An agonist of the dopamine D1 receptor (Ki=40 nM); induces activity equal to or greater than dopamine in fish retinas and rat caudate-putman (EC50s = 7.4 and 1.1 nM

A-77636 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
145307-34-2
Storage:
-20
UN-No:
Non-Hazardous - /

A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM).{40976} It induces activity equal to or greater than dopamine (Item No. 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.{40977} 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.{40976} Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg.{40978} 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 (Item No. 15631).  

 

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Description

An agonist of the dopamine D1 receptor (Ki=40 nM); induces activity equal to or greater than dopamine in fish retinas and rat caudate-putman (EC50s = 7.4 and 1.1 nM, respectively); does not show agonist behavior for the D2 receptor expressed in MMQ cells (≤10 μM); induces desensitization of dopamine-stimulated cAMP accumulation and reduces D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors (10 μM); increases locomotor activity 5.3-fold and reduces disease severity in a MPTP-treated marmoset model of Parkinson’s disease (3 μmol/kg s.c.); elicits over a 230% increase in cortical and hippocampal acetylcholine release (4 μmol/kg, s.c.)

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

Synonyms: 

Molecular weight: 365.9

CAS: 145307-34-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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