A-77636,778546-51-3

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A-77636

CAS No. : 778546-51-3

MCE 国际站：A-77636

产品活性：A-77636 是一种口服有效的、选择性的长效 多巴胺 D1 受体 激动剂 (pEC50 = 8.13; EC50 = 1.1 nM)。A-77636 对多巴胺 D1 受体显示出最高的亲和力 (pKi = 7.40 ± 0.09；Ki = 39.8 nM)。A-77636 具有抗帕金森病活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

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.).
A-77636 (1-10 mg/kg) attenuates addiction-induced locomotor activity in a dose-dependent manner.
A-77636 produce forelimb clonus in rats (ED₅₀=12.3 μmol/kg s.c.) and mice (ED₅₀=12.1 μmol/kg s.c.).
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.

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