Centhaquine (Centhaquin; PMZ-2010)

Alias: Centhaquine PMZ-2010 PMZ2010 PMZ 2010 Compound 7173
Cat No.:V17892 Purity: ≥98%
Centhaquine, formerly known as PMZ-2010, is a centrally-acting modulator of adrenergic receptor potentially for the treatment of postoperative pain and for the resuscitation of hypovolemic shock.
Centhaquine (Centhaquin; PMZ-2010) Chemical Structure CAS No.: 57961-90-7
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Centhaquine, formerly known as PMZ-2010, is a centrally-acting modulator of adrenergic receptor potentially for the treatment of postoperative pain and for the resuscitation of hypovolemic shock. Centhaquin is a compound that produces hypotension and bradycardia in higher doses and resuscitation in lower doses. It is water insoluble, and is unsuitable for intravenous use.

Biological Activity I Assay Protocols (From Reference)
ln Vivo
In both anesthetized and unanesthetized (decerebrated) cats, centhaquine (Centhaquin) (intravenous, 0.01-1.0 mg/kg; intraduodenal, 1.0-2.5 mg/kg) decreases blood pressure and heart rate in a dose-dependent way [1]. Intravertebral artery injection of centhaquine (5–10 μg) or topical application to the fourth ventral floor or exposed ventral surface of the medulla lowers vasomotor excitability and produces hypotension and bradycardia [1]. During cardiac resuscitation, centhaquine (Centhaquin; PMZ-2010) (intravenous; 0.015 mg/kg) can enhance macro and microcirculation and lessen the negative effects of catecholamines [2].
Animal Protocol
Animal/Disease Models: Landrace pig/Large White piglet[2]
Doses: 0.015mg/kg
Route of Administration: intravenous (iv) (iv)injection; epinephrine 0.02mg/kg plus Centhaquin 0.015mg/kg
Experimental Results: Adding epinephrine can improve VF cardiac arrest pig model ROSC rate.
References
[1]. Srimal RC,et al. Pharmacological studies on 2-(2-(4-(3-methylphenyl)-1-piperazinyl)ethyl) quinoline (centhaquin). I. Hypotensive activity.Pharmacol Res. 1990 May-Jun;22(3):319-29.
[2]. Papalexopoulou K, et al. Centhaquin Effects in a Swine Model of Ventricular Fibrillation: Centhaquin and Cardiac Arrest.Heart Lung Circ. 2017 Aug;26(8):856-863.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H25N3
Molecular Weight
331.463
Exact Mass
331.2048
CAS #
57961-90-7
Related CAS #
1480809-77-5 (citrate);57961-90-7;2379873-37-5 (lactate);
SMILES
CC1=CC(N2CCN(CCC3=NC4=CC=CC=C4C=C3)CC2)=CC=C1
InChi Key
UJNWGFBJUHIJKK-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H25N3/c1-18-5-4-7-21(17-18)25-15-13-24(14-16-25)12-11-20-10-9-19-6-2-3-8-22(19)23-20/h2-10,17H,11-16H2,1H3
Chemical Name
2-(2-(4-(m-tolyl)piperazin-1-yl)ethyl)quinoline
Synonyms
Centhaquine PMZ-2010 PMZ2010 PMZ 2010 Compound 7173
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~188.57 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 6.25 mg/mL (18.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0170 mL 15.0848 mL 30.1696 mL
5 mM 0.6034 mL 3.0170 mL 6.0339 mL
10 mM 0.3017 mL 1.5085 mL 3.0170 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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