Levonordefrin
(Synonyms: (-)-3,4-二羟基去甲麻黄碱,(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) 目录号 : GC40807A vasoconstrictor
Cas No.:829-74-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Levonordefrin is the (-)-enantiomer of nordefrin, a synthetic derivative of norepinephrine , that acts as a vasoconstrictor. Levonordefrin (1-5 µg/kg) rapidly increases blood pressure and heart rate in anesthetized dogs and has a more potent effect on blood pressure than the dextronordefrin enantiomer. It also inhibits carbamylcholine-induced uterine contractions in isolated rat uterine strips (EC50 = 0.0032 µg/ml). Levonordefrin (0.514 and 1.542 mg/kg), in combination with mepivacaine and administered via intraoral infiltration, increases systolic arterial blood pressure in anesthetized dogs, however, the effect is not dose-dependent and the increase is not greater than 5.33%. Formulations containing levonordefrin have been used in combination with local anesthetics in dentistry to prolong anesthetic effects.
| Cas No. | 829-74-3 | SDF | |
| 别名 | (-)-3,4-二羟基去甲麻黄碱,(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin | ||
| Canonical SMILES | OC1=C(O)C=CC([C@@H](O)[C@@H](N)C)=C1 | ||
| 分子式 | C9H13NO3 | 分子量 | 183.2 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at -20°C; protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.4585 mL | 27.2926 mL | 54.5852 mL |
| 5 mM | 1.0917 mL | 5.4585 mL | 10.917 mL |
| 10 mM | 0.5459 mL | 2.7293 mL | 5.4585 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quantitative and qualitative analysis of the pressor effects of Levonordefrin
J Cardiovasc Pharmacol 1984 Sep-Oct;6(5):929-35.PMID:6209502DOI:10.1097/00005344-198409000-00029.
Levonordefrin, a common alternative to levoepinephrine as a vasoconstrictor in dental local anesthetic preparations, is usually used in fivefold higher concentrations, and, as such, is generally considered equivalent to epinephrine. We used anesthetized dogs that had autonomic reflexes blocked by mecamylamine to reevaluate the cardiovascular actions of intravenously administered nordefrin with respect to those of epinephrine and norepinephrine over a 100-fold dose range (0.1-10.0 micrograms/kg). Epinephrine caused a significantly greater pressor effect than nordefrin only at the highest dose studied; at low to moderate doses there was no significant difference between the two drugs. Blockade of alpha-adrenoceptors with phentolamine attenuated the peak pressor effects of all three agents. The epinephrine dose-response curve was suppressed more than the curves for norephinephrine and nordefrin, which were not significantly different from each other. Nordefrin was indistinguishable qualitatively from norepinephrine in that neither agent showed any evidence of beta 2-adrenoceptor vasodilation as seen with epinephrine. These findings suggest that nordefrin resembles norepinephrine rather than epinephrine in the receptor profile through which it produces its cardiovascular effects, and that the true potency difference between nordefrin and epinephrine with respect to pressor activity may be somewhat less than the fivefold difference commonly assumed.
A prospective, randomized, double-blind comparison of 2% mepivacaine with 1 : 20,000 Levonordefrin versus 2% lidocaine with 1 : 100,000 epinephrine for maxillary infiltrations
Anesth Prog 2010 Winter;57(4):139-44.PMID:21174567DOI:10.2344/0003-3006-57.4.139.
The purpose of this prospective, randomized, double-blind crossover study was to compare the anesthetic efficacy of 2% mepivacaine with 1 : 20,000 Levonordefrin versus 2% lidocaine with 1 : 100,000 epinephrine in maxillary central incisors and first molars. Sixty subjects randomly received, in a double-blind manner, maxillary central incisor and first molar infiltrations of 1.8 mL of 2% mepivacaine with 1 : 20,000 Levonordefrin and 1.8 mL of 2% lidocaine with 1 : 100,000 epinephrine at 2 separate appointments spaced at least 1 week apart. The teeth were electric pulp tested in 2-minute cycles for a total of 60 minutes. Anesthetic success (obtaining 2 consecutive 80 readings with the electric pulp tester within 10 minutes) was not significantly different between 2% mepivacaine with 1 : 20,000 Levonordefrin and 2% lidocaine with 1 : 100,000 epinephrine for the central incisor and first molar. However, neither anesthetic agent provided an hour of pulpal anesthesia.
Anesthetic efficacy and heart rate effects of the supplemental intraosseous injection of 2% mepivacaine with 1:20,000 Levonordefrin
Oral Surg Oral Med Oral Pathol Oral Radiol Endod 1999 Mar;87(3):284-93.PMID:10102587DOI:10.1016/s1079-2104(99)70210-6.
