Rationally designed chimeric peptide of met-enkephalin and FMRFa-[D-Ala2, p-Cl-Phe4]YFa induce multiple opioid receptors mediated antinociception and up-regulate their expression

European Journal of Pharmacology

Volumn 638, Issue 1-3, 2010, Pages 54-60

  Vats, Ishwar Dutt ^a,b   Chaudhary, Snehlata ^a   Sharma, Ahuti ^a   Nath, Mahendra ^b   Pasha, Santosh ^a  

^a CSIR INSTITUTE OF GENOMICS AND INTEGRATIVE BIOLOGY   (India)

^b UNIVERSITY OF DELHI   (India)

Author keywords

Antinociception; Chimeric opioid peptides; Opioid receptor expression; Real time RT PCR; Tolerance

Indexed keywords

ANTINOCICEPTIVE AGENT; KAPPA OPIATE RECEPTOR; MESSENGER RNA; MORPHINE; MU OPIATE RECEPTOR; NALOXONAZINE; NALOXONE; NALTRINDOLE; NORBINALTORPHIMINE; OPIATE RECEPTOR; SIGMA OPIATE RECEPTOR; TYROSYL DEXTRO ALANYLGLYCYL 4 CHLOROPHENYLMETHIONYLLYSYLLYSYLLYSYLPHENYLALANYLMETHIONYLARGINYLPHENYLALANINAMIDE; TYROSYLGLYCYLGLYCYLPHENYLALANYLMETHIONYLLYSYLLYSYLLYSYLPHENYLALANYLMETHIONYLARGINYLPHENYLALANINAMIDE; UNCLASSIFIED DRUG; METENKEPHALIN; NARCOTIC ANALGESIC AGENT; NARCOTIC ANTAGONIST; OLIGOPEPTIDE; PEPTIDE; PHENYLALANYLMETHIONYLARGINYLPHENYLALANINAMIDE; YFA PEPTIDE, ALANYL(2)-P-CL-PHE(4)-;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; BRAIN; CHRONIC DRUG ADMINISTRATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG SELECTIVITY; DRUG SPECIFICITY; GENE EXPRESSION REGULATION; MALE; NONHUMAN; PAIN; PRIORITY JOURNAL; PROTEIN STRUCTURE; RAT; SPINAL CORD; STRUCTURE ACTIVITY RELATION; TAIL FLICK TEST; UPREGULATION; ANALOGS AND DERIVATIVES; ANIMAL; CHEMISTRY; DRUG EFFECTS; METABOLISM; PAIN MEASUREMENT; SYNTHESIS; TIME; TRANSCRIPTION INITIATION; WISTAR RAT;

ANALGESICS, OPIOID; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ENKEPHALIN, METHIONINE; FMRFAMIDE; MALE; OLIGOPEPTIDES; PAIN MEASUREMENT; PEPTIDES; RATS; RATS, WISTAR; RECEPTORS, OPIOID; TIME FACTORS; TRANSCRIPTIONAL ACTIVATION; UP-REGULATION; NARCOTIC ANTAGONISTS;

EID: 77953540045     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.02.060     Document Type: Article

References (38)

