telenzepine
Small moleculeexperimental
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. — Wikipedia
Clinical trial activity
1 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
1
Phase 2
0
Phase 3
0
Phase 4
0
Earliest trial started May 1, 2010 (NCT01155531)
Timeline
2010s
- Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Muscarinic acetylcholine receptor M1ANTAGONIST
CHRM1 antagonist
Chemistry & pharmacology
Loading structure…
SMILES
Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O- Mol. weight
- 370.48 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTelenzepine ↗
- ChEMBLCHEMBL253978 ↗
Also known as
- 4,9-dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl)-10h-thieno(3,4-b)(1,5)benzodiazepin-10-one
- telenzepine
- telenzepine
- telenzepine
- telenzepine
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01155531 | Phase 1 | May 1, 2010 | PRACS, Theracos |
Showing 1 of 1 trials
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