A-77636
Modify Date: 2024-02-05 16:04:45
A-77636 structure
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Common Name | A-77636 | ||
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| CAS Number | 778546-51-3 | Molecular Weight | 329.43 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H27NO3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of A-77636A-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 |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C20H27NO3 |
|---|---|
| Molecular Weight | 329.43 |
| Exact Mass | 329.19900 |
| PSA | 75.71000 |
| LogP | 3.95560 |
| Lopac-A-255 |
| Tocris-1701 |