Serotonergic Drugs

Question 1

What is serotonin made from

Answer 1

Tryptophan => converted to serotonin

Question 2

Inhibitory receptors of serotonin at synapse

Answer 2

1. 5HT 1A 1B 1D
   = G COUPLED RECEPTOR
2. 5HT 2A 2B 2C
   = Gq receptors
3. Channel 5HT3
   = cation channels = conducts na and ca
   = forms a CYS-loop nicotinic acetylchomine receptor

Question 3

Stimulatory serotonergic receptors qt synapse

Answer 3

5HT 4 6 7
5HT 5

Question 4

SAR of triptans

Answer 4

1. Aromatic ring (indole)
2. Protonated nitrogen
3. Large substation at 5 position of indole ring
4. Amphipathic - both lipophilic and hydropholic characteristics
5. Electron withdrawing group on C2 position

Question 5

How does SUMATRIPTAN WORK?

Answer 5

5HT B/D/F agonists

BINDING AT
5HT 1B = constricts blood vessels

5HT 1D = inhibits release of calcitonin gene-related peptide

Question 6

Relation of neuropeptides (calcitonin gene related peptide) and MIGRAINES

Answer 6

CGRP increases during a migraine

Question 7

How does Humanised Antibody Therapy = ERENUMAB work?

Answer 7

Competes with CGRP for the receptor-