Metergoline

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. It blocks 5-HT7 receptor-stimulated cAMP production (IC50 = 321 nM) in HEK293 cells. 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. Formulations containing metergoline have been studied for the treatment of hormone dysfunction, seasonal affective disorder, and anxiety.Formal Name: N-[[(8beta)-1,6-dimethylergolin-8-yl]methyl]-carbamic acid, phenylmethyl ester. CAS Number: 17692-51-2. Molecular Formula: C25H29N3O2. Formula Weight: 403.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 25 mg/ml, Ethanol: 5 mg/ml. lambdamax: 226, 289 nm. SMILES: CN1C2=CC=CC([C@@]3([H])C[C@@H](CNC(OCC4=CC=CC=C4)=O)CN(C)[C@]3([H])C5)=C2C5=C1. InChi Code: InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1. InChi Key: WZHJKEUHNJHDLS-QTGUNEKASA-N.