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| 50mg |
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| 500mg |
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| Targets |
The primary targets of (±)-Norepinephrine (+)-bitartrate are adrenergic receptors, specifically α1, α2, β1, and β3 receptors. As an endogenous agonist, norepinephrine binds to and activates these receptors with varying affinities. Activation of α1 receptors mediates vasoconstriction, α2 receptors mediate feedback inhibition of norepinephrine release, β1 receptors mediate positive inotropic and chronotropic effects on the heart, and β3 receptors mediate lipolysis and thermogenesis. The compound's effects are mediated through G-protein coupled receptor signaling pathways, including the activation of phospholipase C (α1) and adenylyl cyclase (β receptors).
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| ln Vitro |
In vitro, (±)-Norepinephrine (+)-bitartrate is a potent agonist of adrenergic receptors. Its activity is typically measured using radioligand binding assays with cell membranes expressing adrenergic receptors, and functional assays that measure receptor-mediated signaling, such as calcium mobilization (α1), inhibition of cAMP accumulation (α2), or stimulation of cAMP accumulation (β receptors). EC50 values are determined from dose-response curves. The compound's effects on various cell types, including vascular smooth muscle cells, cardiomyocytes, and neurons, are studied in vitro.
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| ln Vivo |
In vivo, (±)-Norepinephrine (+)-bitartrate is used clinically as a vasopressor agent to treat hypotension and shock. It is administered intravenously to increase blood pressure by causing vasoconstriction and increasing cardiac output. The compound's effects on heart rate, blood pressure, and peripheral vascular resistance are well-characterized. In research, it is used to study sympathetic nervous system function and adrenergic receptor pharmacology.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (±)-Norepinephrine (+)-bitartrate involve radioligand binding studies using cell membranes expressing adrenergic receptors (α1, α2, β1, β2, β3). Competitive binding assays are performed using selective radiolabeled ligands to determine the compound's affinity (Ki) for each receptor subtype. Functional assays that measure receptor-mediated signaling, such as calcium mobilization, cAMP accumulation, or inositol phosphate accumulation, are employed to assess the compound's agonist activity and to determine EC50 values.
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| Cell Assay |
In vitro cellular assays for (±)-Norepinephrine (+)-bitartrate are conducted in cell lines expressing adrenergic receptors, such as HEK293 cells transfected with specific receptor subtypes, or in primary cells such as vascular smooth muscle cells, cardiomyocytes, or neurons. Cells are treated with varying concentrations of norepinephrine, and receptor-mediated signaling is assessed using appropriate readouts (calcium, cAMP, etc.). The compound's effects on cell contraction, proliferation, or other functional responses are also assessed.
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| Animal Protocol |
In vivo animal studies for (±)-Norepinephrine (+)-bitartrate are conducted in animal models to study its effects on cardiovascular function. Animals are administered the compound intravenously, and blood pressure, heart rate, and peripheral vascular resistance are monitored. The compound's effects on renal function, pulmonary function, and other organ systems are also studied. Pharmacokinetic studies are performed to determine the compound's half-life, volume of distribution, and clearance.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (±)-Norepinephrine (+)-bitartrate indicate that it has a molecular weight of 319.22 and a molecular formula of C12H17NO9. The compound is a catecholamine that is rapidly metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). It has a very short half-life (approximately 2 minutes) and is administered by continuous intravenous infusion. The compound is poorly absorbed orally and does not cross the blood-brain barrier to a significant extent. For storage, the powder should be kept under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological information for (±)-Norepinephrine (+)-bitartrate is derived from its clinical use as a vasopressor. Adverse effects include hypertension, tachycardia, arrhythmias, and tissue ischemia at the site of extravasation. The compound's use requires careful monitoring of blood pressure and cardiac function. Overdose can lead to severe hypertension, cerebral hemorrhage, and cardiac arrest.
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| References |
MacGregor DA, et al. Relative efficacy and potency of beta-adrenoceptor agonists for generating cAMP in human lymphocytes. Chest. 1996 Jan;109(1):194-200. [2]. Littlejohn NK, et al. Suppression of Resting Metabolism by the Angiotensin AT2 Receptor. Cell Rep. 2016 Aug 9;16(6):1548-60. |
| Additional Infomation |
(±)-Norepinephrine (+)-bitartrate is the salt form of the endogenous catecholamine neurotransmitter norepinephrine. It is used clinically as a vasopressor to treat hypotension and shock. The compound is also used in research to study adrenergic receptor pharmacology. It is available from pharmaceutical and research chemical suppliers.
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| Molecular Formula |
C12H17NO9
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| Molecular Weight |
319.26468
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| Exact Mass |
319.09
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| CAS # |
3414-63-9
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| Related CAS # |
108341-18-0 (bitartrate monohydrate);
51-40-1 (bitartrate) 51-41-2329-56-6 (HCl) 149-95-1
(d-isomer) 138-65-8 (dl-isomer) 55-27-6 (+ isomer HCl)
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| PubChem CID |
165118
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| Appearance |
White to off-white solid powder
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| Boiling Point |
442.6ºC at 760 mmHg
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| Flash Point |
221.5ºC
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
265
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1(C(O)CN)=CC=C(O)C(O)=C1.[C@H](O)(C(=O)O)[C@@H](O)C(=O)O
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| InChi Key |
WNPNNLQNNJQYFA-LREBCSMRSA-L
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| InChi Code |
1S/C8H11NO3.C4H6O6/c9-4-8(12)5-1-2-6(10)7(11)3-55-1(3(7)8)2(6)4(9)10/h1-3,8,10-12H,4,9H21-2,5-6H,(H,7,8)(H,9,10)/p-2/t1-,2-/m.1/s1
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| Chemical Name |
1,2-Benzenediol, 4-(2-amino-1-hydroxyethyl)-, (+-)-, (R-(R*,R*))- 2,3-dihydroxybutanedioate (1
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| Synonyms |
(±)-Arterenol (+)-bitartrate saltArterenol bitartrate, Norepinephrine bitartrate salt
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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) |
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 | 3.1322 mL | 15.6612 mL | 31.3224 mL | |
| 5 mM | 0.6264 mL | 3.1322 mL | 6.2645 mL | |
| 10 mM | 0.3132 mL | 1.5661 mL | 3.1322 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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