4333-v 0.5 mg | 21.00 EUR
4333-25 mg | 290.00 EUR
Tyr-Pro-Trp-Phe-NH2 · AcOH · H2O
|(M.W. 610.70 · 60.05 · 18.01)||C34H38N6O5 · CH3COOH · H2O|
The purity is guaranteed to be higher than 99% by HPLC
Endomorphin-1 | Endogenous µ-Opiate Receptor Selective Agonist
The biological activity of Endomorphin-1 is examined by the Division of Pharmacology, Peptide Institute, Inc.
The discovery and isolation of a potent and selective agonist for the µ- opiate receptor from brain
More than three opioid-receptor subtypes, termed µ, δ, κ have been reported.
The endogenous ligand for δ -receptor is enkephalin, and that for κ -receptor is dynorphin.
Although opiate alkaloids morphine is well-known for the µ-selective and potent ligand, endogenous ligand "endogenous morphine" has never reported.
Recently, endogenous agonists for the µ-opiate receptor, were first isolated from bovine brain [Nature, 386, 499 (1997)]. These are endomorphin-1; Tyr-Pro-Trp-Phe-NH2, and endomorphin-2; Tyr-Pro-Phe-Phe-NH2. The isolation of relatively large amounts of endomorphin-1 and endomorphin-2 from human brain cortex has also reported [Peptides, 18, 1635 (1997)].
The immunoreactivity for endomorphin was also detected in rat brain near the µ-opiate receptor containing neurons, but the molecular form of the rat peptide has not yet been elucidated [Peptides, 18, 1641 (1997)]. These observations may be considered to indicate that endomorphin-1 and 2 are common µ-opiate agonists in mammals. In addition to the originally discovered µ-opiate agonistic function, these peptides have been reported to show hypotensive activity and Ca2+ channel current inhibitory activity [Biochem. Biophys. Res. Commun., 235, 567 (1997)]. Endomorphins would be useful for the study of pain perception together with some other biological functions in the body.
- J.E. Zadina, L. Hackler, L.J. Ge and A.J. Kastin, Nature, 386, 499 (1997) (Original; Bovine)
- H.C. Champion, J.E. Zadina, A.J. Kastin, L. Hackler, L.J. Ge and P.J. Kadowitz, Biochem. Biophys. Res. Commun, 235, 567 (1997) (Pharmacol.)
- L.S. Stone, C.A. Fairbanks, T.M. Laughlin, H.O. Nguyen, T.M. Bushy, M.W. Wessendorf and G.L. Wilcox, Neuroreport, 8, 3131 (1997) (Pharmacol.)
- L. Hackler, J.E. Zadina, L.J. Ge and A.J. Kastin, Peptides, 18, 1635 (1997) (Isolation from Human Brain)