| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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. 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.
| 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].
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|---|---|
| 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. |
| Additional Infomation |
Centhaquine is under investigation in clinical trial NCT04045327 (Efficacy of PMZ-2010 (Centhaquine) a Resuscitative Agent for Hypovolemic Shock).
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| Molecular Formula |
C22H25N3
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|---|---|
| Molecular Weight |
331.463
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| Exact Mass |
331.205
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| CAS # |
57961-90-7
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| Related CAS # |
1480809-77-5 (citrate);57961-90-7;2379873-37-5 (lactate);
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| PubChem CID |
162163
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.124g/cm3
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| Boiling Point |
499ºC at 760mmHg
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| Flash Point |
255.6ºC
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| Index of Refraction |
1.628
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| LogP |
3.91
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
404
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC(N2CCN(CCC3C=CC4C(=CC=CC=4)N=3)CC2)=C1
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| InChi Key |
UJNWGFBJUHIJKK-UHFFFAOYSA-N
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| 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
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| Chemical Name |
2-(2-(4-(m-tolyl)piperazin-1-yl)ethyl)quinoline
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| Synonyms |
Centhaquine PMZ-2010 PMZ2010 PMZ 2010 Compound 7173
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~188.57 mM)
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|---|---|
| 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.
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.
(2) Be sure to add the solvent(s) in order.
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