2-[125I]iodo-5-methoxycarbonylamino-N-acetyltryptamine: A selective radioligand for the characterization of melatonin ML2 binding sites

European Journal of Pharmacology

Volumn 301, Issue 1-3, 1996, Pages 159-168

  Molinari, Eduardo J ^a   North, Peter C ^b   Dubocovich, Margarita L ^a  

^a NORTHWESTERN UNIVERSITY   (United States)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

2 125I iodomelatonin; 2 125I MCA NAT (2 125I iodo 5 methoxy carbonylamino N acetyltryptamine); Brain, hamster; Kidney; Melatonin; Melatonin ML2 receptor; Testes

Indexed keywords

2 IODO 5 METHOXYCARBONYLAMINO N ACETYLTRYPTAMINE; 2-IODO-5-METHOXYCARBONYLAMINO-N-ACETYLTRYPTAMINE; CELL RECEPTOR; CELL SURFACE RECEPTOR; DIAGNOSTIC AGENT; LIGAND; MELATONIN RECEPTOR; RADIOACTIVE IODINE; TRYPTAMINE DERIVATIVE; 2 BROMO 5 METHOXYCARBONYLAMINO N ACETYLTRYPTAMINE; 2 IODOMELATONIN; 5 METHOXY N,N DIMETHYLTRYPTAMINE; 5 METHOXYLUZINDOLE; 5 METHOXYTRYPTAMINE; 6 CHLORO 2 METHYLMELATONIN; 6 CHLOROMELATONIN; 6 METHOXYTRYPTAMINE; FLUPHENAZINE; GALLOPAMIL; IODINE 125; KETANSERIN; LUZINDOLE; MELATONIN; MELATONIN ML1 RECEPTOR; MELATONIN ML2 RECEPTOR; METHYSERGIDE; N ACETYLSEROTONIN; N ACETYLTRYPTAMINE; PHENTOLAMINE; PRAZOSIN; RADIOLIGAND; RECEPTOR SUBTYPE; SEROTONIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; VERAPAMIL;

ANIMAL; ARTICLE; BRAIN; C3H MOUSE; CHICKEN; DRUG EFFECT; GUINEA PIG; HAMSTER; IN VITRO STUDY; KINETICS; MEMBRANE; METABOLISM; MOUSE; PHODOPUS; RABBIT; RAT; RETINA; SPRAGUE DAWLEY RAT; SYNTHESIS; SYRIAN HAMSTER; ANIMAL TISSUE; BINDING AFFINITY; BINDING COMPETITION; BINDING KINETICS; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG SELECTIVITY; DRUG SPECIFICITY; ISOTOPE LABELING; KIDNEY; MALE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR BINDING; TESTIS;

ANIMALS; BRAIN; CHICKENS; CRICETINAE; GUINEA PIGS; IODINE RADIOISOTOPES; KINETICS; LIGANDS; MEMBRANES; MESOCRICETUS; MICE; MICE, INBRED C3H; PHODOPUS; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CELL SURFACE; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, MELATONIN; RETINA; TRYPTAMINES;

EID: 0029658993     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/0014-2999(95)00870-5     Document Type: Article

References (45)

