Endomorphin-1

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SKU: 4333 Category:

Endomorphin-1
(Human, Bovine)

4333-v 0.5 mg | 21.00 EUR

Tyr-Pro-Trp-Phe-NH2

(M.W. 610.70) C34H38N6O5 [189388-22-5]

4333-25 mg | 290.00 EUR

Tyr-Pro-Trp-Phe-NH2 · AcOH · H2O

(M.W. 610.70 · 60.05 · 18.01) C34H38N6O5 · CH3COOH · H2O

Synthetic Product

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.

References:

  1. J.E. Zadina, L. Hackler, L.J. Ge and A.J. Kastin, Nature, 386, 499 (1997) (Original; Bovine)
  2. 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.)
  3. 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.)
  4. L. Hackler, J.E. Zadina, L.J. Ge and A.J. Kastin, Peptides, 18, 1635 (1997) (Isolation from Human Brain)

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