778546-51-3

778546-51-3 structure

Name: A-77636
Chemical Name: (1R,3S)-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1H-isochromene-5,6-diol
CAS Number: 778546-51-3
Molecular Formula: C₂₀H₂₇NO₃
Molecular Weight: 329.43
Create Date: 2017-05-31 00:00:20
Modify Date: 2024-02-05 16:04:45
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].

Name	(1R,3S)-3-(1-adamantyl)-1-(aminomethyl)-3,4-dihydro-1H-isochromene-5,6-diol
Synonyms	Lopac-A-255 Tocris-1701

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
Target	Dopamine D1 receptor:1.1 nM (EC50) Dopamine D1 receptor:39.8 nM (Ki)
In Vivo	A-77636 (0-3.2 μmol/kg，皮下注射) 在 6-OHDA 损伤的大鼠中引发旋转行为(ED50=0.32 μmol/kg sc)[1]。 A-77636 (1-10 mg/kg) 以剂量依赖性方式减弱成瘾剂诱导的运动活动[2]。 A-77636 在大鼠 (ED50=12.3 μmol/kg s.c.) 和小鼠 (ED50=12.1 μmol/kg s.c.) 中产生前肢阵挛[1] 。在用 MPTP 处理以诱导帕金森样状态的狨猴中，A-77636 (0.5、1.0 或 2.0 μmol/kg，口服)可增加运动活性并降低帕金森样症状的严重程度：该化合物在皮下或口服给药后均有活性[1]。 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.
References	[1]. Kebabian JW, et al. A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets. Eur J Pharmacol. 1992 Dec 15;229(2-3):203-9. [2]. Chausmer AL, et al. Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents. Psychopharmacology (Berl). 2002 Jan;159(2):145-53.

Molecular Formula	C₂₀H₂₇NO₃
Molecular Weight	329.43
Exact Mass	329.19900
PSA	75.71000
LogP	3.95560

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