| Bioactivity | 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]. |
| 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: |
| Name | A-77636 |
| CAS | 778546-51-3 |
| Formula | C20H27NO3 |
| Molar Mass | 329.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |