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Tiamenidine

Tiamenidine (BAN, USAN, INN, also known as thiamenidine, Hoe 440) is an imidazoline compound that shares many of the pharmacological properties of clonidine. It is a centrally-acting α<sub>2</sub> adrenergic receptor agonist (IC<sub>50</sub> = 9.1&nbsp;nM). It also acts as an α<sub>1</sub>-adrenergic receptor agonist to a far lesser extent (IC<sub>50</sub> = 4.85&nbsp;μM). In hypertensive volunteers, like clonidine, it significantly increased sinus node recovery time and lowered cardiac output. It was marketed (as tiamenidine hydrochloride) by Sanofi-Aventis under the brand name Sundralen for the management of essential hypertension.

Synthesis

Reaction of thiourea 1 with methyl iodide gives the corresponding S-methyl analogue (2), followed by heating with ethylenediamine, completes the synthesis of tiamenidine (3).

See also

References