产品描述:
Metergoline is a serotonin (5-HT) receptor antagonist that is active at 5-HT1 (pKi = 7.8 for 5-HT1B), 5-HT2, (pKi = 8.64, 8.75, and 8.75 for 5-HT2A, 5-HT2B, and 5-HT2C respectively), and 5-HT7 receptor subtypes.{41065,41063} It blocks 5-HT7 receptor-stimulated cAMP production (IC50 = 321 nM) in HEK293 cells.{34420} Metergoline has been widely used to study serotonin receptor function, but it also dose-dependently inhibits voltage-dependent sodium and potassium channels transfected into Xenopus oocytes.{34421,41064} Formulations containing metergoline have been studied for the treatment of hormone dysfunction, seasonal affective disorder, and anxiety.{34421}