Chemistry

The best known of the muscarinic blocking drugs are the belladonna alkaloids, atropine (Atropine) and scopol-amine (Scopolamine). They are tertiary amines that contain an ester linkage. Atropine is a racemic mixture of dl-hyoscyamine, of which only the levorotatory isomer is pharmacologically active. Atropine and scopolamine are parent compounds for several semisynthetic derivatives, and some synthetic compounds with little structural similarity to the belladonna alkaloids are also in use. All of the antimuscarinic compounds are amino alcohol esters with a tertiary amine or quaternary ammonium group.

The control of access to muscarinic receptors in the central nervous system (CNS) by a tertiary amine versus quaternary ammonium group is fundamentally important in selecting among antimuscarinic agents.

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