Mecamylamine

Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area^[1][2][5]. IC50 & Target: nAChR^[1], histamine receptor^[2] In Vitro: Mecamylamine (0.5-9 μM, bath administered) increases the firing frequency of identified 5-HT DRN (dorsal raphe nucleus) neurons^[1].
Mecamylamine (0.5-9 μM, bath administered) increases the glutamatergic and decreases the GABAergic input of 5-HT DRN neurons^[1].
Mecamylamine (1 mM, 5 min) blocks the histamine receptor and the histamine-induced contractions in helically cut strips of rabbit aorta^[2].
Mecamylamine (10 μM,48 h) attenuates the effect of nicotine’s action of neuroprotection^[3].
Mecamylamine (1-100 nM, 30 min) dose-dependently attenuates endothelial tube formation in HDMVECs^[4]. In Vivo: Mecamylamine (subcutaneous pumps, 50 mg/kg/day, 2 days) inhibits choroidal neovascularization (CNV) in CNV mice model^[4].
Mecamylamine (intraperitoneal injection, 0.5-1 mg/kg) has antidepressant-like effects in both the TST (tail suspension test) and FST (forced swim test) in C57BL/6J mice, which are dependent on both β2 and α7 subunits^[5].