| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| References | |
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| Additional Infomation |
Alpha-methylnoradrenaline is a catecholamine in which the 2-aminoethyl group is substituted with a hydroxy group at C-1 and a methyl group at C-2, with configurations 1R,2S. A metabolite of alpha-methyl-L-dopa, it is an alpha2-adrenergic agonist and acts as a topical nasal decongestant and vasoconstrictor, most often used in dentistry. It has a role as an alpha-adrenergic agonist, a vasoconstrictor agent and a nasal decongestant.
Levonordefrin acts as a topical nasal decongestant and vasoconstrictor, most often used in dentistry. Levonordefrin is the levoisomer of nordefrin, a synthetic catecholamine and norepinephrine derivative with sympathomimetic and antihypertensive effects. Levonordefrin's antihypertensive effect is exerted through activation of alpha 2-adrenergic receptors in the cardiovascular control center of the CNS thereby suppressing the sympathetic output from the brain and subsequently lowering blood pressure. Levonordefrin binds to and activates peripheral alpha 2- adrenergic receptors, thereby causing vasoconstriction. A norepinephrine derivative used as a vasoconstrictor agent. Drug Indication Used as a topical nasal decongestant and vasoconstrictor in dentistry. Mechanism of Action It is designed to mimic the molecular shape of adrenaline. It binds to alpha-adrenergic receptors in the nasal mucosa. Here it can, therefore, cause vasoconstriction. Pharmacodynamics Levonordefrin is a sympathomimetic amine used as a vasoconstrictor in local anesthetic solutions. It has pharmacologic activity similar to that of Epinephrine but it is more stable than Epinephrine. In equal concentrations, Levonordefrin is less potent than Epinephrine in raising blood pressure, and as a vasoconstrictor. |
| Exact Mass |
183.09
|
|---|---|
| CAS # |
829-74-3
|
| Related CAS # |
829-74-3 (freebase);10390-18-8 (HCl);
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| PubChem CID |
164739
|
| Appearance |
Off-white to light brown solid powder
|
| Density |
1.328g/cm3
|
| Boiling Point |
431.575ºC at 760 mmHg
|
| Melting Point |
212-215ºC dec.
|
| Flash Point |
214.809ºC
|
| Index of Refraction |
1.633
|
| LogP |
1.178
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
|
| Complexity |
165
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
[C@H](C1C=CC(O)=C(O)C=1)(O)[C@@H](N)C
|
| InChi Key |
GEFQWZLICWMTKF-CDUCUWFYSA-N
|
| InChi Code |
InChI=1S/C9H13NO3/c1-5(10)9(13)6-2-3-7(11)8(12)4-6/h2-5,9,11-13H,10H2,1H3/t5-,9-/m0/s1
|
| Chemical Name |
4-[(1R,2S)-2-amino-1-hydroxypropyl]benzene-1,2-diol
|
| Synonyms |
Neo-CobefrineNordefrin α-methylnorepinephrineLevonordefrin Corbadrine
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| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~272.93 mM)
H2O : ~5 mg/mL (~27.29 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (13.65 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (13.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02603198 | UNKNOWN STATUS | Drug: mepivacaine chloridrato epinephrine Drug: mepivacaine chloridrato levonordefrin |
Edema Pain Trismus |
University of Sao Paulo | 2014-08 | Not Applicable |
| NCT04561921 | UNKNOWN STATUS | Drug: Magnesium sulfate Drug: Mepivacaine-Levonordefrin Hydrochloride |
Success of Inferior Alveolar Nerve Block | Cairo University | 2020-10-22 | Not Applicable |
| NCT05875519 | ACTIVE, NOT RECRUITING | Drug: Local anaesthesia with vasocontrictor (Mepivacaine hydrochloride 20 mg (2%) + Levonordefrin hydrochloride 0.06 mg) |
Anesthesia, Local Diabetes |
Minia University | 2023-05-01 | Not Applicable |
| NCT03745105 | UNKNOWN STATUS | Drug: Dexamethasone sodium phosphate Drug: Piroxicam Injectable Solution Drug: Mepivacaine HCL |
Postoperative Pain | Cairo University | 2018-12-25 | Not Applicable |
| NCT04477317 | COMPLETED | Drug: 4% Articaine Hydrochloride with 1:100,000 Adrenaline Drug: 2% Mepivacaine Hydrochloride with 1:20,000 Levonordefrin |
Local Anesthesia | Cairo University | 2021-08-01 | Phase 3 |
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