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