5-HT1D agonists

Figure 4.1 5-HT1D agonists and PGD2 receptor antagonist.

Cutler, N., Gomez-Mancilla, B., Leibowitz, M., Fleishaker, J. A study of safety and efficacy in patients with acute migraine, using PNU-142633, a selective 5-HT1D agonist, Cephalalgia 2000, 20, 268. 

Sumatriptan and the other triptans are selective agonists for 5-HT1D and 5-HT1B receptors the similarity of the triptan structure to that of the 5-HT nucleus can be seen in the structure below. These receptor types are found in cerebral and meningeal vessels and mediate vasoconstriction. They are also found on neurons and probably function as presynaptic inhibitory receptors. 

Schoeffier P, Hoyer D. Interaction of the alpha-adrenoceptor agonist oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HTlc and 5-HT1D receptors. Eur J Pharmacol 1991 196 213-216. 

MacLeod AM, Street LJ, Reeve AJ, et al. Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem 1997 40 3501-3503. 

Migraine 5-HT1D/1B receptor agonist Croscarmellose sodium, hypromellose, lactose, magnesium stearate, MCC GSK... 

Sumatriptan is a serotonin agonist, acting at 5-HT1D receptors. 

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