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| Targets |
Denopamine targets the β1-adrenergic receptor, a G protein-coupled receptor that is primarily located in the heart. Activation of the β1-adrenergic receptor by Denopamine stimulates the production of cyclic AMP (cAMP) through adenylyl cyclase, leading to the activation of protein kinase A (PKA). This results in increased intracellular calcium levels and enhanced myocardial contractility. Denopamine is a selective agonist of the β1-receptor, with minimal effects on β2- and α-adrenergic receptors.
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| ln Vitro |
In a concentration-dependent way, denopamine (0.1-100 μM) suppresses the generation of TNF-α produced by LPS [1].
In vitro, Denopamine is a selective agonist of the β1-adrenergic receptor. Its activity is typically measured using receptor binding and functional assays. In functional assays, the compound's ability to stimulate cAMP accumulation in cells expressing the β1-adrenergic receptor is assessed. Its selectivity is confirmed by its lack of activity at β2- and α-adrenergic receptors. These in vitro studies confirm Denopamine's mechanism of action as a selective β1-agonist. |
| ln Vivo |
A single 14 μmol/kg dose of denopamine in mice produced peak levels within 1 hour [1]. Denopramine plasma concentrations were 13.1±1.9 nmol/L at 1 hour, 4.3±0.9 nmol/L at 2 hours, 1.8±0.5 nmol/L at 3 hours, and <0.6 nmol/L at 5 hours. Denopamine (14 μmol/kg per day; oral; for 14 days) can significantly improve the survival rate of animals, reduce myocardial damage, and inhibit the body's production of TNF-α [1].
In vivo, Denopamine is used as a cardiotonic agent for the treatment of chronic heart failure. It increases myocardial contractility without significantly affecting heart rate. It also dilates coronary vessels and is less likely to cause arrhythmias. Denopamine is an approved drug in some countries. In research, it is used to study β1-adrenergic receptor signaling and cardiac function. |
| Enzyme Assay |
In vitro receptor binding assays for Denopamine measure its affinity for β1-adrenergic receptors. Membranes from cells expressing β1-adrenergic receptors are incubated with a radiolabeled β1 ligand and varying concentrations of Denopamine. The Ki is determined from competition binding curves. Selectivity is assessed by testing the compound against β2- and α-adrenergic receptors. Functional assays measure the stimulation of cAMP accumulation in cells expressing the β1-adrenergic receptor.
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| Cell Assay |
Cell viability assay [1]
Cell Types: Mouse spleen cells Tested Concentrations: 0, 0.1, 1, 10, 100 μM Incubation Duration: 5 hrs (hours) Experimental Results: TNF-α levels diminished by 96.9±6.7%, 62.7±6.5%, 53.2±8.8 % and 40.3±1.5% at 0.1, 1, 10 and 100 μmol/L respectively. In vitro cell-based assays for Denopamine are used to study its effects on β1-adrenergic receptor signaling. Cells expressing the β1-adrenergic receptor are treated with Denopamine, and the accumulation of cAMP is measured. The EC50 is determined from the dose-response curve. These assays confirm the compound's agonist activity at the β1-adrenergic receptor. |
| Animal Protocol |
Animal/Disease Models: 4weeks old inbred male DBA/2 mice [1]
Doses: 14 μmol/kg/day Route of Administration: oral; 14 days Experimental Results: Treatment Dramatically improved the survival rate of animals (25 animals received treatment 14 of 25 (56%) mice compared with 5 of 25 (20%) of control mice). On day 14, the survival rate of the treatment group was 57.1% (16 of 28 mice), which was Dramatically higher than the survival rate of 33.3% (10 of 30 mice) of the control group. Survival from day 6 to day 14 was also Dramatically improved in the treatment group (69.6%; 10 of 23 mice, p < 0.05) compared with the control group (45.5%; 10 of 22 mice, p < 0.05) 16 only). In vivo animal experiments for Denopamine are conducted in animal models of heart failure. In a typical study, Denopamine is administered to animals with induced heart failure, and cardiac function is assessed by measuring parameters such as cardiac output, stroke volume, and left ventricular pressure. The compound's ability to improve cardiac function is measured. These studies confirm the in vivo efficacy of Denopamine as a cardiotonic agent. |
| ADME/Pharmacokinetics |
Denopamine has a molecular weight of 317.38 g/mol and a molecular formula of C18H23NO4. It has a CAS number of 71771-90-9. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized. Denopamine is orally active.
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| Toxicity/Toxicokinetics |
Denopamine is an approved drug and its safety profile has been established. Common side effects may include tachycardia, palpitations, and gastrointestinal disturbances. As a β1-agonist, it may also cause arrhythmias in susceptible patients. It should be used with caution in patients with ischemic heart disease or hypertension. For research use, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
Denopramine is a dimethoxybenzene.
Denopamine is an approved drug for the treatment of chronic heart failure in some countries. It is a selective, orally active β1-adrenoceptor agonist. It increases myocardial contractility without significantly affecting heart rate or β2- and α-adrenergic receptors. It dilates coronary vessels and is less likely to cause arrhythmias. Denopamine is a valuable research tool for studying β1-adrenergic receptor signaling and cardiac function. |
| Molecular Formula |
C18H23NO4
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| Molecular Weight |
317.379
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| Exact Mass |
317.163
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| CAS # |
71771-90-9
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| PubChem CID |
5311064
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| Appearance |
White to off-white solid powder
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| Density |
1.177g/cm3
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| Boiling Point |
518.8ºC at 760 mmHg
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| Flash Point |
267.6ºC
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| Index of Refraction |
1.581
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| LogP |
2.666
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
320
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=C(C=C(C=C1)CCNC[C@@H](C2=CC=C(C=C2)O)O)OC
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| InChi Key |
VHSBBVZJABQOSG-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C18H23NO4/c1-22-17-8-3-13(11-18(17)23-2)9-10-19-12-16(21)14-4-6-15(20)7-5-14/h3-8,11,16,19-21H,9-10,12H2,1-2H3/t16-/m0/s1
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| Chemical Name |
4-[(1R)-2-[2-(3,4-dimethoxyphenyl)ethylamino]-1-hydroxyethyl]phenol
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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 : ~5 mg/mL (~15.75 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1508 mL | 15.7540 mL | 31.5080 mL | |
| 5 mM | 0.6302 mL | 3.1508 mL | 6.3016 mL | |
| 10 mM | 0.3151 mL | 1.5754 mL | 3.1508 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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