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Trade names | Sundralen, Symcorad, Symcor |
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Pharmacokinetic data | |
Elimination half-life | 2.3–5 hours[1] |
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Chemical and physical data | |
Formula | C8H10ClN3S |
Molar mass | 215.70 g·mol−1 |
3D model (JSmol) | |
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NY (what is this?) (verify) |
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 α2 adrenergic receptor agonist (IC50 = 9.1 nM).[2] It also acts as an α1-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 lowered cardiac output.[3] It was marketed (as tiamenidine hydrochloride) by Sanofi-Aventis[4] under the brand name Sundralen[5] for the management of essential hypertension.[6]
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).
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Sympatholytics (antagonize α-adrenergic vasoconstriction) |
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Other antagonists |
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α1 |
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α2 |
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β |
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