Mecamylamine hydrochloride is a non-selective, non-competitive nAChR antagonist, has oral activity, and has certain therapeutic effects on various neuropsychiatric diseases. It can easily cross the blood-brain barrier[1,2].
At a holding potential of –70 mV, mecamylamine (1-20 μM) reduces the amplitude of the induced end plate current (EPC), the Hill constant is equal to 1.2, IC50 = 7.8 μM] [2].
Mecamylamine (0.5-1 mg/kg; Intraperitoneal injection; C57BL/6J mice) has antidepressant-like effects on both the TST and FST and these effects are dependent on the β2 and α7 subunits[3].
References:
[1]. Bacher I, et al. Mecamylamine-a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders. Expert Opin Pharmacother. 2009, 10(16): 2709-21.
[2]. Ostroumov K, et al. Modeling study of mecamylamine block of muscle type acetylcholine receptors. Eur Biophys J. 2008, 37(4): 393-402.
[3]. Rabenstein R L, et al. The nicotinic antagonist mecamylamine has antidepressant-like effects in wild-type but not beta2- or alpha7-nicotinic acetylcholine receptor subunit knockout mice. Psychopharmacology (Berl). 2006 Dec, 189(3): 395-401.
