1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Telenzepine dihydrochloride

Telenzepine dihydrochloride 

Cat. No.: HY-B1789A
Handling Instructions

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects.

For research use only. We do not sell to patients.

Telenzepine dihydrochloride Chemical Structure

Telenzepine dihydrochloride Chemical Structure

CAS No. : 147416-96-4

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Description

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects[1][2][3].

IC50 & Target

Ki: 0.94 nM (Muscarinic M1 receptor), 17.8 nM (Muscarinic M2 receptor)[3]

In Vitro

At submicromolar concentrations (100 nM), Telenzepine abolishes responses to either muscarine or the muscarinic component of the acetylcholine response. The excitatory effect of muscarine at postsynaptic M1 receptors is dose dependently inhibited by Telenzepine (0.1-1000 nM) at concentrations[2].
The threshold dose of Telenzepine as an antagonist of the muscarinic depolarization in AH/type 2 neurons is in the range of 0.1-1 nM. The IC50 of Telenzepine needed to abolish the response is 8.5 nM[2].

In Vivo

Intravenous Telenzepine potently inhibits gastric acid secretion in the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or, both intravenously and orally, in the modified Shay rat[1].
Telenzepine (2.7 μmol/kg; orally) treatment shows significantly longer duration antiulcer effects in the modified Shay rat[1].

Molecular Weight

443.39

Formula

C₁₉H₂₄Cl₂N₄O₂S

CAS No.

147416-96-4

SMILES

O=C1C2=CSC(C)=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C4N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TelenzepinemAChRMuscarinic acetylcholine receptorM1-receptorantimuscarinicantisecretoryantiulcergastricacidexcitatoryInhibitorinhibitorinhibit

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Telenzepine dihydrochloride
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HY-B1789A
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