塩酸メカミラミン 化学特性,用途語,生産方法
効能
血圧降下薬
説明
Mecamylamine hydrochloride is a non-competitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC50 = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC50 range from 1-7 μM), previously used to treat hypertension.Displays antidepressant-like effects in mice.
Mecamylamine HCl is supplied as tablets for oral use, each containing 2.5 mg mecamylamine HCl. Inactive ingredients are calcium phosphate, D&C Yellow 10, FD&C Yellow 6, lactose, magnesium stearate, cornstarch, and talc.
化学的特性
Mecamylamine hydrochloride is a white, odorless, or practically odorless, crystalline powder, is highly stable, soluble in water and has a molecular weight of 203.75.
使用
Mecamylamine hydrochloride has been used as an additive in extracellular saline during current-clamp recordings to reduce synaptic input. It has also been used as a non-selective nicotinic acetyl choline receptor blocker in aortic body neurons and in MLO-Y4 cells.
使用
Currently, mecamylamine is the only ganglioblocker used for general hypertension; however, the need has declined because of the possibility of addiction and the introduction of
many other antihypertensive drugs into medical practice.
一般的な説明
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.
生物活性
Non-competitive nicotinic acetylcholine receptor antagonist. Displays antidepressant-like effects in mice.
合成
Mecamylamine, N,2,3,3-tetramethylnorbornan-2-ylamine (14.2.2), is
synthesized from 2,3,3-trimethylnorbornen-2, which is reacted in a Ritter reaction conditions with hydrogen cyanide in concentrated sulfuric acid, giving 2,3,3-trimethylnorbornan-2-ylformylamine (14.2.1), the reduction of which by lithium aluminum hydride leads
to mecamylamine (14.2.2) [32,33].
代謝
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.
塩酸メカミラミン 上流と下流の製品情報
原材料
準備製品