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tiamenidine

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tiamenidine

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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.

Chemical data

Formula
C8H10ClN3S
Molecular weight
215.7 g/mol
IUPAC name
N-(2-chloro-4-methylthiophen-3-yl)-4,5-dihydro-1H-imidazol-2-amine
SMILES
CC1=CSC(=C1NC2=NCCN2)Cl
InChIKey
CVWILQHZFWRYPB-UHFFFAOYSA-N
XLogP
1.6
Polar surface area
64.7 Ų
H-bond donors
2
H-bond acceptors
2
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 2
Molecule type
Small molecule

via ChEMBL · EBI

Wikidata facts

Mass
215.028
Show 3 more facts
chemical formula
C₈H₁₀ClN₃S
canonical SMILES
CC1=CSC(=C1NC2=NCCN2)Cl
Commons category
Tiamenidine
Sources (2)

via Wikidata · CC0

~1 min read

Encyclopedic overview

3 sections
Contents
  • Synthesis
  • See also
  • References

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== [[File:Tiamenidine-synthesis.svg|500px|center|thumb|ChemDrug Synthesis: Patent:]]

Excerpted from Wikipedia’s “tiamenidine” article, available under the CC BY-SA 4.0 licence.

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