A77636hydrochloride , ≥98% , 145307-34-2

Synonym(s):
(−)-(1R,3S)-3-Adamantyl-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyran hydrochloride hydrate

CAS NO.：145307-34-2

Empirical Formula: C20H28ClNO3

Molecular Weight: 365.89

MDL number: MFCD03107804

PRODUCT Properties

• storage temp.: −20°C
• solubility: H₂O: 10 mg/mL
• form: solid
• color: off-white
• Water Solubility: Soluble to 100 mM in water
• InChIKey: KNACNUUSUYTFDY-LIWDBWMRSA-N
• SMILES: O.Cl.NC[C@@H]1O[C@@H](Cc2c(O)c(O)ccc12)C34CC5CC(CC(C5)C3)C4

Description and Uses

A-77636 is a dopamine D₁ receptor agonist (K_i = 40 nM). It induces activity equal to or greater than dopamine 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 D_1A 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 .

The dopamine receptors play important role in cognition, memory, learning, and motor control (1). These receptors have been implicated as a therapeutic target for many psychiatric and neurological disorders. A 77636 Hydrochloride is a selective dopamine D1-like receptor agonist with antiparkinsonian properties (2,3).

Safety

• PPE: Eyeshields, Gloves, type N95 (US)
• WGK Germany: 3
• Storage Class: 11 - Combustible Solids