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Adiphenine is an anticholinergic agent.1,2,3,4 It is an antagonist of nicotinic acetylcholine receptors (nAChRs; IC50s = 1.8, 3.7, and 6.3 µM for the α3β4, α4β2, and α4β4 subunit-containing receptors, respectively), as well as muscarinic acetylcholine receptors (Ki = 0.44 µM).1,2 Adiphenine inhibits contractions induced by acetylcholine (ACh) in isolated guinea pig ileum in a concentration-dependent manner.2 It prevents tonic hindlimb extension in a mouse model of seizures induced by maximal electroshock (MES) with an ED50 value of 62 mg/kg but is neurotoxic at higher doses.3 Adiphenine protects against organophosphate-induced lethality in mice with a 50% protective dose (PD50) value of 3.3 mg/kg.4 It has also been used as a local anesthetic.1,3
WARNING This product is not for human or veterinary use.
1. Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes. J. Pharmacol. Exp. Ther. 299(3), 1038-1048 (2001).
2. Comparison of in vitro actions with behavioral effects of antimuscarinic agents. J. Pharmacol. Exp. Ther. 242(3), 796-803 (1987).
3. Anticonvulsant properties of procaine, cocaine, adiphenine and related structures. Proc. Soc. Exp. Biol. Med. 90(1), 192-1995 (1955).
4. Effective doses of some cholinolytics in the treatment of anticholinesterase poisoning. Eur. J. Pharmacol. 12(1), 85-93 (1970).