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ABT-239

Cat. No. M10773
ABT-239  Structure
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Biological Activity

ABT-239 is a novel, highly effective, non-imidazole H3R antagonist and antagonist of TRPV1.

Chemical Information
Molecular Weight 330.42
Formula C22H22N2O
CAS Number 460746-46-7
Solubility (25°C) DMSO ≥ 60 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] Emil Trofimiuk, et al. Front Syst Neurosci. Selective H3 Antagonist (ABT-239) Differentially Modifies Cognitive Function Under the Impact of Restraint Stress

[2] Malay Bhowmik, et al. Brain Res. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice

[3] Rafael K Varaschin, et al. J Pharmacol Exp Ther. Effects of the cognition-enhancing agent ABT-239 on fetal ethanol-induced deficits in dentate gyrus synaptic plasticity

[4] Timothy A Esbenshade, et al. J Pharmacol Exp Ther. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties

[5] Gerard B Fox, et al. J Pharmacol Exp Ther. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 re䲧璷Ỵ璸㧀璶羹瘬

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