11- CNS neuropharm

Question 1

Precursors and key enzymes for synthesis of

ACh

Answer 1

Acetyl CoA + choline – CAT –> ACh + CoA

enzyme = CAT = choline acetyl transferase

Question 2

Precursors and key enzymes for synthesis of

Serotonin

Answer 2

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

TrypH = tryptophan hydroxylase
AAADec = L-aromatic AA decarboxylase

Question 3

Precursors and key enzymes for synthesis of

catecholamines

Answer 3

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

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

Question 4

Precursors and key enzymes for synthesis of

AA transmitter (GABA)

Answer 4

Glutamate –GAD –> GABA

GAD = glutamic acid decarboxylase

Question 5

Precursors and key enzymes for synthesis of

AA transmitter (glutamate)

Answer 5

Glutamine – glutaminasse –> glutamate

glutaminase

Question 6

Precursors and key enzymes for synthesis of

opioid peptides

Answer 6

synthesized in neuronal soma via mRNA synth on ribosomes

neuropeptides then cleaved to active form by proteolytic enzymes

Question 7

Inactivation at synpase

ACh

Answer 7

enzymatic degradation by AChE

Question 8

Inactivation at synpase
where take place

serotonin

Answer 8

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

Degradation in neuron

Question 9

Inactivation at synpase
where take place

catecholamines

Answer 9

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

in neuron or liver

Question 10

Inactivation at synpase

GABA

Answer 10

reuptake by GABA transporter

Question 11

Inactivation at synpase

glutamate

Answer 11

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

Question 12

Inactivation at synpase

opioid peptides

Answer 12

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

Question 13

potentiate effects of NT by

Answer 13

potentiate effects of NT by

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

Question 14

decr activity of NT by

Answer 14

decrease activity of NT

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

Question 15

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

ACh
muscarinic antagonists
Nicotinic agonists

Answer 15

muscarinic antagonists for Parkinson’s disease

Nicotinic agonists for smoking cessation and schizo

Question 16

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

Catecholamines
Tyr hydroxylase inhib f

Answer 16

Tyr hydroxylase inhib for pheochromocytoma

Question 17

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

Catecholamines
Storage inhib

Answer 17

Storage inhib for schizo

Question 18

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

Catecholamines
Dopamine releasers

Answer 18

Dopamine releasers for ADHD

Question 19

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

Catecholamines

Dopamine/NE reuptake inhib

Answer 19

Dopamine/NE reuptake inhib for depression

Question 20

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

Catecholamines

MAOI

Answer 20

MAOI for depression and Parkinson’s

Question 21

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

Catecholamines

COMT inhib

Answer 21

COMT inhib for Parkinson’s

Question 22

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

Catecholamines
Alpha1 and alpha2 agonists

Answer 22

Alpha1 and alpha2 agonists for ADHD

Question 23

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

Catecholamines
Beta antagonists

Answer 23

Beta antagonists for anxiety

Question 24

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

Catecholamines

D2 dopamine receptor agonists

Answer 24

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

Question 25

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder Catecholamines D2 dopamine receptor antag for

Answer 25

D2 dopamine receptor antag for schizo

Question 26

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder Catecholamines Partial dopaminergic agonist

Answer 26

Partial dopaminergic agonist in schizo

Question 27

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder 5-HT1A receptor partial agonists for

Answer 27

anxiety

Question 28

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder 5-HT 2 receptor antagonists for

Answer 28

schizo

Question 29

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder 5-HT-1D agonists for

Answer 29

migraines

Question 30

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder GABA agonists (benzo and others) for

Answer 30

sleep disorders anxiety disorders muscle spasticity in neuro disorders

Question 31

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder glutamate NMDA antaonists for

Answer 31

Alzheimer's and pain management

Question 32

Relate drug action at molecular targets at the synapse to pharmacologic responses in various CNS disorder opioids receptor agonists for

Answer 32

pain treatment

Question 33

receptor transduction mechanisms | GABA A

Answer 33

opens ligand gated Cl- channel | IPSP (ionotropic)

Question 34

receptor transduction mechanisms GABAB

Answer 34

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

Question 35

receptor transduction mechanisms NMDA AMPA Kainate

Answer 35

incr Ca2+ influx incr Na and Ca influx incr Na influx

Question 36

receptor transduction mechanisms metabotropic receptors R1-R5 R2-R3 R4-R6-R7-R8

Answer 36

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

Question 37

receptor transduction mechanisms M1-M3; Gq M2-M4; Gi/o Nictonic receptors Nn

Answer 37

stim PLC activity inhib AC activity open receptor gated cation channel

Question 38

receptor transduction mechanisms NE alpha1 adrenergic alpha2 adrenergic B1 adrenergic b2 adrenergic

Answer 38

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

Question 39

receptor transduction mechanisms dopamine D1 D2

Answer 39

``` D1 = Gs --> stim AC D2 = Gi/o --> inhib AC ```

Question 40

receptor transduction mechanisms serotonin 5HT 1A, 1B, 1D 5HT 2A, 2B, 2C 5HT 3 5HT 4

Answer 40

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