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CAS No.: 58822-25-6

[Leu5]-Enkephalin/亮氨酸脑啡肽 Catalog No. CSN21444

Synonyms: Leu-enkephalin;Leucine enkephalin;Leucyl-enkephalin

[Leu5]-Enkephalin, an endogenous opioid neurotransmitter or neuromodulator, is an agonist of µ and δ opioid receptors.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors. [Leu5]-Enkephalin is a pentapeptides with morphine like properties, naturally present in mammalian brain^[1]. The antinociceptive effect of [Leu5]enkephalin administered intrathecally on the tail-flick test was increased more than 100-fold under i.t. pretreatment with three peptidase inhibitors. The antinociceptive effect produced by [Leu5]enkephalin in rats pretreated with any single peptidase inhibitor increased antinociception compared to that with saline^[2]. (D-Ala2, D-leu5)-enkephalin (1 mg/kg) treatment also markedly enhanced morphine analgesia^[3]. [D-Ala2, Met5]enkephalinamide and [D-Ala2, D-Leu5]enkephalin as well as [Met5]- and [Leu5]enkephalin increased contractility in a concentration-dependent manner. The enkephalin-induced maximal contractile effects were 28% and 30% above control, with EC50 values of 0.53 and 0.17 microM for [D-Ala2, Met5]enkephalinamide and [D-Ala2, D-Leu5]enkephalin, respectively. Enkephalins exert a direct positive inotropic effect on cultured heart cells, increasing contractile state via specific opiate receptors^[4].
参考文献

[1] Meunier JC, Moisand C. Binding of Leu5-enkephalin and Met5-enkephalin to a particulate fraction from rat cerebrum. FEBS Lett. 1977 May 15;77(2):209-13
[2] Miura M, Yoshikawa M, Watanabe M, Takahashi S, Ajimi J, Ito K, Ito M, Kawaguchi M, Kobayashi H, Suzuki T. Increase in antinociceptive effect of [leu5]enkephalin after intrathecal administration of mixture of three peptidase inhibitors. Tokai J Exp Clin Med. 2013 Jul 20;38(2):62-70
[3] Vaught JL, Takemori AE. Differential effects of leucine and methionine enkephalin on morphine-induced analgesia, acute tolerance and dependence. J Pharmacol Exp Ther. 1979 Jan;208(1):86-90
[4] Laurent S, Marsh JD, Smith TW. Enkephalins have a direct positive inotropic effect on cultured cardiac myocytes. Proc Natl Acad Sci U S A. 1985 Sep;82(17):5930-4

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7998 mL
- 8.9989 mL
- 17.9978 mL
- 5 mM
- 0.3600 mL
- 1.7998 mL
- 3.5996 mL
- 10 mM
- 0.1800 mL
- 0.8999 mL
- 1.7998 mL

技术信息

CAS号

58822-25-6

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H37N5O7

运输

蓝冰

分子量

555.62

别名

Leu-enkephalin;Leucine enkephalin;Leucyl-enkephalin;亮氨酸脑啡肽

溶解度

DMSO	145.0 mg/mL (261.0 mM) warming
Water	100.0 mg/mL (180.0 mM) warming

动物实验配方

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[Leu5]-Enkephalin/亮氨酸脑啡肽 Catalog No. CSN21444

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