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Clinical data | |
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Trade names | Sundralen, Symcorad, Symcor |
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Pharmacokinetic data | |
Eliminationhalf-life | 2.3–5 hours[1] |
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Chemical and physical data | |
Formula | C8H10ClN3S |
Molar mass | 215.70 g·mol−1 |
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Tiamenidine (BAN,USAN,INN, also known asthiamenidine,Hoe 440) is animidazoline compound that shares many of the pharmacological properties ofclonidine. It is acentrally-actingα2 adrenergic receptoragonist (IC50 = 9.1 nM).[2] It also acts as anα1-adrenergic receptor agonist to a far lesser extent (IC50 = 4.85 μM).[2] In hypertensive volunteers, like clonidine, it significantly increased sinus node recovery time and loweredcardiac output.[3] It was marketed (as tiamenidine hydrochloride) bySanofi-Aventis[4] under the brand nameSundralen[5] for the management ofessential hypertension.[6]
Reaction of thiourea1 withmethyl iodide gives the corresponding S-methyl analogue (2), followed by heating withethylenediamine, completes the synthesis of tiamenidine (3).