| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Metaraminol Bitartrate targets α1-adrenergic receptors. It acts as an agonist at these receptors, leading to vasoconstriction and increased blood pressure. It affects adrenergic receptors directly or indirectly, with the alpha effect predominating. Its pressor effect begins one to two minutes after intravenous injection and lasts about 20 minutes to one hour.
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| ln Vitro |
Similar to norepinephrine, metahydroxylamine activates α-adrenergic receptors and speeds up colonial crypt cell proliferation, but not in malignancies [3].
In vitro, metaraminol bitartrate is an α-adrenergic agonist. It is a sympathomimetic amine that directly and indirectly affects adrenergic receptors. Its activity is characterized by its ability to stimulate α1-adrenergic receptors, leading to vasoconstriction in isolated vascular preparations. |
| ln Vivo |
In six of the ten animals under study, lethal endotoxic shock might be avoided by concurrently administering metahydroxylamine [2].
In vivo, metaraminol bitartrate is a vasopressor agent used to treat hypotension. It increases both systolic and diastolic blood pressure. The pressor effect begins one to two minutes after intravenous injection and lasts about 20 minutes to one hour. It is used in the prevention and treatment of hypotension, particularly as a complication of anesthesia. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for metaraminol bitartrate typically involve radioligand binding assays using membrane preparations from cells expressing α1-adrenergic receptors. Competitive binding experiments with labeled ligands such as [3H]-prazosin are performed to determine affinity (Ki). Standard protocols involve incubating membranes with increasing concentrations of metaraminol in the presence of a fixed concentration of radioligand.
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| Cell Assay |
In vitro cellular assays for metaraminol bitartrate involve culturing cells expressing α1-adrenergic receptors in the presence of serial dilutions of the compound. Receptor-mediated signaling, such as calcium mobilization or inositol phosphate production, is measured. Cell viability is assessed using standard assays. Its agonist activity is characterized by its ability to activate α1-adrenergic receptor signaling.
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| Animal Protocol |
Animal/Disease Models: 10 adult dogs weighing between 7.8 and 13 kg[2]
Doses: 25 mg in 250 mL of 5% dextrose and water Route of Administration: intravenous (iv) (iv)infusion Experimental Results: Prevented fatal endotoxic shock , In vivo animal studies for metaraminol bitartrate include models of hypotension, such as hemorrhage or drug-induced hypotension in rodents or dogs. Animals are treated with metaraminol via intravenous injection. Endpoints include blood pressure, heart rate, and survival. Standard protocols include dose-response assessment and comparison to reference vasopressors. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of metaraminol bitartrate include a molecular weight of 317.30 and a molecular formula of C₉H₁₃NO₂·C₄H₆O₆. It is a sympathomimetic amine. It is administered intravenously for rapid onset of action. Its pressor effect lasts about 20 minutes to one hour. It is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicological data for metaraminol bitartrate indicate that it should be given with caution in the presence of heart or thyroid disease, hypertension, or diabetes. It may cause hypertension, arrhythmias, and tissue necrosis at the injection site if extravasation occurs. It is contraindicated in patients with severe hypertension or tachyarrhythmias. Overdose can cause severe hypertension and cerebral hemorrhage.
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| References | |
| Additional Infomation |
sympathomimetic drug that primarily acts on α-1 adrenergic receptors. It is mainly used as a vasoconstrictor to treat hypotension.
Metaraminol Bitartrate is a sympathomimetic amine used as a vasoconstrictor in the treatment of hypotension. It is an α1-adrenergic receptor agonist. It is also known as Metaradrine tartrate. It is used in the prevention and treatment of hypotension, particularly as a complication of anesthesia. It is not approved for human therapeutic use in all jurisdictions. |
| Molecular Formula |
C9H13NO2.C4H6O6
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|---|---|
| Molecular Weight |
317.29186
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| Exact Mass |
317.111
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| CAS # |
33402-03-8
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| Related CAS # |
33402-03-8 (tartrate);54-49-9;
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| PubChem CID |
441414
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| Appearance |
White to off-white solid powder
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| Boiling Point |
357.9ºC at 760 mmHg
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| Flash Point |
170.3ºC
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
274
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@H]([C@@H](C1=CC(=CC=C1)O)O)N.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
VENXSELNXQXCNT-IJYXXVHRSA-N
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| InChi Code |
InChI=1S/C9H13NO2.C4H6O6/c1-6(10)9(12)7-3-2-4-8(11)5-7;5-1(3(7)8)2(6)4(9)10/h2-6,9,11-12H,10H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t6-,9-;1-,2-/m01/s1
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| Chemical Name |
3-[(1R,2S)-2-amino-1-hydroxypropyl]phenol;(2R,3R)-2,3-dihydroxybutanedioic acid
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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 : ≥ 28 mg/mL (~88.25 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 | 3.1517 mL | 15.7585 mL | 31.5169 mL | |
| 5 mM | 0.6303 mL | 3.1517 mL | 6.3034 mL | |
| 10 mM | 0.3152 mL | 1.5758 mL | 3.1517 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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