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Telenzepine dihydrochloride (CAS 147416-96-4)

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Alternate Names:
4,9-Dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride
Application:
Telenzepine dihydrochloride is a potent and selective muscarnic receptor antagonist
CAS Number:
147416-96-4
Molecular Weight:
443.39
Molecular Formula:
C19H22N4O2S•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Telenzepine dihydrochloride is a salt of Telenzepine. Telenzepine is a potent and selective muscarnic receptor antagonist reported to bind to mAChR M1 (Ki = 0.94 nM/L) and mAChR M2 (Ki = 17.8 nM/L) in a study utilizing rabbit and rat isolated superior cervical sympathetic ganglia. Evidence for selective inhibition of gastric acid secretion has been demonstrated in several animal model and in vitro experiments. Telenzepine was found to be 4-10 times more potent than Pirenzepine (sc-204197) in these studies.


Telenzepine dihydrochloride (CAS 147416-96-4) References

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  2. Distinct muscarinic receptors enhance spontaneous GABA release and inhibit electrically evoked GABAergic synaptic transmission in the chick lateral spiriform nucleus.  |  Guo, J. and Chiappinelli, VA. 2001. Neuroscience. 104: 1057-66. PMID: 11457590
  3. Muscarinic acetylcholine receptor-dependent induction of persistent synaptic enhancement in rat hippocampus in vivo.  |  Li, S., et al. 2007. Neuroscience. 144: 754-61. PMID: 17101232
  4. Neuropharmacology of the muscarinic antagonist telenzepine in myenteric ganglia of the guinea-pig small intestine.  |  Christofi, FL., et al. 1991. Eur J Pharmacol. 195: 333-9. PMID: 1868879
  5. Direct comparison between the ulcer-healing effects of two H(+)-K(+)-ATPase inhibitors, one M1-selective antimuscarinic and one H2 receptor antagonist in the rat.  |  Kromer, W., et al. 1990. Pharmacology. 41: 333-7. PMID: 1982899
  6. An in vivo zebrafish screen identifies organophosphate antidotes with diverse mechanisms of action.  |  Jin, S., et al. 2013. J Biomol Screen. 18: 108-15. PMID: 22960781
  7. Involvement of Striatal Cholinergic Interneurons and M1 and M4 Muscarinic Receptors in Motor Symptoms of Parkinson's Disease.  |  Ztaou, S., et al. 2016. J Neurosci. 36: 9161-72. PMID: 27581457
  8. Striatal cholinergic interneurons regulate cognitive and affective dysfunction in partially dopamine-depleted mice.  |  Ztaou, S., et al. 2018. Eur J Neurosci. 48: 2988-3004. PMID: 30230645
  9. Cholinergic modulation inhibits cortical spreading depression in mouse neocortex through activation of muscarinic receptors and decreased excitatory/inhibitory drive.  |  Zerimech, S., et al. 2020. Neuropharmacology. 166: 107951. PMID: 31945385
  10. Determination of telenzepine in human serum by gas chromatography-mass spectrometry.  |  Sturm, E. and Junker, A. 1988. J Chromatogr. 430: 43-51. PMID: 3215960
  11. Unexpected scaffold rearrangement product of pirenzepine found in commercial samples.  |  Ozenil, M., et al. 2021. Sci Rep. 11: 23397. PMID: 34862437
  12. Pharmacological evidence for selective inhibition of gastric acid secretion by telenzepine, a new antimuscarinic drug.  |  Eltze, M., et al. 1985. Eur J Pharmacol. 112: 211-24. PMID: 4029260
  13. Cholinomimetics increase glutamate outflow via an action on the corticostriatal pathway: implications for Alzheimer's disease.  |  Dijk, SN., et al. 1995. J Neurochem. 65: 2165-9. PMID: 7595503
  14. Muscarinic acetylcholine receptor antagonists inhibit chick scleral chondrocytes.  |  Lind, GJ., et al. 1998. Invest Ophthalmol Vis Sci. 39: 2217-31. PMID: 9804129
  15. Use of cyclodextrins in chiral discrimination by NMR spectroscopy: An example of atropisomerism  |  AF Casy. 1993. Magnetic Resonance in Chemistry. 31: 416-417.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Telenzepine dihydrochloride, 10 mg

sc-204332
10 mg
$62.00

Telenzepine dihydrochloride, 25 mg

sc-204332A
25 mg
$128.00