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Neuro_Week1 > 11- CNS neuropharm > Flashcards

11- CNS neuropharm Flashcards

1
Q

Precursors and key enzymes for synthesis of

ACh

A

Acetyl CoA + choline – CAT –> ACh + CoA

enzyme = CAT = choline acetyl transferase

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2
Q

Precursors and key enzymes for synthesis of

Serotonin

A

Tryptophan – TrpH –> 5-OH-Trp –AAADec –> 5-HT

TrypH = tryptophan hydroxylase
AAADec = L-aromatic AA decarboxylase
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3
Q

Precursors and key enzymes for synthesis of

catecholamines

A

Tyr – TH –> L-Dopa – DopaDec –> Dopamine – DBH –> NE – PMNT –> Epi

TH = tyrosine hydroxylase
DopaDec = Dopa decarboxylase
DBH = dopamine beta hydroxylase
PNMT

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4
Q

Precursors and key enzymes for synthesis of

AA transmitter (GABA)

A

Glutamate –GAD –> GABA

GAD = glutamic acid decarboxylase

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5
Q

Precursors and key enzymes for synthesis of

AA transmitter (glutamate)

A

Glutamine – glutaminasse –> glutamate

glutaminase

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6
Q

Precursors and key enzymes for synthesis of

opioid peptides

A

synthesized in neuronal soma via mRNA synth on ribosomes

neuropeptides then cleaved to active form by proteolytic enzymes

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7
Q

Inactivation at synpase

ACh

A

enzymatic degradation by AChE

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8
Q

Inactivation at synpase
where take place

serotonin

A

reuptake via serotonin transporter (SEERT) then degradation by two enzymes (MAO A then aldehyde dehydrogenase)

Degradation in neuron

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9
Q

Inactivation at synpase
where take place

catecholamines

A

reuptake by membrane transporters (DAT or NET) then degradation by MAO or COMT

in neuron or liver

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10
Q

Inactivation at synpase

GABA

A

reuptake by GABA transporter

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11
Q

Inactivation at synpase

glutamate

A

1) reuptake by neuronal glutamate transporter
OR
2) taken up by glial cell transproter –> convert to glutamine by glutamine synthetase –> glutamine then taken up by neuron for conversion to glutamate by glutaminase

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12
Q

Inactivation at synpase

opioid peptides

A

enzymatic cleavage into fragments inactive by peptidases (metalloendopeptidase and aminopeptidase-N)

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13
Q

potentiate effects of NT by

A

potentiate effects of NT by

1) stim release of NT
2) block reuptake
3) block metab
4) agonist to receptor

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14
Q

decr activity of NT by

A

decrease activity of NT

1) interfere with vesicular storage
2) block release
3) block receptor

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15
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

ACh
muscarinic antagonists
Nicotinic agonists

A

muscarinic antagonists for Parkinson’s disease

Nicotinic agonists for smoking cessation and schizo

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16
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
Tyr hydroxylase inhib f

A

Tyr hydroxylase inhib for pheochromocytoma

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17
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
Storage inhib

A

Storage inhib for schizo

18
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
Dopamine releasers

A

Dopamine releasers for ADHD

19
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines

Dopamine/NE reuptake inhib

A

Dopamine/NE reuptake inhib for depression

20
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines

MAOI

A

MAOI for depression and Parkinson’s

21
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines

COMT inhib

A

COMT inhib for Parkinson’s

22
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
Alpha1 and alpha2 agonists

A

Alpha1 and alpha2 agonists for ADHD

23
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
Beta antagonists

A

Beta antagonists for anxiety

24
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines

D2 dopamine receptor agonists

A

D2 dopamine receptor agonists for Parkinson’s and restless leg syndrome

25
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines
D2 dopamine receptor antag for

A

D2 dopamine receptor antag for schizo

26
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

Catecholamines

Partial dopaminergic agonist

A

Partial dopaminergic agonist in schizo

27
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

5-HT1A receptor partial agonists for

28
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

5-HT 2 receptor antagonists for

29
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

5-HT-1D agonists for

30
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

GABA agonists (benzo and others) for

A

sleep disorders
anxiety disorders
muscle spasticity in neuro disorders

31
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

glutamate
NMDA antaonists for

A

Alzheimer’s and pain management

32
Q

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder

opioids
receptor agonists for

A

pain treatment

33
Q

receptor transduction mechanisms

GABA A

A

opens ligand gated Cl- channel

IPSP (ionotropic)

34
Q

receptor transduction mechanisms

GABAB

A

Gi/o
inhib AC
decr Ca2+ conduction
open K+ channel

35
Q

receptor transduction mechanisms

NMDA
AMPA
Kainate

A

incr Ca2+ influx

incr Na and Ca influx

incr Na influx

36
Q

receptor transduction mechanisms

metabotropic receptors
R1-R5
R2-R3
R4-R6-R7-R8

A

R1-R5 = Gq –> incr PLC ctivity

R2-R3 (Gi/o –> decr AC activity –> inhib VSCC- activ K+ channels)

R4-R6-R7-R8 –> G/o –> decr AC activity –> inhib VSCC

37
Q

receptor transduction mechanisms

M1-M3; Gq

M2-M4; Gi/o

Nictonic receptors Nn

A

stim PLC activity

inhib AC activity

open receptor gated cation channel

38
Q

receptor transduction mechanisms
NE

alpha1 adrenergic
alpha2 adrenergic
B1 adrenergic
b2 adrenergic

A

alpha 1 = Gq –> PLC
alpha2 = Gi/o –> inhib AC activity, open K+ channel
Beta1 = Gs –> stim AC
Beta2 = Gs –> stim AC

39
Q

receptor transduction mechanisms
dopamine

D1
D2

A 
D1 = Gs --> stim AC
D2 = Gi/o --> inhib AC
40
Q

receptor transduction mechanisms
serotonin

5HT 1A, 1B, 1D
5HT 2A, 2B, 2C
5HT 3
5HT 4

A

5HT 1A, 1B, 1D = Gi/o = inhib AC , open K+ channel

5HT 2A, 2B, 2C = Gq = stim PLC = close Ca2+ channel

5HT 3 = ligand gated ion channel = excitatory

5HT 4 = stim AC activity

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