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5-Methylurapidil

Cat. No. M8831
5-Methylurapidil Structure
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Biological Activity

Selective α1A-adrenoceptor antagonist; antihypertensive.

Chemical Information
Molecular Weight 401.5
Formula C21H31N5O3
CAS Number 34661-85-3
Solubility (25°C) Water: 0.4 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] P Shane Clifford, et al. Effects of ICV administration of the alpha1A-adrenoceptor antagonist 5-methylurapidil on concurrent measures of eating and locomotion after cocaine in the rat

[2] R F Wang, et al. Effect of 5-methylurapidil, an alpha 1a-adrenergic antagonist and 5-hydroxytryptamine1a agonist, on aqueous humor dynamics in monkeys and rabbits

[3] B Valenta, et al. Hypotensive effects of 8-hydroxy-2-(di-n-propylamino)tetralin and 5-methylurapidil following stereotaxic microinjection into the ventral medulla of the rat

[4] M Endoh, et al. Role of alpha 1A adrenoceptor subtype in production of the positive inotropic effect mediated via myocardial alpha 1 adrenoceptors in the rabbit papillary muscle: influence of selective alpha 1A subtype antagonists WB 4101 and 5-methylurapidil

[5] Y Hiramatsu, et al. 5-Methylurapidil may discriminate between alpha 1-adrenoceptors with a high affinity for WB4101 in rat lung

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