1. Allard M., Geoffre S., Legendre P., Vincent J.D., Simonnet G. Characterization of rat spinal cord receptors to FLFQPQRFamide, a mammalian morphine modulating peptide: a binding study. Brain Research 1989, 500:169-176.
2. Benyhe S., Farkas J., Toth G., Wollemann M. Met5-enkephalin-Arg6-Phe7, an endogenous neuropeptide, binds to multiple opioid and nonopioid sites in rat brain. Journal of Neuroscience Research 1997, 48:249-258.
3. Bhargava H.N., Matwyshyn G.A., Reddy P.L., Veeranna Effects of naltrexone on the binding of [3H]D-Ala2, Met-Phe4, Gly-ol5-enkephalin to brain regions and spinal cord and pharmacological responses to morphine in the rat. General of Pharmacology 1993, 24:1351-1357.
4. Bhargava H.N., Cao Y.J., Zhao G.M. Effect of 7-nitroindazole on tolerance to morphine, U-50, 488H and D-Pen2, D-Pen5] enkephalin in mice. Peptides 1997, 18:797-800.
5. Burford N.T., Tolbert L.M., Sadee W. Specific G protein activation and mu-opioid receptor internalization caused by morphine, DAMGO and endomorphin I. European Journal of Pharmacology 1998, 342:123-126.
6. Buzas B., Cox B.M. Quantitative analysis of mu and delta opioid receptor gene expression in rat brain and peripheral ganglia using competitive polymerase chain reaction. Neuroscience 1997, 76:479-489.
7. Chaturvedi K. Opioid peptides, opioid receptors and mechanism of down regulation. Indian Journal of Experimental Biology 2003, 41:5-13.
8. Clarke S., Zimmer A., Zimmer A.M., Hill R.G., Kitchen I. Region selective upregulation of micro-, delta- and kappa-opioid receptors but not opioid receptor-like 1 receptors in the brains of enkephalin and dynorphin knockout mice. Neuroscience 2003, 122:479-489.
9. Galina H.Z., Kastin A.J. Existence of antiopiate system as illustrated by MIF-1/Tyr-MIF-1. Life Sciences 1986, 39:2153-2159.
10. Goodman C.B., Elmer G.I., Yang H.-Y.T., Lee C.H., Rothman R.B. Modulation of opioid receptors by antiopioid peptides. The Pharmacology of Opioid Peptides 1995, 303-319. Harwood Academic Publishers, Singapore, gmbh. L.F. Tseng (Ed.).
11. Goodman C.B., Emilien B., Becketts K., Cadet J.L., Rothman R.B. Downregulation of m-opioid binding sites following chronic administration of NPFF and morphine. Peptides 1996, 17:389-397.
12. Gouarderes C., Sutak M., Zajac J.M., Jhamandas K. Antinociceptive effects of intrathecally administered F8Famide and FMRFamide in the rat. European Journal of Pharmacology 1993, 237:73-81.
13. Greenberg M.J., Painter S.D., Dobble K.E., Naggle G.T., Price D.A., Lehman H.K. The molluscan neurosecretory peptide FMRFamide: comparative pharmacology and relationship to the enkephalins. Federation Proceedings 1983, 42:82-86.
14. Gupta S., Pasha S., Gupta Y.K., Bhardwaj D.K. Chimeric peptide of met-enkephalin and FMRFa induces antinociception and attenuates development of tolerance to morphine antinociception. Peptides 1999, 20:471-478.
15. Gupta S., Pasha S., Gupta Y.K., Bhardwaj D.K. Effects of intracerebroventricularly administered chimeric peptide of Met-enkephalin and FMRFa-[d-Ala2] YFa- on antinociception and its modulation in mice. Brain Research Bulletin 2001, 55:51-57.
16. Hanif K., Gupta K., Gupta S., Gupta Y.K., Maiti S., Pasha S. Chimeric peptide of met-enkephalin and FMRFa: effect of chlorination on conformation and analgesia. Neurosciences Letters 2006, 403:131-135.
17. Horner K.A., Zadina J.E. Internalization and downregulation of mu opioid receptors by endomorphins and morphine in SH-SY5Y human neuroblastoma cells. Brain Research 2004, 1028:121-132.
18. 7. Proceedings of National Academy of Sciences U.S.A. 1980, 81:5512-5514.
19. 7, an endogenous opioid peptide, in cerebral cortex of human and rat. Life Sciences 2000, 67:61-71.
20. Law P.Y., Louie A.K., Loh H.H. Effect of pertussis toxin treatment on the downregulation of opiate receptors in neuroblastoma X glioma NG108-15 hybrid cells. Journal of Biological Chemistry 1985, 260:14818-14823.
