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
via PubMed
~1 min read
Encyclopedic overview
3 sectionsContents
- See also
- References
- External links
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
Excerpted from Wikipedia’s “telenzepine” article, available under the CC BY-SA 4.0 licence.
Available in 8 languages
via Wikidata sitelinks · CC0