Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.

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Cowley PM, Baker J, Buchanan KI, Carlyle I, Clark JK, Clarkson TR, Deehan M, Edwards D, Kiyoi Y, Martin I, Osbourn D, Walker G, Ward N, Wishart G

Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2034-9. doi: 10.1016/j.bmcl.2011.02.019. Epub 2011 Feb 19.

PubMed ID

21334892 [ View in PubMed

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Abstract

The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted human oral bioavailability.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	IC 50 (nM)	11.22	N/A	N/A	Details
Rimonabant	Cannabinoid receptor 1	Ki (nM)	0.933	N/A	N/A	Details