A-77636 (hydrochloride)

A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM). It induces activity equal to or greater than dopamine (Cay-21992) in an adenylate cyclase assay of D1 receptor activity in fish retina and rat caudate putamen (EC50s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D2 receptors expressed in MMQ cells when used at concentrations up to 10 µM. A-77636 (10 µM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D1 receptors, reducing D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors. In a marmoset model of Parkinson's disease induced by MPTP, A-77636 (3 µmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity. Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 µmol/kg. It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 µmol/kg, an effect that is blocked by the D1 antagonist SCH 23390 (Cay-15631).Formal Name: (1R,3S)-1-(aminomethyl)-3,4-dihydro-3-tricyclo[3.3.1.13,7]dec-1-yl-1H-2-benzopyran-5,6-diol, monohydrochloride. CAS Number: 145307-34-2. Molecular Formula: C20H27NO3 . HCl. Formula Weight: 365.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, Ethanol: 33 mg/ml, Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/ml. SMILES: OC1=CC=C2C(C[C@@H](C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3)O[C@H]2CN)=C1O.Cl. InChi Code: InChI=1S/C20H27NO3.ClH/c21-10-17-14-1-2-16(22)19(23)15(14)6-18(24-17)20-7-11-3-12(8-20)5-13(4-11)9-20,/h1-2,11-13,17-18,22-23H,3-10,21H2,1H/t11-,12+,13-,17-,18-,20?,/m0./s1. InChi Key: BWHPNJVKFAPVOG-WUAVIEMVSA-N.