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

Pirenzepine dihydrochloride (Synonyms: LS519)

Cat. No.: HY-17037 Purity: 99.65%
Handling Instructions

Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.

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

Pirenzepine dihydrochloride Chemical Structure

Pirenzepine dihydrochloride Chemical Structure

CAS No. : 29868-97-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
500 mg USD 96 In-stock
Estimated Time of Arrival: December 31
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.

In Vitro

The antisecretory properties of pirenzepine on gastric acid and pepsin secretion may be attributed to the antagonistic activity of the drug on muscarinic M1 receptors of gastric intramural plexuses, whereas the effect on parietal muscarinic M2 receptors seems of less importance. Additional inhibitory mechanisms on gastric secretion may be represented by pirenzepine-induced increase in somatostatin release from gastrointestinal system. Significant cytoprotective properties of pirenzepinehave been observed on a variety of experimentally induced peptic ulcerations[1]. Pirenzepine (5-500 μg/mL) inhibits agonist-(acetylcholine-, carbachol- or nicotine-) induced contractions of the toad isolated rectus abdominis muscle, and depresses electrically provoked twitches of the rat phrenic nerve-hemidiaphragm muscle preparation[2].

In Vivo

Pirenzepine is potent in impairing learning of an avoidance; much higher doses are required to antagonize other central muscarinic effects. Pirenzepine is found to impair passive avoidance learning when given i.c.v. 20 min pre-training. The median latencies in pirenzepine-treated animals are 79.5, 11, 27 and 25.5 seconds with doses of 0.03, 0.1, 0.3 and 1 μg per mouse respectively[3]. Acid and pepsin secretion stimulated by either bethanechol or the vagus are inhibited in a dose-responsive manner by pirenzepine[4]. Pirenzepine (5-25 mg/kg i.v.) depresses indirect electrical stimulation-evoked twitches of the cat tibialis anterior and soleus muscle preparations[2].

Molecular Weight

424.32

Formula

C₁₉H₂₃Cl₂N₅O₂

CAS No.

29868-97-1

SMILES

O=C1NC2=CC=CN=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C14.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 75 mg/mL (176.75 mM; Need ultrasonic)

DMSO : 25 mg/mL (58.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3567 mL 11.7836 mL 23.5671 mL
5 mM 0.4713 mL 2.3567 mL 4.7134 mL
10 mM 0.2357 mL 1.1784 mL 2.3567 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[4]

Dogs: In three of the Dogs, gastric secretion also is stimulated by bethanechol infused i.v. at the rate of 80 μg (0.4 μM)/kg.hr for 3 hr. Atropine (1.4, 2.8, 5.6 and 11.2 nM/kg) or pirenzepine (6, 12 and 24 nM/kg) are injected at 15-mm intervals, beginning 1 hr after initiation of bethanechol infusion. Heart rate is measured every 7.5 mm during infusion of the drugs and for 75 mins thereafter[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

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:

PirenzepineLS519LS 519LS-519mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
Pirenzepine dihydrochloride
Cat. No.:
HY-17037
Quantity:
MCE Japan Authorized Agent: