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)
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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Cholinergic modulation of basal and amphetamine-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. | 2002 Dec 20 |
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Miniaturization of fluorescence polarization receptor-binding assays using CyDye-labeled ligands. | 2003 Aug |
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N-desmethylclozapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. | 2005 Nov |
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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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Muscarinic acetylcholine receptor-dependent induction of persistent synaptic enhancement in rat hippocampus in vivo. | 2007 Jan 19 |
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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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Muscarinic receptor M1 and phosphodiesterase 1 are key determinants in pulmonary vascular dysfunction following perinatal hypoxia in mice. | 2008 Jul |
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Galantamine improves apomorphine-induced deficits in prepulse inhibition via muscarinic ACh receptors in mice. | 2009 Jan |
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Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules. | 2010 Feb 9 |
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[Beneficial effect of galantamine on sensory information-processing deficits]. | 2010 Oct |
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
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C29704
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C75285
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Telenzepine
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)