Drugs - receptor/NT association

Question 1

Amphetamines

Answer 1

Postsynaptic D1
Postsynaptic a2a

*Also increases NE/DA vesicular release

(inhibit NE/DA reuptake)

Question 2

Methylphenidate and dexmethylphenidate

Answer 2

Postsynaptic D1
Postsynaptic a2a

(inhibit NE/DA reuptake)

Question 3

Atomoxetine

Answer 3

Presynaptic NE transporter

inhibits NE reuptake

Question 4

Guanfacine and clonidine

Answer 4

Postsynaptic a2a

improves signaling

Question 5

Methadone (binding action)

Answer 5

Full agonist

Question 6

Buprenorphine (binding action)

Answer 6

Partial agonist

Question 7

Naltrexone (binding action)

Answer 7

Full antagonist

Question 8

First gen antipsychotics

Answer 8

Non-selective D2 receptor antagonist

(increases DA in mesolimbic AND mesocortical pathways)

(also anti-H1.A1.M)

Question 9

Second gen antipsychotics

Answer 9

D2 antagonism
5HT2A antagonism

(increases DA in mesolimbic; increases serotonin in mesocortical –> increase DA activity)

(also anti-H1.A1.M)

Question 10

Lithium

Answer 10

Unknown MOA

• Increased 5HT action/release; attenuation of NE

AE from:

• reduced IP3/DAG
• inhibited adenyl cyclase
• uncoupled G proteins (TSH, vasopressin)

Question 11

SSRIs

Answer 11

Potent inhibition of presynaptic 5HT transporter

subsequent serotonin binding to 5HT1A in prefrontal cortex, hippocampus, and amygdala mediates therapeutic effects

Question 12

Vilazodone

Answer 12

Two actions:

• SSRI action: potent inhibition of presynaptic 5HT transporter
• Partial 5HT1A agonist (both mixed-action “V” antidepressants agonize this receptor)

Question 13

Vortioxetine

Answer 13

Three actions:
(vorTIOexetine = vor TRIO exetine = 3 actions)

• SSRI action: potent inhibition of presynaptic 5HT transporter
• Partial 5HT1A agonist (both mixed-action “V” antidepressants agonize this receptor)
• 5HT3 antagonist (3rd action)

Question 14

Trazodone

Answer 14

3 actions:

• SSRI action: potent inhibition of presynaptic 5HT transporter
• 5HT2a antagonist
• H1 agonist

Question 15

SNRIs

Answer 15

Inhibits reuptake of serotonin and NE

• Postsynaptic a1A
• Postsynaptic 5HT1A

Question 16

Mirtazapine

Answer 16

NaSSA:

• Presynaptic a2 antagonist
  (increases NE/serotonin release)
• Blocks a bunch of postsynaptic receptors (= fewer AE)

Question 17

Bupropion

Answer 17

Weakly inhibits reuptake of NE/DA

maybe enhances NE/DA release - presynaptic

Question 18

TCAs

Answer 18

Block reuptake of NE/5HT/both

also anti-H1.A1.M.

Question 19

MAOIs

Answer 19

• Inhibit metabolism of epi, NE, 5HT, dopamine

Question 20

Buspirone

Answer 20

• Partial 5HT1A agonist (similar to vortioxetine)

possible D2/a2 antagonist

Question 21

Benzos

Answer 21

Enhance GABA induced ionic current through channels

GABA a = ionotropic Cl conductance