a vesicle, how many H ions are taken out?
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2
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What ligand blocks the ACh vesicular transporter?
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vesamical
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