Receptors
5-HT receptors are all G-protein coupled receptors (GPCR) except for 5-HT3 which is a ligand gated ion channel. The receptors that have been found to be involved in migraine are 5-HT1B, 5-HT1D and 5-HT1F receptors. 5-HT1B are found in meningeal arteries, agonism of 5-HT1B causes vasoconstriction in cranial nerves. The 5-HT1D receptors are located primarily in the trigeminal nerve in the central nervous system (CNS). They are also found in vascular smooth muscles, mediating contraction. Agonism of 5-HT1D receptors subdues the release of inflammatory inducing nerve stimulants. The amino acids contributing to the binding of ligands to the receptor are aspartic acid (Asp), phenylalanine (Phe), serine (Ser), threonine (Thr), tryptophan (Trp) and tyrosine (Tyr). It has been shown that both 5-HT1B and 5-HT1D receptors in humans have a very similar amino acids structures which demonstrates the similarities in binding properties.
Read more about this topic: Discovery And Development Of Triptans
Famous quotes containing the word receptors:
“Our talk of external things, our very notion of things, is just a conceptual apparatus that helps us to foresee and control the triggerings of our sensory receptors in the light of previous triggering of our sensory receptors.”
—Willard Van Orman Quine (b. 1908)