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A 77636 hydrochloride

Cat. No. M6372
A 77636 hydrochloride Structure
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10mg USD 460  USD460 Custom Synthesis
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Quality Control & Documentation
Biological Activity

A 77636 hydrochloride is a potent and selective dopamine D1-like receptor agonist (pEC50 values are 8.97 and < 5 for D1-like and D2-like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo.

Chemical Information
Molecular Weight 365.9
Formula C20H27NO3.HCl
CAS Number 145307-34-2
Form Solid
Solubility (25°C) Water 36.59 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] R K Pearce, et al. Actions of the D1 agonists A-77636 and A-86929 on locomotion and dyskinesia in MPTP-treated L-dopa-primed common marmosets

[2] P J Blanchet, et al. Dopamine D1 receptor desensitization profile in MPTP-lesioned primates

[3] E F Domino, et al. Relative potency and efficacy of some dopamine agonists with varying selectivities for D1 and D2 receptors in MPTP-induced hemiparkinsonian monkeys

[4] D Wirtshafter, et al. Interactive effects of stimulation of D1 and D2 dopamine receptors on fos-like immunoreactivity in the normosensitive rat striatum

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

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