1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. mAChR
    Potassium Channel
  3. Pirmenol hydrochloride

Pirmenol hydrochloride (Synonyms: Cl-845; (±)-Pirmenol hydrochlorid)

Cat. No.: HY-100795A Purity: 95.63%
Handling Instructions

Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

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

Pirmenol hydrochloride Chemical Structure

Pirmenol hydrochloride Chemical Structure

CAS No. : 61477-94-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   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

Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

IC50 & Target

IC50: 0.1 μM (IK.ACh)[1]

In Vitro

Pirmenol inhibits the carbachol-induced IK.ACh in a concentration-dependent manner. Pirmenol also inhibits the GTPγS-induced current although the concentrations of Pirmenol needed to inhibit the GTPγS-induced current are much higher than those to inhibit the carbachol-induced IK.ACh. The IC50 of Pirmenol for inhibition of the GTPγS-induced currents is 30 μM. The inhibitory effect of Pirmenol on these IK.ACh is almost completely reversible and the outward current reappeared upon washout of Pirmenol. Pirmenol on the muscarinic acetylcholine receptor-operated K+ current (IK.ACh) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts. In isolated atrial myocytes, Pirmenol concentration dependently inhibits the IK.ACh induced by carbachol or intracellular loading of GTPγS. In Langendorff-perfused hearts Pirmenol reverses the carbachol-induced decreases in effective refractory periods and atrial fibrillation threshold[1].

In Vivo

The pyridine-methanol derivative Pirmenol hydrochloride is a new antiarrhythmic agent. Single-dose studies in rodents demonstrate a 10- to 15-fold difference between the po and iv LD50 values. In rats, the po LD50 is 359.9 mg/kg and the iv LD50 is 23.6 mg/kg. Mice LD50 values are 215.5 and 20.8 mg/kg for po and iv routes, respectively. Short-term subacute iv toxicity studies in rats (2.5, 5.0, and 7.5 mg/kg) and dogs (2.5, 5, and 10 mg/kg) for 4 weeks elicite minimal reactions. Cardiac effects in dogs include drug related increases in heart rate, increases QRS duration, shortening of ST interval without evidence of cardiac tissue damage and mild local reaction at the injection site. Orally, Pirmenol is well tolerated for 13 weeks in rats receiving 25, 50, and 100 mg/kg/day while dogs given 5, 10, and 15 mg/kg/day shows anticholinergic effects at high levels (dryness of mucosae, body tremors). Heart rates are significantly accelerated only at the beginning of the study and QRS changes are seen with wide individual variations. No drug-related tissue changes are elicited in these species. Teratology studies in rats (50, 100, and 150 mg/kg) and in rabbits (10, 25, and 50 mg/kg) show no overt effect on organogenesis but embryotoxicity is seen at 150 mg/kg in rats[2].

Molecular Weight

374.95

Formula

C₂₂H₃₁ClN₂O

CAS No.

61477-94-9

SMILES

OC(C1=CC=CC=C1)(CCCN2[[email protected]@H](C)CCC[[email protected]]2C)C3=CC=CC=N3.Cl[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (74.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6670 mL 13.3351 mL 26.6702 mL
5 mM 0.5334 mL 2.6670 mL 5.3340 mL
10 mM 0.2667 mL 1.3335 mL 2.6670 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice and Rats[2]
The species and strains used in these studies are: male mice, 21-29 g; rats, 116-261 g; purebred beagle dogs,6.8-12.4 kg;and rabbits, 2.9 kg average. For acute oral and intravenous studies and subacute oral studies, Pirmenol hydrochloride, hereafter referred to as Pirmenol, is supplied as bulk white crystalline compound of approximately 89% purity. Doses are calculated on the basis of base content. In acute studies, Pirmenol is given by gavage as 2 (mice) or 2.5% (rats) in aqueous solution; for iv administration, as 0.5 (mice) or 1% (rats) aqueous solution. In oral subacute studies in dogs, it is given in gelatin capsules, and in rats, it is mixed with the diet to yield the intended dose concentrations. Rabbits received the drug in a 5% aqueous solution by intragastric intubation. For subacute iv studies, Pirmenol is supplied in sterile vials as a 1% solution. In rats, iv injection approximated 0.6 mL/min, and in dogs, the drug is administered via an infusion pump at the rate of 1 mg/kg/min.

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:

PirmenolCl-845(±)-Pirmenol hydrochloridCl845Cl 845mAChRPotassium ChannelMuscarinic acetylcholine receptorKcsAInhibitorinhibitorinhibit

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 *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pirmenol hydrochloride
Cat. No.:
HY-100795A
Quantity:
MCE Japan Authorized Agent: