Exam 2 Pharmacology Flashcards

1
Q

bioterpin

A

glycine transporter 1 antagonist

(increases NMDAR activity since NMDARs need glycine as a co-agonist, potential antipsychotic)

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2
Q

N-methylglycine sarcosine

A

Glycine transporter 1 antagonist

(increases NMDAR activity since NMDARs need glycine as a co-agonist, potential antipsychotic)

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3
Q

glycine, b-alanine, taurine, d and l-alanine, l-serine, d-serine

A

glycine receptor agonists

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4
Q

glycine receptor agonists

A

amino acids: glycine, b-alanine, taurine, d and l-alanine, l-serine, d-serine

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5
Q

strychnine

A

competitive glycine receptor antagonist

a convulsant and pesticide, lethal

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6
Q

picrotoxin and picrotin

A

noncompetitive inhibitors of alpha-homomeric glycine receptors and gaba a receptors

a convulsant, insecticide, antidote for barbituate poisoning in GABAA

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7
Q

cyano-triphenyl-borate (CBT)

A

noncompetitive antagonist of alpha 2 homomeric glycine receptors, use-dependent meaning it binds in the open conformation

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8
Q

vigabatrin

A

blocks gaba transaminase, meaning there is more GABA around

acts as an anticonvulsant

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9
Q

tiagabine

A

GABA transporter inhibitor

anticonvulsant

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10
Q

muscimol

A

GABA A agonist at the GABA site

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11
Q

bicuculline

A

GABAA antagonist at the GABA site

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12
Q

what do benzodiazepines, ethanol, and anaesthetics have in common

A

positive allosteric modulators of GABA A, potentiate GABA A current

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13
Q

benzodiazepines

A

potentiate the gaba a current, making it stronger

anxiolytic, anticonvulsant, sedative, alcohol detox

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14
Q

beta-carboline/ b-cce

A

inverse agonist of GABAA, binding at the benzodiazepine site

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15
Q

flumazenil

A

antagonist of GABAa at the benzodiazepine site, reverses the benzodiazepine overdose, reduces sleepiness

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16
Q

barbituates

A

bind gabaa on the beta subunit, potentiate GABAA current, sedatives/anxiolytics w/ high abuse potential

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17
Q

neurosteroids

A

allopregnanolone, ganaxalone

positive allosteric modulators of GABAa that act as anxiolytics or anticonvulsants

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18
Q

allopregnanolone, ganaxalone

A

positive allosteric modulators of GABAa that act as anxiolytics or anticonvulsants

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19
Q

anaesthetics

A

potentiate gabaA current

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20
Q

desflurane, isoflurane, sevoflurane

A

volatile anasthetics that potentiate gaba A current

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21
Q

propofol

A

intravenous anaesthetics that potentiate the GABA a current

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22
Q

ethanol

A

potentiates the GABAa current and can also weakly antagonize NMDARs

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23
Q

baclofen

A

gaba b agonist

a muscle relaxant for spastic movement disorders and maybe alcoholism

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24
Q

3-APPA

A

gabab agonist

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25
Q

phaclofen

A

gabab r antagonist

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26
Q

nAchr agonists

A

acetylcholine, nicotine, carbachol, arecoline, coniine

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27
Q

turbocurarine

A

nachr competitive reversible antagonist, active component of curare

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28
Q

varenicline

A

partial agonist at nachr receptors, helps with smoking quitting

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29
Q

mecamylmine

A

noncompetitive nachr antagonist

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30
Q

alpha-bungarotoxin

A

nachr antagonist– competitive and irreversible

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31
Q

muscarine

A

nonspecific agonist of machrs, causes salivation, sweating, tearing, diarrhea, cardiac/respiratory failure

antidote is atropine

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32
Q

muscarinic agonists

A

muscarine, arecoline, oxotremorine, carbachol, pilocarpine

33
Q

tabun and sarin

A

gas acetylcholinesterase inhibitors

34
Q

diazinon

A

ache inhibitor

35
Q

carbamates and carbamyl

A

reversible covalent ache inhibitors

36
Q

physostigmine, rivastigmine, neostigmine

A

carbamate ache inhibitors, riva used for cns but neo isnt

37
Q

galantamine

A

ache inhibitor for dementia

38
Q

tacrine

A

ache inhibitor for dementia

39
Q

donzepil

A

ache inhibitor for dementia

40
Q

atropine

A

nonspecific competitive machr antagonist that counteracts muscarine and ache inhibitor poisoning

reduces salivation and diarrhea, counteracts bradycardia

41
Q

benzatropine

A

nonspecific competitive machr antagonist, reduces parkinsonism and tremors

42
Q

ampa receptor agonists

A

ampa, quisqualate, fluorowillardiine

43
Q

quisqualate

A

ampar agonist, also group 1 mglur agonist

44
Q

fluorowillardiine

A

ampar agonist

45
Q

nbqx

A

ampar competitive antagonist

46
Q

cnqx

A

ampar competitive antagonist

47
Q

dnqx

A

ampar competitive antagonist

48
Q

quinoxaline family

A

ampar competitive antagonist– NBQX, CNQX, DNQX

49
Q

tofisopram

A

noncompetitive antagonist of AMPAr

2,3 benzodiazepine

anticonvulsant, neuroprotective

50
Q

2,3 benzodiazepines

A

noncompetitive antagonist of ampar

anticonvulsant, neuroprotective

51
Q

iem 1460, spermine, philanthotoxin 74

A

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

52
Q

cyclothiazide

A

blocks desensitization of AMPARs
a positive allosteric modulator

53
Q

ampakines

A

positive allosteric modulators of AMPA receptors. usually have CX and a number

can be nootropic

54
Q

aniracetam and piracetam

A

racetams that act as ampakines

ampakines are positive allosteric modulators of AMPA receptors

55
Q

benzylpiperidines

A

ampakines

they are positive allosteric modulators of AMPA receptors.

56
Q

families of drugs that are ampakines

A

racetams and benzylpiperdines

57
Q

cycloserine

A

partial NMDAR agonist at the glycine site

may help with cognitive symptoms of schizophrenia

58
Q

aspartic acid

A

NMDAR agonist at the glutamate site

59
Q

NMDAR agonists

A

NMDA, aspartic acid, cycloserine

60
Q

AP5

A

antagonist at glutamate site of NMDAR

61
Q

5,7 DCK

A

antagonist at glycine site of NMDAR

62
Q

MK801, Ketamine, PCP

A

use-dependent channel blockers of NMDARs

bind the open conformation, anesthetic, dissociative/hallucinogenic

63
Q

s-mcpg

A

mglur antagonist

64
Q

ACPD

A

mglur agonist for all families

65
Q

phenylglycines

A

family of mglur antagonists

66
Q

dhpg

A

group 1 mglur agonist

67
Q

mcpg

A

mglur group 1 antagonist

68
Q

aida

A

group 1 mglur antagonist

69
Q

cpccoet

A

mglur type 1 channel 1 noncompetitive antagonist

70
Q

mpep

A

mglur type 1 channel 5 noncompetitive antagonist

71
Q

mavoglurant

A

mglur type 1 channel 5 noncompetitive antagonist

failed fragile x clinical trials

72
Q

map4

A

group 2 and 3 mglur antagonist

73
Q

elgumegad and dcg iv

A

group 2 mglur agonist

addiction, anxiety, neuroprotective

74
Q

eglu, pccg4

A

group 2 mglur antagonists

75
Q

biphenylinadone A

A

positive allosteric modulator of group 2 mglur

anxiolytic, may be antipsychotic

76
Q

l-ap4

A

mglur group 3 agonist

77
Q

mppg

A

mglur group 3 antagonist

78
Q
A