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RS 56812 hydrochloride

Cat. No. M7225
RS 56812 hydrochloride Structure
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Biological Activity

RS 56812 hydrochloride is a a highly potent and selective 5-HT3 partial agonist, with a pKi at 5-HT3 receptors in rat brain of 9.6, and greater than 1000-fold selectivity over a wide range of other neurotransmitter receptors.

Chemical Information
Molecular Weight 347.84
Formula C18H21N3O2.HCl
CAS Number 143339-12-2
Solubility (25°C) Water 34.78 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] Peroutka and Synder. Am J Psychiatry. Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency.

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