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α-methyl­ norepinephrine

from methyldopa

What it isAlpha-methylnorepinephrine, the CNS metabolite through which methyldopa works.

Why it mattersMethyldopa is a prodrug: this false transmitter stimulates central alpha-2 receptors and lowers sympathetic outflow — the actual antihypertensive.

What it changesIt explains the drug’s lag to effect and its central side effects (sedation, depression) despite a peripheral-looking parent.

NO BOXED WARNINGS

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: α-methyl­ norepinephrine ballicule

α-methyl norepinephrine ballicule: receptor binding, kinetics and half-life diagram

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