| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Caroverine hydrochloride targets NMDA and AMPA glutamate receptors (iGluRs). It acts as a non-selective, competitive, and reversible antagonist at these receptors. Additionally, it acts as a class B calcium-channel blocker and has antioxidant properties.
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| ln Vitro |
In rat hindquarter preparations, carvacrol (1 μM; 10 min pretreatment) decreases the pressor response to KCl (80 mM) and norepinephrine (1 μM). In isolated rat aortas, carvacine dramatically reduces the contraction caused by KCl (40 mM) [3].
In vitro, Caroverine hydrochloride inhibits the pressor response to KCl (80 mM) and noradrenaline (1 μM) in the rat hindquarter preparation at a concentration of 1 μM (pretreated for 10 min). As an NMDA and AMPA receptor antagonist, it inhibits excitatory neurotransmission. Its calcium-blocking activity contributes to vasorelaxant effects. |
| ln Vivo |
Caroverine (1.44 mg/rat; subcutaneous injection; 1.0 mL/h for 72 hours) can reduce impulse noise-induced hearing loss in rats [4].
In vivo, Caroverine hydrochloride has been investigated for the treatment of inner ear tinnitus. It has also been used clinically in some countries (e.g., Switzerland) as a muscle relaxant (Spasmium, Tinnitin, Tinnex) to relieve spasms in smooth muscles. Its combined ion-channel and receptor-targeting actions make it useful for exploring neuroprotective and auditory therapeutic strategies. |
| Enzyme Assay |
The binding of Caroverine hydrochloride to NMDA and AMPA receptors is typically assessed using radioligand binding assays. Membranes from brain tissue or cells expressing recombinant receptors are incubated with a radiolabeled ligand (e.g., [³H]-MK-801 for NMDA or [³H]-AMPA for AMPA) in the presence of varying concentrations of the compound. IC50 or Ki values are calculated from competition binding curves.
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| Cell Assay |
In vitro cellular assays for Caroverine hydrochloride involve the use of neuronal cell cultures or cell lines expressing NMDA and AMPA receptors. Receptor-mediated calcium influx is measured using fluorescent calcium indicators (e.g., Fura-2 or Fluo-4). Cells are pre-incubated with the compound and then stimulated with glutamate or specific agonists. The reduction in calcium influx is quantified to determine antagonist potency.
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rats (250-300 g) of either sex underwent pulsed noise exposure [4]
Doses: 1.44 mg/rat Doses: 20 mg/mL; sc 1.0 mL/h for 72 hrs (hrs (hours)) Experimental Results: Significant protection of the cochlea from impulse noise damage. In vivo studies of Caroverine hydrochloride are conducted in animal models of tinnitus and neurotoxicity. The compound is administered via intraperitoneal (i.p.) injection or oral gavage. Auditory function is assessed using auditory brainstem response (ABR) testing. Neuroprotection is evaluated in models of excitotoxicity by assessing neuronal survival and tissue damage. Smooth muscle relaxation is assessed in vascular or intestinal preparations. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Caroverine hydrochloride (molecular weight 401.93) are evaluated in preclinical species. The compound has been used clinically, indicating favorable PK properties for oral administration. Plasma concentrations are measured using HPLC or LC-MS/MS to determine key PK parameters including oral bioavailability and half-life.
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| Toxicity/Toxicokinetics |
Caroverine hydrochloride has been used clinically in some countries as a muscle relaxant (Spasmium, Tinnitin, Tinnex). Standard toxicology assessments have been conducted as part of its clinical use. The compound is generally well-tolerated at therapeutic doses. Specific toxicity data is available from clinical use and preclinical studies, though not detailed in public sources.
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| References |
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| Additional Infomation |
Caroverine hydrochloride is a multi-target compound with both receptor antagonist and ion channel blocking activities. It has been used clinically as a muscle relaxant for smooth muscle spasms and investigated for tinnitus and neuroprotection. Its combined actions on glutamate receptors, calcium channels, and oxidative stress make it a unique tool for studying excitotoxicity, neuroprotection, and auditory function.
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| Molecular Formula |
C22H28CLN3O2
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|---|---|
| Molecular Weight |
401.935
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| Exact Mass |
401.187
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| Elemental Analysis |
C, 65.74; H, 7.02; Cl, 8.82; N, 10.45; O, 7.96
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| CAS # |
55750-05-5
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| Related CAS # |
23465-76-1;55750-05-5 (HCl);
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| PubChem CID |
3043582
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| Appearance |
White to off-white solid powder
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| Density |
1.11g/cm3
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| Boiling Point |
521.2ºC at 760mmHg
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| Flash Point |
269ºC
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| LogP |
4.139
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CCN1C2=CC=CC=C2N=C(C1=O)CC3=CC=C(C=C3)OC.Cl
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| InChi Key |
JRNWTJUIMRLKBV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H27N3O2.ClH/c1-4-24(5-2)14-15-25-21-9-7-6-8-19(21)23-20(22(25)26)16-17-10-12-18(27-3)13-11-17;/h6-13H,4-5,14-16H2,1-3H3;1H
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| Chemical Name |
1-(2-(diethylamino)ethyl)-3-(4-methoxybenzyl)quinoxalin-2(1H)-one hydrochloride
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| Synonyms |
P 201-1; P-201-1; P201-1; P 2011; P-2011; P2011; Caroverine HCl; Spadon; Tinnitin; Tinnex;
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~100 mg/mL (~248.80 mM)
H2O : ~20 mg/mL (~49.76 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4879 mL | 12.4397 mL | 24.8793 mL | |
| 5 mM | 0.4976 mL | 2.4879 mL | 4.9759 mL | |
| 10 mM | 0.2488 mL | 1.2440 mL | 2.4879 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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