Exam 2 Pharmacology Flashcards
bioterpin
glycine transporter 1 antagonist
(increases NMDAR activity since NMDARs need glycine as a co-agonist, potential antipsychotic)
N-methylglycine sarcosine
Glycine transporter 1 antagonist
(increases NMDAR activity since NMDARs need glycine as a co-agonist, potential antipsychotic)
glycine, b-alanine, taurine, d and l-alanine, l-serine, d-serine
glycine receptor agonists
glycine receptor agonists
amino acids: glycine, b-alanine, taurine, d and l-alanine, l-serine, d-serine
strychnine
competitive glycine receptor antagonist
a convulsant and pesticide, lethal
picrotoxin and picrotin
noncompetitive inhibitors of alpha-homomeric glycine receptors and gaba a receptors
a convulsant, insecticide, antidote for barbituate poisoning in GABAA
cyano-triphenyl-borate (CBT)
noncompetitive antagonist of alpha 2 homomeric glycine receptors, use-dependent meaning it binds in the open conformation
vigabatrin
blocks gaba transaminase, meaning there is more GABA around
acts as an anticonvulsant
tiagabine
GABA transporter inhibitor
anticonvulsant
muscimol
GABA A agonist at the GABA site
bicuculline
GABAA antagonist at the GABA site
what do benzodiazepines, ethanol, and anaesthetics have in common
positive allosteric modulators of GABA A, potentiate GABA A current
benzodiazepines
potentiate the gaba a current, making it stronger
anxiolytic, anticonvulsant, sedative, alcohol detox
beta-carboline/ b-cce
inverse agonist of GABAA, binding at the benzodiazepine site
flumazenil
antagonist of GABAa at the benzodiazepine site, reverses the benzodiazepine overdose, reduces sleepiness
barbituates
bind gabaa on the beta subunit, potentiate GABAA current, sedatives/anxiolytics w/ high abuse potential
neurosteroids
allopregnanolone, ganaxalone
positive allosteric modulators of GABAa that act as anxiolytics or anticonvulsants
allopregnanolone, ganaxalone
positive allosteric modulators of GABAa that act as anxiolytics or anticonvulsants
anaesthetics
potentiate gabaA current
desflurane, isoflurane, sevoflurane
volatile anasthetics that potentiate gaba A current
propofol
intravenous anaesthetics that potentiate the GABA a current
ethanol
potentiates the GABAa current and can also weakly antagonize NMDARs
baclofen
gaba b agonist
a muscle relaxant for spastic movement disorders and maybe alcoholism
3-APPA
gabab agonist
phaclofen
gabab r antagonist
nAchr agonists
acetylcholine, nicotine, carbachol, arecoline, coniine
turbocurarine
nachr competitive reversible antagonist, active component of curare
varenicline
partial agonist at nachr receptors, helps with smoking quitting
mecamylmine
noncompetitive nachr antagonist
alpha-bungarotoxin
nachr antagonist– competitive and irreversible
muscarine
nonspecific agonist of machrs, causes salivation, sweating, tearing, diarrhea, cardiac/respiratory failure
antidote is atropine
muscarinic agonists
muscarine, arecoline, oxotremorine, carbachol, pilocarpine
tabun and sarin
gas acetylcholinesterase inhibitors
diazinon
ache inhibitor
carbamates and carbamyl
reversible covalent ache inhibitors
physostigmine, rivastigmine, neostigmine
carbamate ache inhibitors, riva used for cns but neo isnt
galantamine
ache inhibitor for dementia
tacrine
ache inhibitor for dementia
donzepil
ache inhibitor for dementia
atropine
nonspecific competitive machr antagonist that counteracts muscarine and ache inhibitor poisoning
reduces salivation and diarrhea, counteracts bradycardia
benzatropine
nonspecific competitive machr antagonist, reduces parkinsonism and tremors
ampa receptor agonists
ampa, quisqualate, fluorowillardiine
quisqualate
ampar agonist, also group 1 mglur agonist
fluorowillardiine
ampar agonist
nbqx
ampar competitive antagonist
cnqx
ampar competitive antagonist
dnqx
ampar competitive antagonist
quinoxaline family
ampar competitive antagonist– NBQX, CNQX, DNQX
tofisopram
noncompetitive antagonist of AMPAr
2,3 benzodiazepine
anticonvulsant, neuroprotective
2,3 benzodiazepines
noncompetitive antagonist of ampar
anticonvulsant, neuroprotective
iem 1460, spermine, philanthotoxin 74
bind glua2 lacking ampars, which can pass calcium
they block the ampa4 calcium current, and spermine helps give inward rectification to potassium channels
this is important because we can compare calcium passing and noncalcium passing channels
cyclothiazide
blocks desensitization of AMPARs
a positive allosteric modulator
ampakines
positive allosteric modulators of AMPA receptors. usually have CX and a number
can be nootropic
aniracetam and piracetam
racetams that act as ampakines
ampakines are positive allosteric modulators of AMPA receptors
benzylpiperidines
ampakines
they are positive allosteric modulators of AMPA receptors.
families of drugs that are ampakines
racetams and benzylpiperdines
cycloserine
partial NMDAR agonist at the glycine site
may help with cognitive symptoms of schizophrenia
aspartic acid
NMDAR agonist at the glutamate site
NMDAR agonists
NMDA, aspartic acid, cycloserine
AP5
antagonist at glutamate site of NMDAR
5,7 DCK
antagonist at glycine site of NMDAR
MK801, Ketamine, PCP
use-dependent channel blockers of NMDARs
bind the open conformation, anesthetic, dissociative/hallucinogenic
s-mcpg
mglur antagonist
ACPD
mglur agonist for all families
phenylglycines
family of mglur antagonists
dhpg
group 1 mglur agonist
mcpg
mglur group 1 antagonist
aida
group 1 mglur antagonist
cpccoet
mglur type 1 channel 1 noncompetitive antagonist
mpep
mglur type 1 channel 5 noncompetitive antagonist
mavoglurant
mglur type 1 channel 5 noncompetitive antagonist
failed fragile x clinical trials
map4
group 2 and 3 mglur antagonist
elgumegad and dcg iv
group 2 mglur agonist
addiction, anxiety, neuroprotective
eglu, pccg4
group 2 mglur antagonists
biphenylinadone A
positive allosteric modulator of group 2 mglur
anxiolytic, may be antipsychotic
l-ap4
mglur group 3 agonist
mppg
mglur group 3 antagonist