Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H22N4O2S.2ClH.2H2O |
| Molecular Weight | 479.421 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.Cl.Cl.CN1CCN(CC(=O)N2C3=C(C)SC=C3C(=O)NC4=CC=CC=C24)CC1
InChI
InChIKey=FGZLYNOZVXLZSO-UHFFFAOYSA-N
InChI=1S/C19H22N4O2S.2ClH.2H2O/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);2*1H;2*1H2
| 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 |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| 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 |
|---|---|---|
| The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes. | 1989 Apr |
|
| Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes. | 1989 Nov 28 |
|
| Assessment of the muscarinic receptor subtypes involved in pilocarpine-induced seizures in mice. | 1994 Feb 28 |
|
| Characterization of the muscarinic receptor subtype mediating pilocarpine-induced tremulous jaw movements in rats. | 1999 Jan 1 |
|
| Distinct muscarinic receptors enhance spontaneous GABA release and inhibit electrically evoked GABAergic synaptic transmission in the chick lateral spiriform nucleus. | 2001 |
|
| Inhibition of field stimulation-induced contractions of rabbit vas deferens by muscarinic receptor agonists: selectivity of McN-A-343 for M1 receptors. | 2001 Apr |
|
| Interleukin-2 and interleukin-4 increase the survival of retinal ganglion cells in culture. | 2001 Jan 22 |
|
| Cholinergic modulation of basal and amphetamine-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. | 2002 Dec 20 |
|
| Miniaturization of fluorescence polarization receptor-binding assays using CyDye-labeled ligands. | 2003 Aug |
|
| PMA decreases the proliferation of retinal cells in vitro: the involvement of acetylcholine and BDNF. | 2003 Jan |
|
| Cholinergic modulation of memory in the basolateral amygdala involves activation of both m1 and m2 receptors. | 2003 May |
|
| Muscarinic acetylcholine receptors potentiate the GABAergic transmission in the developing rat inferior colliculus. | 2003 Sep |
|
| Muscarinic modulation of nitrergic neurotransmission in guinea-pig gastric fundus. | 2004 Apr |
|
| M3 subtype of muscarinic receptors mediate Ca2+ release from intracellular stores in rat prostate neuroendocrine cells. | 2005 Apr |
|
| Effect of muscarinic receptor blockade on canine gastric tone and compliance in vivo. | 2005 Apr |
|
| N-desmethylclozapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. | 2005 Nov |
|
| Effects of muscarinic M1 receptor blockade on cocaine-induced elevations of brain dopamine levels and locomotor behavior in rats. | 2007 Apr |
|
| Segment-dependent expression of muscarinic acetylcholine receptors and G-protein coupling in the equine respiratory tract. | 2007 Feb |
|
| Muscarinic acetylcholine receptor-dependent induction of persistent synaptic enhancement in rat hippocampus in vivo. | 2007 Jan 19 |
|
| Muscarinic preferential M(1) receptor antagonists enhance the discriminative-stimulus effects of cocaine in rats. | 2007 Oct |
|
| AC260584 (4-[3-(4-butylpiperidin-1-yl)-propyl]-7-fluoro-4H-benzo[1,4]oxazin-3-one), a selective muscarinic M1 receptor agonist, increases acetylcholine and dopamine release in rat medial prefrontal cortex and hippocampus. | 2007 Oct 31 |
|
| Modulation of long-term potentiation by individual subtypes of muscarinic acetylcholine receptor in the rat dentate gyrus. | 2008 |
|
| Muscarinic receptor M1 and phosphodiesterase 1 are key determinants in pulmonary vascular dysfunction following perinatal hypoxia in mice. | 2008 Jul |
|
| Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism. | 2008 Mar 17 |
|
| 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 |
|
| Development of a homogeneous high-throughput live-cell G-protein-coupled receptor binding assay. | 2008 Sep |
|
| Galantamine improves apomorphine-induced deficits in prepulse inhibition via muscarinic ACh receptors in mice. | 2009 Jan |
|
| Secretion from acinar cells of the exocrine pancreas: role of enteropancreatic reflexes and cholecystokinin. | 2009 Jan |
|
| Differential effects of M1 and 5-hydroxytryptamine1A receptors on atypical antipsychotic drug-induced dopamine efflux in the medial prefrontal cortex. | 2009 Sep |
|
| Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules. | 2010 Feb 9 |
|
| [Beneficial effect of galantamine on sensory information-processing deficits]. | 2010 Oct |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:08:37 GMT 2023
by
admin
on
Sat Dec 16 18:08:37 GMT 2023
|
| Record UNII |
FC9LY2D3RS
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
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D11098
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134822646
Created by
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PARENT -> SALT/SOLVATE |
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