Telenzepine dihydrochlorideA potent and selective muscarnic receptor antagonist

Telenzepine dihydrochloride (CAS 147416-96-4)

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Synonym: 4,9-Dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride
Application: A potent and selective muscarnic receptor antagonist
CAS Number: 147416-96-4
Molecular Weight: 443.39
Molecular Formula: C19H22N4O2S•2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

1. Eltze, M., et al. 1985. Eur. J. Pharmacol. 112: 211-224. PMID: 4029260
2. Christofi, F.L., et al. 1991. Eur. J. Pharmacol. 195: 333-339. PMID: 1868879

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (25 mM), and water (100 mM).
Storage :
Store at room temperature
Melting Point :
230-231° C
Refractive Index :
n20D 1.62 (Predicted)
Ki Data :
mAChR M1: Ki= 0.94 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
XJ9008630
PubChem CID :
6419995
MDL Number :
MFCD01529948
SMILES :
CC1=C2C(=CS1)C(=O)NC3=CC=CC=C3N2C(=O)CN4CCN(CC4)C.Cl.Cl

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Certificate of Analysis

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