Characterization of the binding of [3H][Dmt1]H-Dmt-D-Arg-Phe-Lys-NH2, a highly potent opioid peptide

Journal of Pharmacology and Experimental Therapeutics

Volumn 306, Issue 2, 2003, Pages 430-436

  Neilan, Claire L ^a   Janvey, Adam J ^a   Bolan, Elizabeth ^a   Berezowska, Irena ^b   Nguyen, Thi M D ^b   Schiller, Peter W ^b   Pasternak, Gavril W ^a,c  

^a MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

^b CLIN RESEARCH INSTITUTE OF MONTREAL   (Canada)

^c Department of Neurology ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2',6' DIMETHYLTYROSINE; 3 METHOXYNALTREXONE; 3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE METHANESULFONATE; CODEINE; DERMORPHIN DERIVATIVE; DEXTRO PHENYLALANYLCYSTEINYLTYROSYL DEXTRO TRYPTOPHYLARGINYLTHREONYLPENICILLAMINYLTHREONINAMIDE 2,7 DISULFIDE; DIPRENORPHINE; DIVALENT CATION; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; ENKEPHALIN[2,5 DEXTRO PENICILLAMINE]; FENTANYL; GUANINE NUCLEOTIDE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); METHADONE; MORPHINE; MU OPIATE RECEPTOR; MU OPIATE RECEPTOR AGONIST; MU OPIATE RECEPTOR ANTAGONIST; NALOXONE; NALOXONE BENZOYLHYDRAZONE; NALTREXONE DERIVATIVE; OPIATE PEPTIDE; SODIUM CHLORIDE; SODIUM ION; TYROSINE DERIVATIVE; TYROSYL DEXTRO ARGINYLPHENYLALANYLLYSINAMIDE; UNCLASSIFIED DRUG; ANALGESIC AGENT; ION; NUCLEOTIDE; OLIGOPEPTIDE; SULFUR; TRITIUM; TYROSYL ARGINYL PHENYLALANYL LYSINAMIDE; TYROSYL-ARGINYL-PHENYLALANYL-LYSINAMIDE;

ANALGESIA; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; BRAIN MEMBRANE; CATTLE; CONTROLLED STUDY; DRUG CROSS TOLERANCE; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; NONHUMAN; NUCLEIC ACID PROBE; PRIORITY JOURNAL; RADIOASSAY; SPINAL CORD; ALTERNATIVE RNA SPLICING; ANIMAL; BINDING SITE; DRUG POTENTIATION; METABOLISM; MOUSE;

ALTERNATIVE SPLICING; ANALGESICS; ANIMALS; BINDING SITES; CATTLE; ENKEPHALIN, ALA(2)-MEPHE(4)-GLY(5)-; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); IONS; MICE; NUCLEOTIDES; OLIGOPEPTIDES; OPIOID PEPTIDES; RECEPTORS, OPIOID, MU; SULFUR RADIOISOTOPES; TRITIUM;

EID: 0038637219     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.103.049742     Document Type: Article

References (36)

