ライフサイエンスコーパス: endomorphin-2

1 ociceptin, while it did block the effects of endomorphin-2.

2 maximally effective concentration), but not endomorphin-2 (0.6 mM; an endogenous ligand for micro -o

3 austively stereodiversified library based on endomorphin-2 (1) to discover mu opioid receptor (MOR) l

4 slices with a micro-opioid receptor agonist (endomorphin-2, 100 nM).

5 -Me-Phe(4),Gly(5)-ol]-enkephalin (DAMGO) and endomorphin-2 activated inwardly rectifying K(+) current

6 or l-Pro, a more metabolically-stable d-Pro2-endomorphin-2 analog should produce longer analgesic act

7 lates, including enalaprilat, perindoprilat, endomorphin-2 and isoniazid, and subjected to biological

8 e exists for functional interactions between endomorphin-2 and MOR1.

9 ercising muscle and evoke a pressor reflex), endomorphin-2 and naloxone resulted in a significantly g

10 , N-MePhe(4), Gly-ol(5)]-enkephalin (DAMGO), endomorphin-2, and morphine in rat and mouse locus coeru

11 A small proportion of these endomorphin-2 axons contained MOR1, but many of the dend

12 ts by [N-Phe(1)]-nociceptin-(1-13)-NH(2) and endomorphin-2 by naloxone, was not due to some nonspecif

13 ail-flick test, analgesia elicited by either endomorphin-2, d-Pro2-endomorphin-2 or Ala-Pyrrolidonyl-

14 The endomorphin-2 derivative displayed increased activity at

15 previously reported that microinjections of endomorphin-2 (E-2; an endogenous mu-receptor agonist) i

16 d-Pro2-endomorphin-2 (ED50=0.05 microg) was more potent than en

17 in-2 (ED50=0.05 microg) was more potent than endomorphin-2 (ED50=30 microg) in significantly increasi

18 functional domains of the endogenous opioid endomorphin-2 (EM-2) and the tachykinin SP, respectively

19 c.v.) injections of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) in the rat brain to determine the s

20 us opioid peptides, endomorphin-1 (EM-1) and endomorphin-2 (EM-2), on mu opioid receptor (MOR) intern

21 activity of a constrained cyclic analogue of endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH(2)) and related

22 Endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH(2)) is an endoge

23 We find that the magnitude of spinal endomorphin 2 (EM2) antinociception not only varies with

24 We show that endomorphin-2 (EM2), an arrestin-biased ligand for micro

25 re and after systemic administration of EM1, endomorphin-2 (EM2), DAMGO, and morphine in the consciou

26 ously showed that intrathecal application of endomorphin 2 [EM2; the highly specific endogenous mu-op

27 el of pharmacological agonism confirmed that endomorphin-2 had a much lower operational efficacy for

28 idase IV plays a role in the inactivation of endomorphin-2 in vivo, and thereby modulates its central

29 However, endomorphin-2 induced faster desensitization of the K(+)

30 , has been described which should potentiate endomorphin-2-induced analgesia.

31 anatomical data support the hypothesis that endomorphin-2 is a ligand for MORs in the trigeminal dor

32 Together, these results indicate that endomorphin-2 is an arrestin-biased agonist at MOPr and

33 Endomorphin-2 is present in high density in the spinal a

34 sia elicited by either endomorphin-2, d-Pro2-endomorphin-2 or Ala-Pyrrolidonyl-2-nitrile returned aft

35 ia, and potentiated the analgesic actions of endomorphin-2, particularly on the tail-flick test.

36 d MOR1, but many of the dendritic targets of endomorphin-2 terminals contained MOR1.

37 , because the potencies of endomorphin-1 and endomorphin-2 to elicit internalization were unaffected

38 ason for this is likely to be the ability of endomorphin-2 to induce greater phosphorylation of MOPr

39 cells stably expressing MOPr, the ability of endomorphin-2 to induce phosphorylation of Ser375 in the

40 We confirmed the localization of endomorphin-2 to unmyelinated axons and axon terminals i

41 endomorphin 1 (Tyr-Pro-Trp-Phe-NH2; EM1) and endomorphin 2 (Tyr-Pro-Phe-Phe-NH2; EM2) in the rat cent

42 domorphin-1 (Tyr-Pro-Trp-Phe-NH(2); EM1) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH(2); EM2) have been loc

43 immunoreactive for the endogenous MOR ligand endomorphin-2 (Tyr-Pro-Phe-Phe-NH2) (EM-2) have been rep

44 A second peptide, endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), which differs by on

45 The tetrapeptide, endomorphin-2 (Tyr-Pro-Phe-PheNH2) possesses high affini

46 estigated this phenomenon in more detail for endomorphin-2, using endogenous MOPr in rat brain as wel

47 Consistent with previous studies, endomorphin-2 was contained primarily in dense core vesi

48 The present study found that endomorphin-2 was degraded approximately twice as fast t

49 , by dipeptidyl peptidase IV, whereas d-Pro2-endomorphin-2 was totally resistant to this enzyme's act

50 The effects of endomorphin 2 were qualitatively similar.

51 If endomorphin-2 were an endogenous ligand for the MOR1, we

52 f bilorphin and the strongly arrestin-biased endomorphin-2 with the MOPr indicate distinct receptor i