Neuropharamcology

Question 1

What are cotransmitters in the SNS?

Answer 1

ATP, galanin, neuropeptide Y

Question 2

What is the RLS in neurotransmitter production?

Answer 2

Tyrosine–>Dopa via tyrosine hydroxylase. Can be up or down regulated by stress levels

Question 3

What enzyme converts norepinephrine to epinephrine? What upregulates this enzyme?

Answer 3

Phenylethanolamine N methyltransferase (PNMT). GCs from the adrenal cortex upregulate the enzyme (ie stress)

Question 4

How does the adrenal medulla come into play with NTs?

Answer 4

Adrenal medulla has two types of cells. Those with PNMT and those without. NE diffuses from granules in the medulla, gets methylated in the cytoplasm, then re-enters granules as epinephrine.

Question 5

What pump takes up catecholamines in cytoplasm and puts them in vesicles?

Answer 5

VMAT

Question 6

What is calcium’s role in NT release?

Answer 6

Interacts with VAMPs triggering fusion of the vesicle and ell membrane

Question 7

GCPRs alpha and beta and their G proteins…

Answer 7

Alpha 1: Gq
Alpha 2: Gi
Beta 1&2: Gs

Question 8

What are the factors determining actions of sympathomimetic amines?

Answer 8

1. Potency
   - NE and E are very potent in activation of alpha/beta
2. Proportion and density of receptors
   - More there are, more response will have
3. Reflex or homeostatic adjustments
   - Brain says calm down
4. Refractoriness/desensitization of the receptor
   - Either beta arrestin causes receptor to be internalized or the ligand to lose its affinity for the receptor

Question 9

Describe the NT reuptake systems

Answer 9

Uptake 1:

• NT reuptake into nerve endings
• Saturated easily
• High affinity, low capacity

Uptake 2:

• NT reuptake into extra-neuronal areas
• Low-affinity, high capacity

Question 10

Alpha-methyldopa

Answer 10

Drug that inhibits LAAD (dopa–>dopamine blocked)

Question 11

Carbidopa

Answer 11

Drug that inhibits LAAD in the periphery, will not cross the BBB

Question 12

Disulfiram

Answer 12

Inhibits dopamine beta hydroxylase (dopamine to NE) and inhibits ALDH

Question 13

Reserpine

Answer 13

Blocks VMAT uptake of dopamine into vesicle

Question 14

L-DOPA

Answer 14

Synthetic DOPA to use as precursor to dopamine in parkinson’s patients

Question 15

Bromocriptine

Answer 15

Selective agonist for D2 receptors tx for parkinson’s

Question 16

Cocaine

Answer 16

Vasoconstriction and blocks uptake 1

Question 17

Imipramine and TCAs

Answer 17

Reuptake inhibs

Question 18

Selegiline

Answer 18

MAO-B inhibitor