Objective: The purpose of this study was to determine the anesthetic efficacy and heart rate effects of a supplemental intraosseous injection of 2% mepivacaine with 1:20,000 Levonordefrin. Study design: Through use of a repeated-measures design, 40 subjects randomly received 3 combinations of injections at 3 separate appointments. The combinations were as follows: inferior alveolar nerve (IAN) block (with 3% mepivacaine) + intraosseous injection of 1.8 mL of 2% mepivacaine with 1:20,000 Levonordefrin; IAN block + intraosseous injection of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine (positive control); IAN block + mock intraosseous injection (negative control). Each first molar, second molar, and second premolar was blindly tested with a pulp tester at 2-minute cycles for 60 minutes after injection. Anesthesia was considered successful when 2 consecutive readings of 80 were obtained. Heart rate (pulse rate) was measured with a pulse oximeter. Results: One hundred percent of the subjects had lip numbness with the IAN block + intraosseous mock technique and IAN block + intraosseous techniques. The anesthetic success rates for IAN block + mock intraosseous injection, IAN block + intraosseous lidocaine, and IAN block + intraosseous mepivacaine, respectively, were as follows: 80%, 100%, and 100% for the first molar; 90%, 100%, and 100% for the second molar; 77%, 97%, and 97% for the second premolar. For the first molar and second premolar, the differences were significant (P< .05) when the intraosseous mepivacaine and lidocaine techniques were compared with the IAN block + mock intraosseous injection. There were no significant differences between the intraosseous mepivacaine and lidocaine techniques. Eighty percent of the subjects had a mean increase in heart rate of 23-24 beats per minute with the intraosseous injection of the mepivacaine and lidocaine solutions; there were no significant differences between results with the 2 solutions. Conclusions: We concluded that intraosseous injection of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine or 2% mepivacaine with 1:20,000 Levonordefrin, used to supplement an IAN block, significantly increased anesthetic success in first molars and second premolars. The 2 solutions were equivalent with regard to intraosseous anesthetic success rate, failure rate, and heart rate increase after IAN block.
Hypertensive response to Levonordefrin in a patient receiving propranolol: report of case
J Am Dent Assoc 1988 Jan;116(1):55-7.PMID:3278028DOI:10.14219/jada.archive.1988.0155.
Propranolol is a commonly used drug; of new and refilled prescriptions, it ranked no. 1 in 1984 and no. 2 in 1985. Medical conditions for its use include angina pectoris, myocardial infarction, hypertension, cardiac dysrhythmias, hypertrophic subaortic stenosis, migraine headache, hyperthyroidism, and pheochromocytoma. Almost all dental practitioners will treat a patient receiving propranolol for one of these conditions. The following recommendations seem appropriate at this time: The patient should continue to receive propranolol during dental treatment. Sudden withdrawal of the beta-blocker will cost the patient the benefit of propranolol therapy and may lead to acute myocardial ischemia. Acute stress should be minimized, as hypertensive responses may also be caused by endogenously released epinephrine. Short appointments scheduled in the morning, possibly with conscious sedation, should be considered. The dosage of adrenergic vasoconstrictors should be limited and gingival retraction cord containing epinephrine avoided entirely. The blood pressure should be taken approximately 5 minutes after local anesthesia is administered to determine if a systemic response has occurred. In the unlikely event of a hypertensive emergency, a rapidly acting, short-duration antihypertensive drug, such as the alpha-blocker phentolamine (Regitine, 5 mg intravenously) should be administered. Sublingual nitroglycerin (Nitrostat, 0.4 mg) may be useful as a nonparenteral alternative. These recommendations apply to other nonselective beta-blockers, including nadolol (Corgard) and timolol (Blocadren). They may also apply to labetalol (Normodyne, Trandate), a nonselective beta-antagonist with some alpha-blocking activity and to pindolol (Visken), a beta-blocker with some intrinsic beta 2-agonistic activity.(ABSTRACT TRUNCATED AT 250 WORDS)
An evaluation of 4% prilocaine with 1:200,000 epinephrine and 2% mepivacaine with 1:20,000 Levonordefrin compared with 2% lidocaine with:100,000 epinephrine for inferior alveolar nerve block
Anesth Prog 1991 May-Jun;38(3):84-9.PMID:1814249doi
The purpose of this study was to measure the degree of anesthesia obtained with 4% prilocaine with 1:200,000 epinephrine and 2% mepivacaine with 1:20,000 Levonordefrin compared with 2% lidocaine with 1:100,000 epinephrine for inferior alveolar nerve block. Using a repeated measures design, 30 subjects randomly received an inferior alveolar injection using masked cartridges of each solution at three successive appointments. The first molar, first premolar, lateral incisor, and contralateral canine (control) were blindly tested with an Analytic Technology pulp tester at 3-min cycles for 50 min. Anesthetic success was defined as no subject response to the maximum output of the pulp tester (80 reading) within 16 min and maintenance of this reading for the remainder of the testing period.Although subjects felt numb subjectively, anesthetic success as defined here occurred in 46% to 57% of the molars, in 50% to 57% of the premolars, and in 21% to 36% of the lateral incisors. No statistically significant differences in onset, success, failure, or incidence were found among the solutions. We conclude that the three preparations are equivalent for inferior alveolar nerve block of 50-min duration.