Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.
Article Details
- CitationCopy to clipboard
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]
- 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