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Chemical Compound Review

Deproceptin     (2S)-N-[(2S)-1-[(2S)-2...

Synonyms: Morphiceptin, CHEMBL362991, HMDB05777, CHEBI:422134, DNC013044, ...
 
 
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Disease relevance of AIDS-002088

 

Psychiatry related information on AIDS-002088

 

High impact information on AIDS-002088

  • The synthetic peptide NH2-Tyr-Pro-Phe-Pro-CONH2 (morphiceptin), which is the amide of a fragment of the milk protein beta-casein, has morphinelike activities and is highly specific for morphine (mu) receptors but not for enkephalin (delta) receptors [9].
  • Morphiceptin did not activate phospholipase C-mediated phosphatidylinositol hydrolysis but did transiently activate (2- to 3-fold) phospholipase D (PLD), as measured by phosphatidylethanol formation in neuron cultures derived from embryonic day 6 or day 7 cerebral hemispheres [10].
  • Both morphiceptin (in a naloxone-reversible manner) and phorbol ester increased phosphorylation of similar cytosolic proteins in intact cells, demonstrating a functional role for the PKC-epsilon activation by opioids [10].
  • The mu-opioid peptide morphiceptin stimulated a Ca(2+)-independent protein kinase C (PKC-epsilon) that is expressed both in embryonic day 6 chicken telencephalon and in derived neuronal cultures [10].
  • The simultaneous addition of [D-Ala2, D-Leu5]-enkephalin and morphiceptin at concentrations at which 98% of enkephalin (delta) and morphine (mu) receptors are occupied only partially inhibits the binding of [3H]diprenorphine to rat brain membranes [11].
 

Chemical compound and disease context of AIDS-002088

 

Biological context of AIDS-002088

 

Anatomical context of AIDS-002088

 

Associations of AIDS-002088 with other chemical compounds

  • Two other selective mu agonists, trimu 5 and morphiceptin, inhibited cAMP production in membranes of striatal neurons as well [22].
  • Specific [3H]etorphine binding was also demonstrable after preincubation of NIL membranes with DAGO and (Leu5)enkephalin and after preincubation of Ht membranes with morphiceptin and (Leu5)enkephalin; such binding could be displaced by nonradioactive dynorphin A [23].
  • First, many DRG neurons responded to dynorphin A but not to morphiceptin or Leu-enkephalin [24].
  • In the present study we investigated and compared the in vivo analgesia of centrally administered endomorphin-2 and morphiceptin, and their analogs modified in position 3 [25].
  • Microinjections of saline, morphine sulfate, morphiceptin (specific mu agonist), D-pen-2-D-pen-5-enkephalin (delta agonist), and U-50488H (kappa agonist) were given to the freely moving animals (doses 0.8-2.4 x 10(-9) M, in a volume of 0.05 microliters of saline) [26].
 

Gene context of AIDS-002088

  • Furthermore, following intravenous administration of Tyr-Pro-Phe-Pro-NH2, a peptide that is exclusively hydrolyzed by DPP IV, urinary excretion of the peptide in the intact form was many-fold greater in DPP IV-negative rats than in control rats [27].
  • Chronic treatment with the low-efficacy mu-selective opioid peptide morphiceptin (10 microM; 3 days), but not with the highly potent mu-agonist DAGO (0.1 microM; 3 days) produced a comparable increase in G-protein abundance [28].
  • The intramolecular bridge created by cyclization of morphiceptin prevents dipeptidyl peptidase IV from interacting with these analogues [29].
  • [D-1-Nal3]Morphiceptin was the most potent analog of this series with a 26-fold increase in mu-opioid receptor affinity, a 15-fold potency increase in the GPI assay, and a significant potency increase in the hot-plate analgesic test, as compared with morphiceptin [30].
  • Interestingly, morphiceptin (a specific mu receptor agonist; 10 micrograms) markedly suppressed LH release, but only sparingly stimulated PRL release [31].
 

Analytical, diagnostic and therapeutic context of AIDS-002088

  • Specific radioimmunoassays have been developed for the measurement of naturally occurring morphiceptin and beta-casomorphin [20].
  • Various amounts of the mu-receptor agonists, morphine and morphiceptin, and the delta agonists, D-Ala2-D-Leu5-enkephalin (DADL) and Tyr-D-Ser-Gly-Phe-Leu-Thr (DSLET), were then administered intracerebroventricularly (icv) with continuous EEG monitoring [32].
  • The effect of MC was fully present in bilaterally vagotomized rats and in rats under artificial respiration [33].
  • Microinjections of morphiceptin and DPDPE failed to alter response thresholds for circling behavior also elicited from electrical stimulation of dorsal PAG [34].
  • The intrathecal injection of 1.25, 2.5 and 5 micrograms of [ NMePhe3 ,D-Pro4] morphiceptin (MC), a highly selective mu receptor agonist, in pentobarbital-anesthetized rats resulted in a dose-dependent decrease of mean arterial pressure, reaching a maximal effect 1 h after its administration [33].

References

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  2. Opioid peptides with differential affinity for mu and delta receptors decrease sensory neuron calcium-dependent action potentials. Werz, M.A., Macdonald, R.L. J. Pharmacol. Exp. Ther. (1983) [Pubmed]
  3. Selective activation of opioid receptors differentially affects lordosis behavior in female rats. Pfaus, J.G., Gorzalka, B.B. Peptides (1987) [Pubmed]
  4. Binding of the new morphiceptin analogs to human MCF-7 breast cancer cells and their effect on growth. Janecka, A., Fichna, J., Kosson, P., Zalewska-Kaszubska, J., Krajewska, U., Mirowski, M., Rozalski, M. Regul. Pept. (2004) [Pubmed]
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  10. Opioid peptides activate phospholipase D and protein kinase C-epsilon in chicken embryo neuron cultures. Mangoura, D., Dawson, G. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  11. Novel opiate binding sites selective for benzomorphan drugs. Chang, K.J., Hazum, E., Cuatrecasas, P. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  12. Cardiovascular responses to opioid agonists injected into the nucleus of tractus solitarius of anesthetized cats. Hassen, A.H., Feuerstein, G.Z., Faden, A.I. Life Sci. (1982) [Pubmed]
  13. Morphine and morphiceptin increase the threshold for epinephrine-induced cardiac arrhythmias in the rat through brain mu opioid receptors. Rabkin, S.W. Clin. Exp. Pharmacol. Physiol. (1993) [Pubmed]
  14. Dual effect of morphiceptin on lordosis behavior: possible mediation by different opioid receptor subtypes. Pfaus, J.G., Pendleton, N., Gorzalka, B.B. Pharmacol. Biochem. Behav. (1986) [Pubmed]
  15. Differential cardiovascular effects of mu, delta and kappa opiate agonists at discrete hypothalamic sites in the anesthetized rat. Feuerstein, G., Faden, A.I. Life Sci. (1982) [Pubmed]
  16. Morphine cross-reacts with somatostatin receptor SSTR2 in the T47D human breast cancer cell line and decreases cell growth. Hatzoglou, A., Ouafik, L., Bakogeorgou, E., Thermos, K., Castanas, E. Cancer Res. (1995) [Pubmed]
  17. Cyclic AMP protects against staurosporine and wortmannin-induced apoptosis and opioid-enhanced apoptosis in both embryonic and immortalized (F-11kappa7) neurons. Goswami, R., Dawson, S.A., Dawson, G. J. Neurochem. (1998) [Pubmed]
  18. Potent morphiceptin analogs: structure activity relationships and morphine-like activities. Chang, K.J., Wei, E.T., Killian, A., Chang, J.K. J. Pharmacol. Exp. Ther. (1983) [Pubmed]
  19. Characteristics of [3H]fentanyl binding to the opiate receptor. Villiger, J.W., Ray, L.J., Taylor, K.M. Neuropharmacology (1983) [Pubmed]
  20. Isolation of a specific mu-opiate receptor peptide, morphiceptin, from an enzymatic digest of milk proteins. Chang, K.J., Su, Y.F., Brent, D.A., Chang, J.K. J. Biol. Chem. (1985) [Pubmed]
  21. Opioid receptors on guinea-pig intestinal crypt epithelial cells. Lang, M.E., Davison, J.S., Bates, S.L., Meddings, J.B. J. Physiol. (Lond.) (1996) [Pubmed]
  22. Mu and delta opiate receptors coupled negatively to adenylate cyclase on embryonic neurons from the mouse striatum in primary cultures. Chneiweiss, H., Glowinski, J., Premont, J. J. Neurosci. (1988) [Pubmed]
  23. Opiate receptor subtypes in the rat hypothalamus and neurointermediate lobe. Stojilković, S.S., Dufau, M.L., Catt, K.J. Endocrinology (1987) [Pubmed]
  24. Dynorphin and neoendorphin peptides decrease dorsal root ganglion neuron calcium-dependent action potential duration. Werz, M.A., Macdonald, R.L. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  25. Characterization of antinociceptive activity of novel endomorphin-2 and morphiceptin analogs modified in the third position. Fichna, J., do-Rego, J.C., Kosson, P., Costentin, J., Janecka, A. Biochem. Pharmacol. (2005) [Pubmed]
  26. Effects of opioid microinjections in the nucleus of the solitary tract on the sleep-wakefulness cycle states in cats. Reinoso-Barbero, F., de Andrés, I. Anesthesiology (1995) [Pubmed]
  27. Hydrolysis and transport of proline-containing peptides in renal brush-border membrane vesicles from dipeptidyl peptidase IV-positive and dipeptidyl peptidase IV-negative rat strains. Tiruppathi, C., Miyamoto, Y., Ganapathy, V., Roesel, R.A., Whitford, G.M., Leibach, F.H. J. Biol. Chem. (1990) [Pubmed]
  28. Alterations in the expression of G-proteins and regulation of adenylate cyclase in human neuroblastoma SH-SY5Y cells chronically exposed to low-efficacy mu-opioids. Ammer, H., Schulz, R. Biochem. J. (1993) [Pubmed]
  29. Synthesis and electrophysiological characterization of cyclic morphiceptin analogues. Pil, J., Van der Veken, P., Bal, G., Augustyns, K., Haemers, A., Tytgat, J. Biochem. Pharmacol. (2004) [Pubmed]
  30. Opioid receptor binding and in vivo antinociceptive activity of position 3-substituted morphiceptin analogs. Fichna, J., do-Rego, J.C., Costentin, J., Chung, N.N., Schiller, P.W., Kosson, P., Janecka, A. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
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  32. Opiate-induced seizures: a study of mu and delta specific mechanisms. Snead, O.C. Exp. Neurol. (1986) [Pubmed]
  33. Depressor and bradycardic effect following intrathecal injection of [NMePhe3,D-Pro4]morphiceptin in rats. Li, S.J., Han, J.S. Eur. J. Pharmacol. (1984) [Pubmed]
  34. Affective defense behavior elicited from the feline midbrain periqueductal gray is regulated by mu and delta opioid receptors. Shaikh, M.B., Lu, C.L., Siegel, A. Brain Res. (1991) [Pubmed]
 
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