Molecular Formula | C28H38N6O6 |
Molar Mass | 554.64 |
Density | 1.254±0.06 g/cm3(Predicted) |
Melting Point | 123-126 °C |
Boling Point | 1012.8±65.0 °C(Predicted) |
pKa | 9.97±0.15(Predicted) |
Storage Condition | −20°C |
In vitro study | [Leu5]-Enkephalin causes concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC 50 value of 2.1 nM. |
In vivo study | 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). |
WGK Germany | 3 |
biological activity | [Leu5]-Enkephalin, amide is a delta opioid receptor (opioid receptor) agonist. |
target | δ opioid receptor |
in vitro research | [Leu5]-Enkephalin concentration-dependent, reversible inhibition of pelvic nerve-evoked contractions, with an IC 50 value of 2.1 nM. |
in vivo studies | 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). |