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SB-204070 hydrochloride

Cat. No. M8167
SB-204070 hydrochloride Structure
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Quality Control & Documentation
Biological Activity

Selective 5-HT4 serotonin receptor antagonist.

Chemical Information
Molecular Weight 419.34
Formula C19H27ClN2O4 · HCl
CAS Number 148702-58-3
Solubility (25°C) Water: 20 mg/mL (with heating)
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] C Reavill, et al. 5-HT4 receptor antagonism does not affect motor and reward mechanisms in the rat

[2] M Barras, et al. Characterisation of the 5-HT receptor potentiating neurotransmission in rabbit bladder

[3] S E Banner, et al. Increased defaecation caused by 5-HT4 receptor activation in the mouse

[4] S Bingham, et al. Antagonism by SB 204070 of 5-HT-evoked contractions in the dog stomach: an in-vivo model of 5-HT4 receptor function

[5] C M Franks, et al. Do 5-HT4 receptors mediate the intestinal secretory response to 5-HT in rat in-vivo?

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