[Leu5]-Enkephalin, amide

Research use only, not for human use.

[Leu5]-Enkephalin, amide is a δ opioid receptor agonist. Enkephalin, one of several naturally occurring morphinelike substances (endorphins) released from nerve endings of the central nervous system and the adrenal medulla.

[Leu5]-Enkephalin, amide is a δ opioid receptor agonist. Enkephalin, one of several naturally occurring morphinelike substances (endorphins) released from nerve endings of the central nervous system and the adrenal medulla. (In Vitro):[Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC50 value of 2.1 nM.(In Vivo):Levels of [Leu5]-Enkephalin are significantly increased in the nucleus raphe magnus (NRM) of rats 2 weeks after the injection of complete Freund's 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 protein) compared with levels in saline-treated rats (0.38±0.02 pmol/mg protein; p<0.05).

[Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC50 value of 2.1 nM.

Levels of [Leu5]-Enkephalin are significantly increased in thenucleus raphe magnus (NRM) of rats 2 weeks after the injection of complete Freund's 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 protein) compared with levels in saline-treated rats (0.38±0.02 pmol/mg protein; p<0.05).

Leu-Enkephalin amide

Others

Other Targets

δ opioid receptor

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60117-24-0

554.64

C28H38N6O6

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (450.74 mM)

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Sequence:Tyr-Gly-Gly-Phe-Leu-NH2

(-20℃)

With Ice Pack

≥ 2 years