| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| ln Vitro |
Arbutamine has a pD2 value of 8.45 and promotes myocardial contractility at concentrations between 0.1 and 100 nM. Abutamine's affinity constant (KA) for cardiac β1-adrenergic receptors is 7.32 [3].
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|---|---|
| ln Vivo |
Abbutamide (intravenous; 5, 10, 50, 100, and 250 ng/kg/min) increased mean heart rate, peak left ventricular positive pressure and its first derivative, and normal zone myocardium thickness in 8 open-chest dogs ( average body weight, 26.91 kg) [3].
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
The primary metabolite is methoxyabbutamine. Another possible metabolite is ketoabbutamine. Abbutamine metabolites appear to have lower pharmacological activity and longer half-lives than the parent drug. Biological Half-Life The elimination half-life is approximately 8 minutes. |
| Toxicity/Toxicokinetics |
Protein Binding
58% |
| References |
[1]. Ruiz M, et al. Arbutamine stress perfusion imaging in dogs with critical coronary artery stenoses: (99m)Tc-sestamibi versus (201)Tl. J Nucl Med. 2002 May;43(5):664-70.
[2]. Nagarajan R, et al. A novel catecholamine, arbutamine, for a pharmacological cardiac stress agent. Cardiovasc Drugs Ther. 1996 Mar;10(1):31-8. [3]. Abou-Mohamed G, et, al. Characterization of the adrenergic activity of arbutamine, a novel agent for pharmacological stress testing. Cardiovasc Drugs Ther. 1996 Mar;10(1):39-47. |
| Additional Infomation |
Arbutamine is a catecholamine drug with the effects of a β-adrenergic agonist and a cardiotonic agent. Arbutamine is administered via a closed-loop, computer-controlled drug delivery system to induce an acute cardiovascular response similar to that induced by exercise, aiding in the diagnosis of coronary artery disease in patients unable to exercise adequately. Arbutamine is a synthetic catecholamine with positive chronotropic and positive inotropic properties, used in echocardiography and diagnostic coronary angiography. Arbutamine binds to and activates β1-adrenergic receptors in the myocardium, thereby increasing heart rate and myocardial contractility. By exerting positive chronotropic and positive inotropic effects, Arbutamine mimics exercise-induced cardiac stress, which can lead to tissue hypoperfusion and oxygenation and may induce myocardial ischemia in patients with coronary artery disease. Drug Indications: Used to induce an acute cardiovascular response (cardiac stimulation) similar to that induced by exercise to aid in the diagnosis of coronary artery disease (CAD) in patients unable to exercise adequately.
Mechanism of Action Abaleptamine is a synthetic catecholamine with positive chronotropic and positive inotropic effects. Its positive chronotropic (increased heart rate) and positive inotropic (enhanced myocardial contractility) effects mimic exercise by increasing cardiac workload (generating stress) and induce myocardial ischemia in patients with impaired coronary artery function. The increased heart rate induced by abaleptamine is thought to limit subendocardial perfusion, thereby limiting tissue oxygenation. In functional studies, abaleptamine exhibits higher selectivity for β-adrenergic receptors than α-adrenergic receptors. Abaleptamine's β-agonist activity increases cardiac load by increasing heart rate, myocardial contractility, and systolic blood pressure. Due to the preservation of α-receptor activity, abaleptamine induces less hypotension under the same chronotropic effects than drugs such as isoproterenol. |
| Molecular Formula |
C18H23NO4
|
|---|---|
| Molecular Weight |
317.37952
|
| Exact Mass |
317.163
|
| CAS # |
128470-16-6
|
| Related CAS # |
Arbutamine hydrochloride;125251-66-3
|
| PubChem CID |
60789
|
| Appearance |
Yellow to brown solid powder
|
| Density |
1.262g/cm3
|
| Boiling Point |
578.3ºC at 760mmHg
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| Flash Point |
195.1ºC
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| LogP |
2.84
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
23
|
| Complexity |
320
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(CCNC[C@@H](C1=CC(=C(C=C1)O)O)O)CC2=CC=C(C=C2)O
|
| InChi Key |
IIRWWTKISYTTBL-SFHVURJKSA-N
|
| InChi Code |
InChI=1S/C18H23NO4/c20-15-7-4-13(5-8-15)3-1-2-10-19-12-18(23)14-6-9-16(21)17(22)11-14/h4-9,11,18-23H,1-3,10,12H2/t18-/m0/s1
|
| Chemical Name |
4-[(1R)-1-hydroxy-2-[4-(4-hydroxyphenyl)butylamino]ethyl]benzene-1,2-diol
|
| 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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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