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SKF-82958 hydrobromide

Cat. No. M25541
SKF-82958 hydrobromide Structure
Synonym:

(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide

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Biological Activity

SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).

Chemical Information
Molecular Weight 410.73
Formula C19H21BrClNO2
CAS Number 74115-01-8
Form Solid
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage 4°C, dry, sealed
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] C N Haile, et al. Eur J Pharmacol. The dopamine D(1) receptor agonist SKF-82958 serves as a discriminative stimulus in the rat

[2] R Grondin, et al. Eur J Pharmacol. Dopamine D1 receptor mRNA and receptor levels in the striatum of MPTP monkeys chronically treated with SKF-82958

[3] B S Abrahams, et al. Eur J Pharmacol. Place conditioning with the dopamine D1-like receptor agonist SKF 82958 but not SKF 81297 or SKF 77434

[4] E F Domino, et al. J Pharmacol Exp Ther. Trihexyphenidyl interactions with the dopamine D1-selective receptor agonist SKF-82958 and the D2-selective receptor agonist N-0923 in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced hemiparkinsonian monkeys

[5] E F Domino, et al. Eur J Pharmacol. Talipexole or pramipexole combinations with chloro-APB (SKF 82958) in MPTP-induced hemiparkinsonian monkeys

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Keywords: SKF-82958 hydrobromide, (±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide supplier, Dopamine Receptor, inhibitors, activators

 
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