| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Dopamine D2 receptor[1]
Carmoxirole hydrochloride selectively targets the dopamine D2 receptor (D2-like agonist). It acts on peripheral D2 receptors to modulate noradrenalin release and sympathetic activation. This peripheral selectivity is a key feature of the compound, distinguishing it from centrally acting dopamine agonists. |
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| ln Vitro |
In cell-free receptor binding assays, Carmoxirole hydrochloride demonstrates high affinity and selectivity for the dopamine D2 receptor. Its activity as an agonist is confirmed by its ability to activate D2 receptor-mediated signaling pathways in vitro. The compound's peripheral selectivity is a result of its physicochemical properties, which limit its penetration into the central nervous system. In cellular assays, Carmoxirole hydrochloride acts as an agonist at dopamine D2 receptors. It activates D2 receptor signaling, which can be measured by its ability to inhibit forskolin-stimulated cAMP production. The compound's effects on noradrenalin release can be studied in cellular models of sympathetic neurons.
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| ln Vivo |
In vivo, Carmoxirole hydrochloride displays antihypertensive properties. By acting on peripheral dopamine D2 receptors, it reduces sympathetic activation and lowers blood pressure. Its peripheral action makes it a useful tool for studying the role of peripheral dopamine receptors in cardiovascular regulation, without the central side effects associated with other dopamine agonists.
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| Enzyme Assay |
Carmoxirole hydrochloride is a selective, peripherally acting dopamine D2 receptor agonist. Cell-free receptor binding assays are performed using membrane preparations from cells expressing the human dopamine D2 receptor. Radioligand displacement studies use [³H]spiperone or similar D2-selective ligands to determine binding affinity.
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| Cell Assay |
Cellular assays for Carmoxirole hydrochloride are conducted using cells expressing the dopamine D2 receptor. The compound's agonist activity is assessed by measuring its ability to inhibit forskolin-stimulated cAMP accumulation. Concentration-response curves are generated to determine EC50 and efficacy values.
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| Animal Protocol |
Carmoxirole hydrochloride displays antihypertensive properties in vivo. In animal models of hypertension, the compound is administered, and its effects on blood pressure are monitored. Its peripheral mechanism of action is confirmed by its lack of central nervous system effects at antihypertensive doses.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Carmoxirole hydrochloride are consistent with a peripherally acting agent. It has limited ability to cross the blood-brain barrier, which contributes to its peripheral selectivity. Detailed pharmacokinetic parameters such as oral bioavailability, half-life, and metabolism are not detailed in the available literature.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for Carmoxirole hydrochloride are not extensively detailed in the available literature. As a selective D2 receptor agonist, its safety profile would be related to its pharmacological activity. Comprehensive toxicological evaluations would be necessary for its development as a therapeutic agent.
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| References |
[1]. Haase AF, et al. Neurochemical profile of EMD 45609 (carmoxirole), a dopamine DA2-receptor agonist. Naunyn Schmiedebergs Arch Pharmacol. 1991 Jun;343(6):588-94.
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| Additional Infomation |
Carmoxirole hydrochloride is prepared by reacting Carmoxirole with an equivalent amount of hydrochloric acid. It is a selective peripheral dopamine D2 receptor agonist that regulates norepinephrine release and sympathetic nerve activation, and has an in vivo hypotensive effect. It functions as a dopamine agonist, antihypertensive drug, and platelet aggregation inhibitor. Its molecular structure contains a Carmoxirole (1+) ligand.
See also: Carmoxirole (note moved here). Carmoxirole hydrochloride is a research compound with potential applications in cardiovascular research. It is a valuable tool for studying the role of peripheral dopamine D2 receptors in blood pressure regulation. It is not approved for clinical use. |
| Molecular Formula |
C24H27CLN2O2
|
|---|---|
| Molecular Weight |
410.94
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| Exact Mass |
410.176
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| CAS # |
115092-85-8
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| PubChem CID |
9822866
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| Appearance |
Yellow to brown solid powder
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| LogP |
5.718
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
|
| Complexity |
555
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].O([H])C(C1C([H])=C([H])C2=C(C=1[H])C(=C([H])N2[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])=C(C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H])=O
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| InChi Key |
LRJUHOBITQUXIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26N2O2.ClH/c27-24(28)20-9-10-23-22(16-20)21(17-25-23)8-4-5-13-26-14-11-19(12-15-26)18-6-2-1-3-7-18;/h1-3,6-7,9-11,16-17,25H,4-5,8,12-15H2,(H,27,28);1H
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| Chemical Name |
3-[4-(4-phenyl-3,6-dihydro-2H-pyridin-1-yl)butyl]-1H-indole-5-carboxylic acid;hydrochloride
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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: 45 mg/mL (109.51 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.48 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 22.5 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: ≥ 2.25 mg/mL (5.48 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 22.5 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: ≥ 2.25 mg/mL (5.48 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 | 2.4334 mL | 12.1672 mL | 24.3345 mL | |
| 5 mM | 0.4867 mL | 2.4334 mL | 4.8669 mL | |
| 10 mM | 0.2433 mL | 1.2167 mL | 2.4334 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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