Vedaclidine

Vedaclidine (LY-297,802, NNC 11-1053) is a novel analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M₁ and M₄ subtypes, yet an antagonist at the M₂, M₃ and M₅ subtypes. It is orally active and an effective analgesic over 3x the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.