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A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | 1.444 € | 6-8 weeks | |
50 mg | 1.881 € | 6-8 weeks | |
100 mg | 2.375 € | 6-8 weeks |
Description | A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1]. |
Targets&IC50 | D1 receptor:1.1 nM (EC50), D1 receptor:39.8 nM (Ki) |
In vivo | A-77636 (0-3.2 μmol/kg, subcutaneous injection) induced rotational behavior in rats with 6-OHDA lesions (ED50 = 0.32 μmol/kg sc) [1], attenuated drug-induced locomotor activity in a dose-dependent manner (1-10 mg/kg) [2], and elicited forelimb clonus in rats (ED50 = 12.3 μmol/kg s.c.) and mice (ED50 = 12.1 μmol/kg s.c.) [1]. In MPTP-treated marmosets, A-77636 (0.5, 1.0, or 2.0 μmol/kg, oral administration) increased motor activity and reduced Parkinsonian symptoms, demonstrating efficacy with both subcutaneous and oral administration [1]. |
Molecular Weight | 329.43 |
Formula | C20H27NO3 |
Cas No. | 778546-51-3 |
Storage | Shipping with blue ice. |
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