1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. A-77636

A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.

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A-77636 Chemical Structure

A-77636 Chemical Structure

CAS No. : 778546-51-3

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Description

A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity[1].

IC50 & Target

Dopamine D1 receptor

1.1 nM (EC50)

Dopamine D1 receptor

39.8 nM (Ki)

In Vivo

A-77636 (0-3.2 μmol/kg, Subcutaneously) elicits rotational behavior in 6-OHDA-lesioned rats (ED50=0.32 μmol/kg s.c.)[1].
A-77636 (1-10 mg/kg) attenuates addiction-induced locomotor activity in a dose-dependent manner[2].
A-77636 produce forelimb clonus in rats (ED50=12.3 μmol/kg s.c.) and mice (ED50=12.1 μmol/kg s.c.)[1].
In marmosets treated with MPTP to induce a parkinsonian-like state, A-77636 (0.5, 1.0 or 2.0 μmol/kg, p.o.) increases locomotor activity and decreases the severity of the parkinsonian-like symptoms: the compound is active after either subcutaneous or oral administration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigrostriatal pathway (six/group)[1]
Dosage: 0.32, 1.0, 3.2 μmol/kg
Administration: Subcutaneously
Result: Elicited prolonged (> 20 h) contralateral turning, which was blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor.
Animal Model: Male Swiss Webster mice (18-25 g, five or six per cage)[2]
Dosage: 1, 3, 10 mg/kg
Administration:
Result: Attenuated addiction-induced locomotor activity in a dose-dependent manner. When administered alone, 1 and 3 mg/kg A-77636 produced little change in locomotor activity, whereas 10 mg/kg produced a significant and substantial decrease in locomotor activity.
Molecular Weight

329.43

Formula

C20H27NO3

CAS No.
SMILES

NC[C@@H]1O[C@H](C2(C[C@@H]3C4)C[C@H](C3)C[C@H]4C2)CC5=C(O)C(O)=CC=C51

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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A-77636 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
A-77636
Cat. No.:
HY-141496
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