Sumatriptan is a tryptamine agonist at 5-HT1B/1D receptors that is clinically used to treat migraines. Sumatriptan exhibits vasoconstrictive and gastrointestinal motility modulating activities. The anti-migraine activity of sumatriptan is likely due to its vasoconstrictive activity and ability to decrease the release of substance P and CGRP. Sumatriptan also increases gastric relaxation and delays gastric emptying. Additionally, this compound inhibits 5-HT- and capsaicin-induced signaling of transient receptor potential vanilloid (TRPV1) channels and release of CGRP in vitro and in vivo.