Telenzepine

Telenzepine

Telenzepine

Chemical compound

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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References

  1. [1]
    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.
  2. [2]
    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.
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