21. Lee S.C., Yoburn B.C. The effect of nimodipine on opioid antagonist-induced upregulation and supersensitivity. Pharmacology Biochemistry and Behaviour 2000, 66:347-351.
22. Liu-Chen L.Y. Agonist-induced regulation and trafficking of kappa opioid receptors. Life Sciences 2004, 75:511-536.
23. 2 like mammalian peptide precipitates opiate-withdrawal syndrome in the rat. Peptides 1990, 11:277-280.
24. 2 like mammalian octapeptide: possible role in opiate dependence and abstinence. Peptides 1990, 11:969-972.
25. Mcconalogue K., Grady E.F., Minnis J., Balestra B., Tonini M., Brecha N.C., Bunnett N.W., Sternini C. Activation and internalization of the mu-opioid receptor by the newly discovered endogenous agonists, endomorphin-1 and endomorphin-2. Neuroscience 1999, 90:1051-1059.
26. 2]FMRFamide and other FMRFamide related peptides on mouse colonic propulsive motility: a structure-activity relationship study. Journal of Pharmacological and Experimental Therapeutics 1990, 254:809-814.
27. Raffa R.B., Kim A., Rice K.C., De Costa B.R., Codd E.E., Rothman R.B. Low affinity of FMRFa and four FaRPs (FMRFamide related peptides), including the mammalian-derived FaRPs F8Fa (NPFF) and A18Fa, for opioid μ, δ, κ1, κ2a or κ2b receptors. Peptides 1994, 15:401-404.
28. 7, present in high amounts in brain of rat, cattle and man, is an opioid agonist. Nature 1980, 288:88-90.
29. 2 -like immunoreactivity. Proceedings of National Academy of Sciences USA 1984, 81:5002-5005.
30. 5]enkephalin-induced internalization of the micro opioid receptor in the spinal cord of morphine tolerant rats. Neuroscience 2004, 125:541-543.
31. Vats I.D., Dolt K.S., Kumar K., Karar J., Nath M., Pasha S. YFa, a chimeric opioid peptide, induces kappa-specific antinociception with no tolerance development during 6days of chronic treatment. Journal of Neuroscience Research 2008, 86:1599-1607.
32. Vats I.D., Chaudhary S., Karar J., Nath M., Pasha M.A., Pasha S. Endogenous peptide: met-enkephalin-arg-phe, differently regulate expression of opioid receptors on chronic treatment. Neuropeptides 2009, 43:355-362.
33. Wang Y., Li J.G., Huang P., Xu W., Liu-Chen L.Y. Differential effects of agonists on adenylyl cyclase superactivation mediated by the kappa opioid receptors: adenylyl cyclase superactivation is independent of agonist-induced phosphorylation, desensitization, internalization, and downregulation. Journal of Pharmacological and Experimental Therapeutics 2003, 307:1127-1134.
34. Yang H.-Y.T., Panula P., Tang J., Costa E. Characterisation and localization of met5-enkephalin-Arg6-Phe7 stored in various rat brain regions. Journal of Neurochemistry 1983, 40:969-976.
35. Yang H.-Y.T., Fratta W., Majane E.A., Costa E. Isolation, sequencing, synthesis and pharmacological characterization of two brain neuropeptides that modulate the action of morphine. Proceedings of National Academy of Sciences U.S.A. 1985, 82:7757-7761.
36. Zadina J.E., Kastin A.J., Harrison L.M., Ge L.J., Chang S.L. Opiate receptor changes after chronic exposure to agonists and antagonists. Annals of New York Academy of Sciences 1995, 757:353-361.
37. Zhang F., Li J., Li J.G., Liu-Chen L.Y. (-)U50, 488H [(trans)-3, 4- dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneace tamide] induces internalization and downregulation of the human, but not the rat, kappa-opioid receptor: structural basis for the differential regulation. Journal of Pharmacological and Experimental Therapeutics 2002, 302:1184-1192.
38. Zhu J., Luo L.Y., Mao G.F., Ashby B., Liu-Chen L.Y. Agonistinduced desensitization and downregulation of the human kappa opioid receptor expressed in Chinese hamster ovary cells. Journal of Pharmacological and Experimental Therapeutics 1998, 285:28-36.