Telenzepine

Telenzepine
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C19H22N4O2S
Molar mass 370.47 g/mol
3D model (JSmol)

Telenzepine is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is 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 than the (–)-isomer at muscarinic receptors in the rat cerebral cortex.[2]

See also

References

  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.
  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.
  • Londong, W; Londong, V; Meierl, A; Voderholzer, U (1987). "Telenzepine is at least 25 times more potent than pirenzepine—a dose response and comparative secretory study in man". Gut. 28 (7): 888–95. doi:10.1136/gut.28.7.888. PMC 1433086. PMID 3653758.


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