Telenzepine

Telenzepine
Systematic (IUPAC) name
	1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	80880-90-6
ATC code	?
PubChem	CID 5387
ChemSpider	5194
UNII	0990EG3K10
ChEMBL	CHEMBL253978
Chemical data
Formula	C19H22N4O2S
Mol. mass	370.47 g/mol
SMILES	eMolecules & PubChem

Telenzepine is an anticholinergic or sympatholytic used in the treatment of peptic ulcers.^[1] 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 has about 500-fold more active as the (–)-isomer at muscarinic receptors in rat cerebal cortex.^[2]

[edit] See also

Pirenzepine

[edit] References

^ P. Eveleigh, E. C. Hulme, C. Schudt, N. J. M. Birdsall, Mol. Pharmacol. 1989, 35, 364.
^ J. Clayden, W. J. Moran, P. J. Edwards, S. R. LaPante: The Challenge of Atropisomerism in Drug Discovery, Angew. Chem. Int. Ed. 2009, 48, 6398-6401.

[edit] External links

Telenzepine is at least 25 times more potent than pirenzepine--a dose response and comparative secretory study in man, Gut., 1987 July; 28(7): 888–895

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[Eveleigh-0] P. Eveleigh, E. C. Hulme, C. Schudt, N. J. M. Birdsall, Mol. Pharmacol. 1989, 35, 364.

[Clayden-1] J. Clayden, W. J. Moran, P. J. Edwards, S. R. LaPante: The Challenge of Atropisomerism in Drug Discovery, Angew. Chem. Int. Ed. 2009, 48, 6398-6401.

[1]

[2]

May	JUN	Jul
	05
2011	2012	2013

Telenzepine

[edit] See also

[edit] References

[edit] External links

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