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CAS No.: 64963-01-5

[D-Ala2]leucine-enkephalin Catalog No. CSN18678

Synonyms: Leuphasyl;NSC-374895

[D-Ala2]Leucine-Enkephalin is a potent, long-acting Leu-enkephalin analog agonist of delta opioid receptor.

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技术信息

生物活性

描述[D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin. The selective mu-opioid agonist [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAGO) (10 microM) reduced the short circuit (Isc) and the L-valine induced increase of the transepithelial potential difference and Isc(delta Vms and delta Isc) measured in-vitro in rabbit ileum, with a mechanism antagonized by naloxone (1 microM). [D-Ala2,D-Leu5]enkephalin (DADLE) (10 microM) had no significant effect on the transepithelial potential difference (Vms), Isc, delta Vms and delta Isc^[2]. Unilateral injections of DADL (D-leu5-enkephalin) into the ACB (nucleus accumbens) produced a depression of locomotor activity, followed by a stimulation^[3]. When injected into the ventromedial hypothalamus this peptide caused a dose-related increase in feeding which was rapid in onset and of short duration, and a short-lived increase in temperature. Since the delta-opioid agonist DADLE is more potent than the mu-agonist, morphine, and produces its effect more rapidly, the delta-opiate receptor may have an influence on the regulation of feeding^[4].
参考文献

[1] US4251438A
[2] Meyer G, Botta G, Tavani A, Algeri S, Cremaschi D. Effect of [D-Ala2,MePhe4,Gly-ol5]enkephalin and [D-Ala2,D-Leu5]enkephalin on ion and amino acid transport in rabbit ileum. J Pharm Pharmacol. 1989 Jul;41(7):494-5
[3] Havemann U, Winkler M, Kuschinsky K. The effects of D-ala2, D-Leu5-enkephalin injections into the nucleus accumbens on the motility of rats. Life Sci. 1983;33 Suppl 1:627-30
[4] Tepperman FS, Hirst M. Effect of intrahypothalamic injection of [D-Ala2,D-Leu5]enkephalin on feeding and temperature in the rat. Eur J Pharmacol. 1983 Dec 23;96(3-4):243-9

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
- 1.7555 mL
- 8.7773 mL
- 17.5547 mL
- 5 mM
- 0.3511 mL
- 1.7555 mL
- 3.5109 mL
- 10 mM
- 0.1755 mL
- 0.8777 mL
- 1.7555 mL

技术信息

CAS号

64963-01-5

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

C29H39N5O7

运输

蓝冰

分子量

569.65

别名

Leuphasyl;NSC-374895

溶解度

Water

50.0 mg/mL (87.8 mM) warming

动物实验配方

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