| 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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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Centhaquine targets the central nervous system to increase sympathetic outflow. It stimulates the release of endogenous catecholamines (norepinephrine and epinephrine) from sympathetic nerve endings and the adrenal medulla. Additionally, centhaquine sensitizes alpha-adrenergic receptors to the effects of catecholamines, enhancing vasoconstriction and improving vascular tone. This dual mechanism results in a potent pressor response and improved cardiac contractility without the adverse effects associated with direct alpha-receptor agonists.
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| ln Vitro |
In vitro, centhaquine has been shown to stimulate the release of catecholamines from isolated nerve endings and adrenal chromaffin cells. It also enhances the contractile response of vascular smooth muscle to norepinephrine, consistent with its vasopressor effects. The compound's in vitro activities are consistent with its mechanism of action as a centrally acting sympathomimetic agent.
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| 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].
In vivo, centhaquine has been extensively studied in animal models of hemorrhagic shock and other forms of hypovolemic shock. In these models, centhaquine rapidly restores blood pressure, improves cardiac output, and increases tissue perfusion. The compound has been shown to reduce mortality in animal models of severe hemorrhagic shock. Clinical trials have been conducted to evaluate centhaquine's efficacy and safety in patients with hypovolemic shock. |
| Enzyme Assay |
Centhaquine's activity can be assessed using in vitro assays measuring catecholamine release from isolated tissues or cells. The compound's ability to stimulate norepinephrine release from sympathetic nerve terminals can be evaluated using isolated nerve preparations or cultured sympathetic neurons. Its effects on vascular smooth muscle contraction can be assessed using isolated blood vessel ring preparations. Receptor binding assays can be used to evaluate its interaction with adrenergic receptors.
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| Cell Assay |
Cellular assays for centhaquine involve treating cells (e.g., adrenal chromaffin cells, sympathetic neurons) with the compound and measuring catecholamine release using HPLC or ELISA. Vascular smooth muscle cells can be used to assess the compound's effects on calcium signaling and contraction. The compound's effects on cardiac myocyte contractility can also be evaluated using isolated cardiomyocytes.
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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. In vivo animal model protocols for centhaquine involve its administration (typically intravenous) to animal models of hemorrhagic shock. Models include controlled hemorrhage in rats, pigs, or other species. Blood pressure, heart rate, cardiac output, and tissue perfusion are monitored. Survival rates and markers of organ injury are assessed. Pharmacokinetic and pharmacodynamic studies are performed to determine the optimal dosing regimen. |
| ADME/Pharmacokinetics |
Centhaquine is administered intravenously. Specific pharmacokinetic data is not extensively detailed in the available literature. As a small molecule, it is expected to have a rapid onset of action and a relatively short half-life, consistent with its use as an acute resuscitative agent. The compound is metabolized in the liver and excreted primarily in the urine.
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| Toxicity/Toxicokinetics |
The toxicity profile of centhaquine has been evaluated in preclinical and clinical studies. Common adverse effects may include tachycardia, arrhythmias, and hypertension, consistent with its sympathomimetic mechanism. The compound should be used with caution in patients with pre-existing cardiovascular disease. The safety profile is generally acceptable for its intended use as a resuscitative agent in emergency settings.
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| 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 being investigated in the clinical trial NCT04045327 (PMZ-2010 (Centhaquine) as a resuscitator for hypovolemic shock).
Centhaquine (Centhaquin; PMZ-2010, CAS# 57961-90-7) is a novel, first-in-class, centrally acting sympathomimetic agent with potent vasopressor and positive inotropic effects. It has been developed as a resuscitative agent for the treatment of hypovolemic shock, particularly hemorrhagic shock. Centhaquine acts by stimulating endogenous catecholamine release and sensitizing the vasculature to their effects, restoring blood pressure and improving tissue perfusion. It has been evaluated in animal models and clinical trials for hypovolemic shock. |
| 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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