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  3. Telenzepine dihydrochloride

Telenzepine dihydrochloride 

目录号: HY-B1789A
产品使用指南

Telenzepine dihydrochloride 是一种选择性和具有口服活性的毒蕈碱 M1 受体拮抗剂,Ki 为 0.94 nM。Telenzepine dihydrochloride 抑制胃酸分泌并具有抗溃疡作用。

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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

中文名称

替仑西平二盐酸盐;太兰泽平二盐酸盐

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TelenzepinemAChRMuscarinic acetylcholine receptorM1-receptorantimuscarinicantisecretoryantiulcergastricacidexcitatoryInhibitorinhibitorinhibit

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产品名称:
Telenzepine dihydrochloride
目录号:
HY-B1789A
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