1. Abbadie C and Pasternak GW (2001) Differential in vivo internalization of MOR-1 and MOR-1C by morphine. Neuroreport 12:3069-3072.
2. Bare LA, Mansson E, and Yang D (1994) Expression of two variants of the human μ opioid receptor mRNA in SK-N-SH cells and human brain. FEBS Lett 354:213-216.
3. Brown GP, Yang K, King MA, Rossi GC, Leventhal L, Chang A, and Pasternak GW (1997a) 3-Methoxynaltrexone, a selective heroin/morphine-6β -glucuronide antagonist. FEBS Lett 412:35-38.
4. 3H-Morphine-6β-glucuronide binding in brain membranes and an MOR-1-transfected cell line. J Pharmacol Exp Ther 282:1291-1297.
5. Burford NT, Tolbert LM, and Sadee W (1998) Specific G protein activation and μ-opioid receptor internalization caused by morphine, DAMGO and endomorphin I. Eur J Pharmacol 342:123-126.
6. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
7. Cherny N, Ripamonti C, Pereira J, Davis C, Fallon M, McQuay H, Mercadante S, Pasternak G, and Ventafridda V (2001) Strategies to manage the adverse effects of oral morphine: an evidence-based report. J Clin Oncol 19:2542-2554.
8. Childers SR and Snyder SH (1980) Differential regulation by guanine nucleotides of opiate agonist and antagonist receptor interactions. J Neurochem 34:583-593.
9. 1 binding assay. Mol Pharmacol 34:308-317.
10. 3 subtype. J Pharmacol Exp Ther 251:461-468.
11. Fairbanks CA, Stone LS, Kitto KF, Nguyen HO, Posthumus IJ, and Wilcox GL (2002) α(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. J Pharmacol Exp Ther 300:282-290.
12. Keith DE, Anton B, Murray SR, Zaki PA, Chu PC, Lissin DV, Monteillet-Agius G, Stewart PL, Evans CJ, and Von Zastrow M (1998) μ-Opioid receptor internalization: opiate drugs have differential effects on a conserved endocytic mechanism in vitro and in the mammalian brain. Mol Pharmacol 53:377-384.
13. Koch T, Schulz S, Pfeiffer M, Klutzny M, Schroder H, Kahl E, and Hollt V (2001) C-terminal splice variants of the mouse β-opioid receptor differ in morphine-induced internalization and receptor resensitization. J Biol Chem 276:31408-31414.
14. Lange DG, Roerig SC, and Fujimoto JM (1980) Absence of cross-tolerance to heroin in morphine-tolerant mice. Science (Wash DC) 206:72-74.
15. 1]DALDA analgesia. Brain Res 974:254-257.
16. 1]DALDA, a highly potent and selective μ-opioid peptide. Eur J Pharmacol 419:15-23.
17. Ossipov MH, Harris S, Lloyd P, and Messineo E (1990) An isobolographic analysis of the antinociceptive effect of systemically and intrathecally administered combinations of clonidine and opiates. J Pharmacol Exp Ther 255:1107-1116.
18. Ossipov MH, Suarez LJ, and Spaulding TC (1989) Antinociceptive interactions between α2-adrenergic and opiate agonists at the spinal level in rodents. Anesth Analg 68:194-200.
19. Pan YX, Xu J, Bolan EA, Abbadie C, Chang A, Zuckerman A, Rossi GC, and Pasternak GW (1999) Identification and characterization of three new alternatively spliced μ opioid receptor isoforms. Mol Pharmacol 56:396-403.
20. Pan YX, Xu J, Bolan E, Chang A, Mahurter L, Rossi G, and Pasternak GW (2000) Isolation and expression of a novel alternatively spliced μ opioid receptor isoform, MOR-1F. FEBS Lett 466:337-340.
21. Pan Y-X, Xu J, Mahurter L, Bolan EA, Xu MM, and Pasternak GW (2001) Generation of the μ opioid receptor (MOR-1) protein by three new splice variants of the Oprm gene. Proc Natl Acad Sci USA 98:14084-14089.
22. Pasternak GW (2001) The pharmacology of μ analgesics: from patients to genes. Neuroscientist 7:220-231.
23. 3H]opiate agonist binding by divalent cations. Mol Pharmacol 11:478-484.
24. Payne R and Pasternak GW (1992) Pharmacology of pain treatment, in Contemporary Neurologic Series: Scientific Basis of Neurologic Drug Therapy (Johnston MV, MacDonald R, and Young AB eds) pp 268-301, Davis, Philadelphia.
25. Pert CB, Pasternak GW, and Snyder SH (1973) Opiate agonists and antagonists discriminated by receptor binding in brain. Science (Wash DC) 182:1359-1361.
26. 1]DALDA is highly selective and potent at μ opioid receptors, but is not cross-tolerant with systemic morphine. Curr Med Chem 9:31-39.
27. Rossi GC, Brown GP, Leventhal L, Yang K, and Pasternak GW (1996) Novel receptor mechanisms for heroin and morphine-6β-glucuronide analgesia. Neurosci Lett 216:1-4.
28. Rossi GC, Pan Y-X, Brown GP, and Pasternak GW (1995) Antisense mapping the MOR-1 opioid receptor: evidence for alternative splicing and a novel morphine-6β-glucuronide receptor. FEBS Lett 369:192-196.
29. Schiller PW, Nguyen TMD, Berezowska I, and Dupuis S (2000) Synthesis and in vitro opioid activity profiles of DALDA analogues. Eur J Med Chem 35:895-901.
30. Schuller AG, King MA, Zhang J, Bolan E, Pan YX, Morgan DJ, Chang A, Czick ME, Unterwald EM, Pasternak GW, et al. (1999) Retention of heroin and morphine-6β-glucuronide analgesia in a new line of mice lacking exon 1 of MOR-1. Nat Neurosci 2:151-156.
31. Selley DE, Cao CC, Liu QX, and Childers SR (2000) Effects of sodium on agonist efficacy for G-protein activation in μ-opioid receptor-transfected CHO cells and rat thalamus. Br J Pharmacol 130:987-996.
32. 1]DALDA. J Pharmacol Exp Ther 297:364-371.
33. Szeto HH, Lovelace JL, Fridland G, Soong Y, Fasolo J, Wu D, Desiderio DM, and Schiller PW (2001) In vivo pharmacokinetics of selective μ-opioid peptide agonists J Pharmacol Exp Ther 298:57-61.
34. Walker JR, King M, Izzo E, Koob GF, and Pasternak GW (1999) Antagonism of heroin and morphine self-administration in rats by the morphine-6β-glucuronide antagonist 3-methylnaltrexone. Eur J Pharmacol 383:115-119.
35. Wolozin BL and Pasternak GW (1981) Classification of multiple morphine and enkephalin binding sites in the central nervous system. Proc Natl Acad Sci USA 78:6181-6185.
36. Zimprich A, Simon T, and Hollt V (1995) Cloning and expression of an isoform of the rat μ opioid receptor (rMOR 1B) which differs in agonist induced desensitization from rMOR1. FEBS Lett 359:142-146.