产品说明书

[Leu5]-Enkephalin

Print
Chemical Structure| 58822-25-6 同义名 : Leu-enkephalin;Leucine enkephalin;Leucyl-enkephalin
CAS号 : 58822-25-6
货号 : A994782
分子式 : C28H37N5O7
纯度 : 98%
分子量 : 555.623
MDL号 : MFCD00076406
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(215.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(179.98 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL
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