Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
性状
Solid
IC50 & Target[1][2]
5-HT2A Receptor
8.64 (pKi)
5-HT2B Receptor
8.75 (pKi)
5-HT2C Receptor
8.75 (pKi)
Human 5-HT7 Receptor
16 nM (Ki)
体外研究(In Vitro)
Metergoline (3 μM) causes a 6.8±1.2 mV depolarizing shift of the steady-state activation curve of the Nacurrents, and does not alter the inactivation curve.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male albino mice (25-40 g)
Dosage:
5 mg/kg
Administration:
Intraperitoneal injection
Result:
Inhibited bites or scratches induced by 5-HT (2 μg).