プロパティ

安全情報(bào)

説明

Methysergide is an agonist of the serotonin (5-HT) receptor subtype 5-HT₁ and an antagonist of 5-HT₂ receptors. It binds to recombinant human 5-HT_1A (K_D = 23.44 nM), 5-HT_1E (K_i = 229.09 nM), 5-HT_1F (K_i = 33.88 nM), and rodent 5-HT_1B receptors (K_D = 1,513.56 nM). It also binds to recombinant human 5-HT_2A (K_i = 2.69 nM) and 5-HT_2C receptors (K_D = 1.26 nM) and is an insurmountable antagonist at 5-HT_2B receptors. It inhibits vasoconstriction induced by 5-HT in isolated postmortem human basilar arterial spiral strips (pA₂ = 8.07). Methysergide decreases external carotid blood flow in a dose-dependent manner in vagosympathectomized dogs, an effect that is inhibited by the 5-HT_1B/1D receptor antagonist GR127935 . It has antinociceptive activity in mouse models of pain induced by intrathecal injection of substance P , glutamate, NMDA , AMPA , or kainic acid. Methysergide reduces zymosan-induced paw edema in rats when administered at a dose of 10 mg/kg. Formulations containing methysergide were previously used in the prevention and treatment of vascular headaches.