Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H22N4O2S |
Molecular Weight | 370.469 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCN(CC(=O)N2C3=C(C)SC=C3C(=O)NC4=CC=CC=C24)CC1
InChI
InChIKey=VSWPGAIWKHPTKX-UHFFFAOYSA-N
InChI=1S/C19H22N4O2S/c1-13-18-14(12-26-13)19(25)20-15-5-3-4-6-16(15)23(18)17(24)11-22-9-7-21(2)8-10-22/h3-6,12H,7-11H2,1-2H3,(H,20,25)
Molecular Formula | C19H22N4O2S |
Molecular Weight | 370.469 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Telenzepine is a selective muscarinic M1 receptor antagonist that was studied for selective inhibition of gastric acid secretion. Telenzepine was used in clinical trials in patients with acute duodenal ulcer, where was found that once daily administration of 3 mg in the evening must be regarded as the optimal dosage regimen of telenzepine. However, the preregistration for peptic ulcer in Germany was discontinued. In addition, the drug was studied in patients with nocturnal asthma. It was shown that telenzepine via the oral route at a dose of up to 5 mg was not effective in preventing nocturnal asthma.
Approval Year
PubMed
Title | Date | PubMed |
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The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes. | 1989 Apr |
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Assessment of the muscarinic receptor subtypes involved in pilocarpine-induced seizures in mice. | 1994 Feb 28 |
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Characterization of the muscarinic receptor subtype mediating pilocarpine-induced tremulous jaw movements in rats. | 1999 Jan 1 |
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Distinct muscarinic receptors enhance spontaneous GABA release and inhibit electrically evoked GABAergic synaptic transmission in the chick lateral spiriform nucleus. | 2001 |
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Inhibition of field stimulation-induced contractions of rabbit vas deferens by muscarinic receptor agonists: selectivity of McN-A-343 for M1 receptors. | 2001 Apr |
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Miniaturization of fluorescence polarization receptor-binding assays using CyDye-labeled ligands. | 2003 Aug |
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PMA decreases the proliferation of retinal cells in vitro: the involvement of acetylcholine and BDNF. | 2003 Jan |
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Cholinergic modulation of memory in the basolateral amygdala involves activation of both m1 and m2 receptors. | 2003 May |
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Effects of muscarinic M1 receptor blockade on cocaine-induced elevations of brain dopamine levels and locomotor behavior in rats. | 2007 Apr |
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Segment-dependent expression of muscarinic acetylcholine receptors and G-protein coupling in the equine respiratory tract. | 2007 Feb |
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Muscarinic preferential M(1) receptor antagonists enhance the discriminative-stimulus effects of cocaine in rats. | 2007 Oct |
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Effect of muscarinic receptor agonists xanomeline and sabcomeline on acetylcholine and dopamine efflux in the rat brain; comparison with effects of 4-[3-(4-butylpiperidin-1-yl)-propyl]-7-fluoro-4H-benzo[1,4]oxazin-3-one (AC260584) and N-desmethylclozapine. | 2008 Oct 31 |
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Development of a homogeneous high-throughput live-cell G-protein-coupled receptor binding assay. | 2008 Sep |
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Galantamine improves apomorphine-induced deficits in prepulse inhibition via muscarinic ACh receptors in mice. | 2009 Jan |
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Secretion from acinar cells of the exocrine pancreas: role of enteropancreatic reflexes and cholecystokinin. | 2009 Jan |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2695806
120 patients with endoscopically proven, florid duodenal ulcer were treated with either 1.5 mg, 3 mg or 5 mg telenzepine once daily at bedtime (40 patients per dose group).
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:32:36 UTC 2023
by
admin
on
Fri Dec 15 16:32:36 UTC 2023
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Record UNII |
0990EG3K10
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C29704
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SUB10871MIG
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100000082461
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5387
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758679
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5379
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C046338
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C75285
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Telenzepine
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m952
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DTXSID5045209
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0990EG3K10
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CHEMBL253978
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80880-90-6
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ACTIVE MOIETY |
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