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]
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| Formula | C19H22N4O2S |
| Molar mass | 370.47 g·mol−1 |
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See also
editReferences
edit- ^ Eveleigh P, Hulme EC, Schudt C, Birdsall NJ (April 1989). "The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes". Molecular Pharmacology. 35 (4): 477–83. PMID 2704371.
- ^ Clayden J, Moran WJ, Edwards PJ, LaPlante SR (2009). "The challenge of atropisomerism in drug discovery". Angewandte Chemie. 48 (35): 6398–401. doi:10.1002/anie.200901719. PMID 19637174.
External links
edit- Londong W, Londong V, Meierl A, Voderholzer U (July 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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