G-protein-linked receptors directly targeted by drugs

Question 1

Antagonist or partial agonist at Dopamine D2

Answer 1

Conventional antipsychotic and atypical antipsychotic creates antipsychotic and antimanic actions

Question 2

Antagonist or inverse agonist at Serotonin 5HT2A

Answer 2

Atypical antipsychotic reduces motor side effects and possibly mood stabilization/antidepressant in BPD. Antidepressant, hypnotic may improve mood and insomnia.

Question 3

Antagonist or partial agonist at Serotonin 5HT1A, 5HT1B/D, 5HT2C, 5HT6, and 5HT7

Answer 3

Atypical antipsychotic has unknown secondary receptor actions, possibly contributing to efficacy and tolerability.

Question 4

Partial agonist at Serotonin 5HT1A

Answer 4

Anxiolytic, booster of antidepressant action.

Question 5

Antagonist Norepinephrine Alpha2

Answer 5

Antidepressant.

Question 6

Agonist to Norepinephrine Alpha2

Answer 6

Antihypertensive improves cognition and behavioral disturbance in ADHD.

Question 7

Antagonist to Norepinephrine Alpha1

Answer 7

Many antipsychotics and antidepressants have side effects of orthostatic hypotension and sedation.

Question 8

Agonist to GABA (GABAb)

Answer 8

Gamma hydroxybutyrate/sodium oxybate to treat cataplexy, sleepiness in narcolepsy, and may enhance slow-wave sleep and pain reduction.

Question 9

Agonist to Melatonin MT1 and MT2

Answer 9

Hypnotic to improve insomnia.

Question 10

Antagonist to Histamine H1

Answer 10

Many antipsychotics and antidepressants, some anxiolytics with therapeutic effects for anxiety and insomnia. May have side effects of sedation and weight gain.

Question 11

Antagonist to acetylcholine M1

Answer 11

Many antipsychotics and antidepressants with side effects of memory disturbance, sedation, dry mouth, blurred vision, constipation, urinary retention.

Question 12

Antagonist to acetylcholine M3/M5

Answer 12

Some atypical antipsychotics which may contribute to metabolic dysregulation (dyslipidemia and diabetes).