Telenzepine

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Telenzepine
Telenzepine.png
Systematic (IUPAC) name
1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one
Clinical data
Legal status
?
Identifiers
CAS number 80880-90-6
ATC code None
PubChem CID 5387
ChemSpider 5194
UNII 0990EG3K10 YesY
ChEMBL CHEMBL253978
Chemical data
Formula C19H22N4O2S 
Mol. mass 370.47 g/mol

Telenzepine is a selective M1 antimuscarinic used in the treatment of peptic ulcers.[1] Telenzepine is atropisomeric, in other words the molecule has a stereogenic C–N-axis; in neutral aqueous solution it displays a half-life for racemization of the order of 1000 years. The enantiomers have been resolved. The activity is related to the (+)-isomer which is about 500-fold more active as the (–)-isomer at muscarinic receptors in the rat cerebal cortex.[2]

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References[edit]

  1. ^ Eveleigh, P.; Hulme, E. C.; Schudt, C.; Birdsall, N. J. (1989). "The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes". Molecular pharmacology 35 (4): 477–483. PMID 2704371.  edit
  2. ^ Clayden, J.; Moran, W. J.; Edwards, P. J.; Laplante, S. R. (2009). "The Challenge of Atropisomerism in Drug Discovery". Angewandte Chemie International Edition 48 (35): 6398–6401. doi:10.1002/anie.200901719. PMID 19637174.  edit

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