Мы используем файлы cookie.
Продолжая использовать сайт, вы даете свое согласие на работу с этими файлами.
Abandoned drugs
Tiamenidine
Другие языки:

Tiamenidine

Подписчиков: 0, рейтинг: 0
Tiamenidine
Tiamenidine.svg
Clinical data
Trade names Sundralen, Symcorad, Symcor
ATC code
Pharmacokinetic data
Elimination half-life 2.3–5 hours
Identifiers
  • N-(2-chloro-4-methylthiophen-3-yl)-4,5-dihydro-1H-imidazol-2-amine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C8H10ClN3S
Molar mass 215.70 g·mol−1
3D model (JSmol)
  • Clc2scc(c2N/C1=N/CCN1)C
  • InChI=1S/C8H10ClN3S/c1-5-4-13-7(9)6(5)12-8-10-2-3-11-8/h4H,2-3H2,1H3,(H2,10,11,12) checkY
  • Key:CVWILQHZFWRYPB-UHFFFAOYSA-N checkY
 ☒NcheckY (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). It also acts as an α1-adrenergic receptor agonist to a far lesser extent (IC50 = 4.85 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

Tiamenidine 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


Новое сообщение