[Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
性状
Solid
IC50 & Target[1][2]
δ opioid receptor
体外研究(In Vitro)
[Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC50 value of 2.1 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Levels of [Leu5]-Enkephalin are significantly increased in the nucleus raphe magnus (NRM) of rats 2 weeks after the injection of complete Freunds adjuvant (CFA) (1.02±0.2 pmol/mg protein) as compared with saline-treated rats (0.49±0.04 pmol/mg protein; p<0.01). Tissue levels of [Leu5]-Enkephalin are uniformly increased in the caudal ventrolateral periaqueductal gray (PAG) 4 hr (1.15±0.25 pmol/mg protein), 4 d (1.16±0.18 pmol/mg protein), and 2 weeks (1.18±0.17 pmol/mg protein) after the injection of CFA as compared with saline-treated rats (0.55±0.03 pmol/mg protein; p<0.05, all times). A smaller increase in the levels of [Leu5]-Enkephalin occurred in the rostral aspect of the ventrolateral PAG at all time points. Finally, levels of [Leu5]-Enkephalin are also increased in the contralateral microcellular tegmental nucleus 4 d after the injection of CFA (0.53±0.04 pmol/mg
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
SequenceShortening
YGGFL-NH2
Sequence
Tyr-Gly-Gly-Phe-Leu-NH2
参考文献
[1]. Hurley RW, et al. Contribution of endogenous enkephalins to the enhanced analgesic effects of supraspinal mu opioid receptor agonists after inflammatory injury. J Neurosci. 2001 Apr 1;21(7):2536-45.[2]. Kennedy C, et al. [Met5]enkephalin acts via delta-opioid receptors to inhibit pelvic nerve-evoked contractions of cat distal colon. Br J Pharmacol. 1987 Oct;92(2):291-8.
溶解度数据
In Vitro: DMSO : 250 mg/mL (450.74 mM; Need ultrasonic)配制储备液