Chemical Properties
White Solid
Uses
Antihypertensive;Cholinergic receptor antagonist
Uses
Mecamylamine is a noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC50 = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC50s range from 1-7 μM). Mecamylamine is widely used as a broad-spectrum antagonist of neuronal nicotinic acetylcholine receptors in basic nicotine research. It has been reported to be effective as an aid to smoking cessation and may also be of use in various nicotine-responsive, neuropsychiatric disorders.[Cayman Chemical]
Uses
A noncompetitive nicotinic AChR inhibitor.
Uses
Nicotinic receptor antagonist; orally active ganglionic blocker. Antihypertensive.
General Description
The secondary aminemecamylamine hydrochloride, N,2,3,3-tetramethyl-2-norbornanaminehydrochloride (Inversine), has a powerful ganglionicblocking effect that is almost identical to that ofhexamethonium. It has an advantage over most of the ganglionicblocking agents in being absorbed readily andsmoothly from the GI tract. It is rarely used, however, forthe treatment of moderate-to-severe hypertension becausesevere orthostatic hypotension occurs when the drug blockssympathetic ganglia.
Biological Activity
Non-competitive nicotinic acetylcholine receptor antagonist. Displays antidepressant-like effects in mice.
Metabolism
Mecamylamine hydrochloride (Inversine) is a secondary amine and can therefore easily penetrate cell membranes. Its absorption from the gastrointestinal tract is more complete than that of the quaternary ammonium compounds. Mecamylamine is well absorbed orally and crosses both the blood-brain and placental barriers; its distribution is not confined to the extracellular space. High concentrations of the drug accumulate in the liver and kidney, and it is excreted unchanged by the kidney. In contrast to most of the highly ionized ganglionic blocking agents, mecamylamine can produce central nervous system effects, including tremors, mental confusion, seizures, mania, and depression.The mechanism by which these central effects are produced is unclear.Mecamylamine is rarely used today as an antihypertensive drug because it blocks both parasympathetic and sympathetic ganglia.
China
