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SB-277011

Cat. No. M29308
SB-277011 Structure
Synonym:

SB-277011A

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Biological Activity

SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant. IC50 value: 8.0 (pKi) Target: D3 receptor

Chemical Information
Molecular Weight 438.56
Formula C28H30N4O
CAS Number 215803-78-4
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] Pierre Clément, et al. J Sex Med. Delay of ejaculation induced by SB-277011, a selective dopamine D3 receptor antagonist, in the rat

[2] Eric Southam, et al. Brain Res. Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain

[3] G Remington, et al. Curr Opin Investig Drugs. SB-277011 GlaxoSmithKline

[4] N E Austin, et al. Xenobiotica. Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey: in vitro/in vivo correlation and the role of aldehyde oxidase

[5] C Reavill, et al. J Pharmacol Exp Ther. Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A

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Keywords: SB-277011, SB-277011A supplier, Dopamine Receptor, inhibitors, activators

 
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