Chemistry:RQ-00202730
From HandWiki
Short description: Chemical structure
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| Formula | C21H34N4O3S |
| Molar mass | 422.59 g·mol−1 |
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RQ-00202730 is a benzimidazole derived drug that acts as a potent and highly selective agonist for the CB2 cannabinoid receptor, with a Ki value of 19nM at CB2 and more than 4000x selectivity over CB1, though it also shows some activity as an antagonist of the unrelated 5-HT2B serotonin receptor. It has analgesic and antiinflammatory effects in animal studies, and was developed for the treatment of irritable bowel syndrome, but was ultimately discontinued from development following disappointing results in Phase II clinical trials.[1][2][3]
See also
References
- ↑ "Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome". Bioorganic & Medicinal Chemistry Letters 25 (2): 236–40. January 2015. doi:10.1016/j.bmcl.2014.11.062. PMID 25499880.
- ↑ "Research programme: irritable bowel syndrome therapeutics - RaQualia.". AdisInsight. Springer Nature Switzerland AG. 23 February 2016. https://adisinsight.springer.com/drugs/800030010.
- ↑ "The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation". Perspectives in Medicinal Chemistry 8: 17–39. 2016. doi:10.4137/PMC.S32171. PMID 27398024.
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