1. Acuña-Castroviejo, D., M.I. Pablos, A. Menendez-Pelaez and R.J. Reiter, 1993, Melatonin receptors in purified cell nuclei of liver, Res. Commun. Chem. Pathol. Pharmacol. 82, 253.
2. Acuña-Castroviejo, D., R.J. Reiter, A. Menendez-Pelaez, M.I. Pablos and A. Burgos, 1994, Characterization of high-affinity melatonin binding sites in purified cell nuclei of rat liver, J. Pineal Res. 16, 100.
3. Becker-Andre, M., I. Wiesenberg, N. Schaeren-Weimers, E. Andre, M. Missbach, J.-H. Saurat and C. Carlberg, 1994, Pineal gland hormone melatonin binds and activates an orphan of the nuclear receptor family, J. Biol. Chem. 269, 28531.
4. Benítez-King, G. and F. Antón-Tay, 1993. Calmodulin mediates melatonin cytoskeletal effects, Experientia 49, 635.
5. Bennett, J.P. and H.I. Yamamura, 1985, Neurotransmitter, hormone, or drug receptor binding models, in: Neurotransmitter Receptor Binding, eds. H.I. Yamamura, S.J. Enna and M.J. Kuhar (Raven Press, New York) 2nd edn., p. 61.
6. Bradford, M.M., 1976, A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding, Anal. Biochem. 72, 248.
7. Bubenik, G.A., L.P. Niles, S.F. Pang and P.J. Pentney, 1993, Diurnal variation and binding characteristics of melatonin in the mouse brain and gastrointestinal tissues, Comp. Biochem. Physiol., C: Comp. Pharmacol. 104, 221.
8. Cardinali, D.P., M.I. Vacas and E.E. Boyer, 1979, Specific binding of melatonin in bovine brain, Endocrinology 105, 437.
9. 50) of an enzymatic reaction, Biochem. Pharmacol. 22, 3099.
10. Coates, I.H., M.D. Dowle, K. Mills, D.E. Bays and C.F. Webb, 1982, Indole derivatives and their medicinal use. Belgian Patent 889931.
11. Cohen, M., D. Roselle, B. Chabner, T.J. Schmidt and M. Lippman, 1978, Evidence for a cytoplasmic melatonin receptor, Nature 274, 894.
12. Dubocovich, M.L., 1983, Melatonin is a potent modulator of dopamine release in the retina, Nature 306, 782.
13. Dubocovich, M.L., 1985, Characterization of a retinal melatonin receptor, J. Pharmacol. Exp. Ther. 234, 395.
14. Dubocovich, M.L., 1988a, Pharmacology and function of melatonin receptors, FASEB J. 2, 2765.
15. Dubocovich, M.L., 1988b, Luzindole (N-0774): a novel melatonin receptor antagonist, J. Pharmacol. Exp. Ther. 246, 902.
16. Dubocovich, M.L., 1995, Melatonin receptor: are there multiple subtypes?, Trends Pharmacol. Sci. 16, 50.
17. 125I]iodomelatonin to characterize melatonin binding sites in the chicken retina, Proc. Natl. Acad. Sci. USA 84, 3916.
18. 125I]iodomelatonin binding sites in hamster brain, Eur. J. Pharmacol. 132, 333.
19. 125I]Iodomelatonin binding sites in hamster brain membranes: pharmacological characteristics and regional distribution, Endocrinology 122, 1825.
20. 125I]iodomelatonin binding sites in Djungarian hamster brain, Endocrinology 125, 1011.
21. Ebisawa. T., S. Karne, M.R. Lerner and S.M. Reppert, 1994, Expression cloning of a high-affinity melatonin receptor from Xenopus dermal melanophores, Proc. Natl. Acad. Sci. USA 91, 6133.
22. Eison, A.S. and U.L. Mullins, 1993, Melatonin binding sites are functionally coupled to phosphoinositide hydrolysis in Syrian hamster RPMI 1846 melanoma cells, Life Sci. 53, 393.
23. Heward, C.B. and M.E. Hadley, 1975, Structure-activity relationships of melatonin and related indolamines, Life Sci. 17, 1167.
24. Kennaway, D.J. and H.M. Hugel, 1992, Melatonin binding sites: are they receptors?, Mol. Cell. Endocrinol. 88, C1.
25. Krause, D.N. and M.L. Dubocovich, 1990, Regulatory sites in the melatonin system of mammals, Trends Neurosci. 13, 464.
26. 125I]-iodomelatonin, FEBS Lett. 197, 9.
27. Menendez-Pelaez, A. and R.J. Reiter, 1993, Distribution of melatonin in mammalian tissue: the relative importance of nuclear versus cystosolic localization, J. Pineal Res. 15, 59.
28. Morgan, P.J., P. