telenzepine
Sign in to saveTelenzepine is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is used in the treatment of peptic ulcers. 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.
Research
184 papers- Telenzepine and its enantiomers, M1-selective antimuscarinics, in guinea pig lung function tests.Agents and actions. Supplements · 1991
- Gastric antisecretory activity of telenzepine, a new M1-selective muscarinic antagonist: comparison with pirenzepine.Archives internationales de pharmacodynamie et de therapie · 1989
- Telenzepine is at least 25 times more potent than pirenzepine--a dose response and comparative secretory study in man.Gut · 1987
- Effect of telenzepine, an M1-selective muscarinic receptor antagonist, in patients with nocturnal asthma.Pulmonary pharmacology · 1994
- Telenzepine, a new M1-receptor antagonist, is a more potent inhibitor of pentagastrin-stimulated gastric acid output than pirenzepine in dogs.Scandinavian journal of gastroenterology · 1990
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Wikidata facts
- Subclass of
- chemical compound
- Mass
- 370.146
Show 4 more facts
- chemical formula
- C₁₉H₂₂N₄O₂S
- canonical SMILES
- CC1=C2C(=CS1)C(=O)NC3=CC=CC=C3N2C(=O)CN4CCN(CC4)C
- subject has role
- parasympatholytic
- Commons category
- Telenzepine
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Encyclopedic overview
3 sectionsContents
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Telenzepine is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is used in the treatment of peptic ulcers. 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.
== See also == Pirenzepine
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