RQ-00202730 is a
benzimidazole derived
drug that acts as a potent and highly selective
agonist for the CB2cannabinoid 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-HT2Bserotonin 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]
^Iwata Y, Ando K, Taniguchi K, Koba N, Sugiura A, Sudo M (January 2015). "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.
doi:
10.1016/j.bmcl.2014.11.062.
PMID25499880.