Endomorphin-2

Endogenous ligand Endomorphin-1,-2 Met/leu-enkephalin Dynorphin A Nociceptin/OFQ... 

Zadina JE, Martiri Schild S, Gerall AA, et al Endomorphins novel endogenous mu-opiate receptor agonists in regions of high mu-opiate receptor density. Ann N Y... 

Ahn SY, Cho CH, Park KG, Lee HI, Lee S, Park SK, Lee IK, Koh GY (2004) Tumor necrosis factor-alpha induces fractaUdne expression preferentially in arterial endothelial cells and mithramycin A suppresses TNF-alpha-induced fractaUdne expression. Am J Pathol 164 1663-1672 Alfano M, Schmidtmayerova H, Amelia CA, Pushkarsky T, Bukrinsky M (1999) The B-oligomer of pertussis toxin deactivates CC chemokine receptor 5 and blocks entry of M-tropic HIV-1 strains, [see comments]. J Exp Med 190 597-605 Ambrosini E, Alois F (2004) Chemokines and glial cells a complex network in the central nervous system. [Review] [239 refs]. Neurochem Res 29 1017-1038 Azuma Y, Ohura K (2002) Endomorphins 1 and 2 inhibit IL-10 and IL-12 production and innate immune functions, and potentiate NE-kappaB DNA binding in THP-1 differentiated to macrophagelike cells. Scand J Immunol 56 260-269... 

Perhaps most importantly, MOP agonists can potentiate HIV propagation in lymphocytes, monocytes, and monocyte-derived macrophages/microglia (Peterson et al. 1990 Carr and Serou 1995). This includes morphine (Peterson et al. 1990, 1999, 2004 Hu et al. 2005), methadone (Douglas 2001), and the MOP peptide agonist endomorphin (Peterson et al. 1999). The effects of morphine on HIV... 

Peterson PK, Gekker G, Hu S, Lokensgard J, Portoghese PS, Chao CC (1999) Endomorphin-1 potentiates HIV-1 expression in human brain cell cultmes implication of an atypical mu-opi-oid receptor. Neuropharmacology 38 273-278... 

The four opioid receptors display in vivo binding preference for mu-endorphins and endomorphins, delta-enkephalins, kappa-dynorphin and ORLl-nociceptin/orphanin FQ (Table 12.2). 

The opioid receptors are for the endogenous opioids, peptide transmitters, jS-endorphin, endomorphins, enkephalins, dynorphins and nociceptin. Thus all the problems of drugs based on peptides need to be overcome in order for the roles of these... 

Endogenous opioid /i-endorphin Endomorphins Enkephalins Dynorphins Nociceptin... 

Thyroliberin (thyrotropin-releasing hormone, Endomorphin 1 Methionine (MET)-enkephalin Cholecystokinin-8S (CCK-8S)... 

Endomorphin-2 (Tyr-Pro-Phe-NH ), a potent and selective MOR agonist, was used as a template for MOR antagonist design [54,55]. Replacing the N-terminal tyrosine residue with 2,6-dimethyltyrosine... 

Mizoguchi, H., Tseng, L. F., Suzuki, T., Sora, I. and Narita, M. Recent advances in the search for the p-opioidergic system differential mechanism of g-protein activation induced by endogenous p-opioid peptides, endomorphin and 5-endorphin. Jpn. J. Pharmacol. 89 239-244, 2002. 

Findings continue to accumulate in the field of endogenous opiates, as exemplified by two tetrapeptides isolated from mammalian brain and found to have high affinity and selectivity for p-opioid receptors. These tetrapeptides are endomorphin-1 (Tyr-Pro-Trp-Phe-NH2) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH2). A number of synthetic analogues have been prepared with the view to improve their metabolic stability and, in some cases, to limit their access to peripheral opioid receptors. The three synthetic endomor-phin analogues Tyr-D-Ala-Phe-Phe-NH2 (6.84), Tyr-D-Arg-Phe-Phe-NH2 (6.85), and Tyr-D-Arg-Phe-Ape-NH2 (6.86), to be discussed in the next section, have potent antinociceptive effects in in vivo inflammatory tests but exhibit modest effects in the CNS. However, and despite the presence of a D-amino acid and a protected C-terminus, they remained sensitive to enzymatic hydrolysis [211][212],... 

DPDPE—D-Pen2, D-Pen5-enkephalin DSLET—D-Ser2, Leu5-enkephalin, Thr6 DYN—Dynorphin EM—endomorphin ENK— enkephalin j8-FNA—j8-funaltrexamine, NTH—naltrindole 5 -isothiocyanate nor-BNI—Nor-binaltorphimine. 

Precursor peptides (1)pro-endomorphin (2)pro-opiomelanocortin, <3)pro-enkephalin, (4)pro-dynorphin, (5)pro-nociceptin ( presumed to exist). 

Endomorphins and nociceptin - subtype selective endogenous opioids... 

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