Telenzepine Explained

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

• Pirenzepine

External links

• Londong W, Londong V, Meierl A, Voderholzer U . Telenzepine is at least 25 times more potent than pirenzepine--a dose response and comparative secretory study in man . Gut . 28 . 7 . 888–95 . July 1987 . 3653758 . 1433086 . 10.1136/gut.28.7.888 .

Notes and References

1. Eveleigh P, Hulme EC, Schudt C, Birdsall NJ . The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes . Molecular Pharmacology . 35 . 4 . 477–83 . April 1989 . 2704371 .
2. Clayden J, Moran WJ, Edwards PJ, LaPlante SR . The challenge of atropisomerism in drug discovery . Angewandte Chemie . 48 . 35 . 6398–401 . 2009 . 19637174 . 10.1002/anie.200901719 .