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SB-269970 hydrochloride

Cat. No. M13876
SB-269970 hydrochloride Structure
Synonym:

SB-269970A

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Biological Activity

SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors.

Chemical Information
Molecular Weight 388.95
CAS Number 261901-57-9
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage 2-8°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] Konstantinos N Tzirogiannis, et al. Effect of 5-HT7 receptor blockade on liver regeneration after 60-70% partial hepatectomy

[2] C Cervantes-Durn, et al. Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats

[3] Tomoko Horisawa, et al. Binding of lurasidone, a novel antipsychotic, to rat 5-HT7 receptor: analysis by [3H]SB-269970 autoradiography

[4] Jos A Terrn, et al. Pharmacological evidence that 5-HT(1B/1D) receptors mediate hypotension in anesthetized rats

[5] David R Thomas, et al. SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats

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  Catalog
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