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A-77636 

Cat. No. M30602
A-77636  Structure
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 329.43
Formula C20H27NO3
CAS Number 778546-51-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yvonne Connolly Martin. Int J Med Chem. The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

[2] Steven J Cooper, et al. Eur J Pharmacol. The anorectic effect of the selective dopamine D1-receptor agonist A-77636 determined by meal pattern analysis in free-feeding rats

[3] R K Pearce, et al. Psychopharmacology (Berl). Actions of the D1 agonists A-77636 and A-86929 on locomotion and dyskinesia in MPTP-treated L-dopa-primed common marmosets

[4] C W Lin, et al. J Pharmacol Exp Ther. Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636

[5] J W Kebabian, et al. Eur J Pharmacol. A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets

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