Recently the discovery of a further class of diarylpyrazolines with high potency and selectivity for the CB1 receptor was described . These compounds were found to be CB1 antagonists. SLV319 was found to be a potent CB1 antagonist (Ki = 7.8 nM) close to that of the Sanofi compound SR-141716A, with more than 1000-fold selectivity against CB2.
Additional synthetic compounds that bind to the CB1 and/or CB2 receptors have been mentioned in patents. These were recently reviewed by Hertzog .
Novartis AG has recently filed a patent application on a series of quinazo-lines as cannabinoid agonists useful for the treatment of pain, osteoarthritis, rheumatoid arthritis and glaucoma, among other indications . Compound 1 binds to both CB1 (K = 34 nM) and CB2 (Ki =11 nM). The patent application refers to the compound as having CB2 agonist activity. Additionally, this compound has been shown to be active in a rodent neuropathic pain model when administered at an oral dose of 0.5 mg/kg.
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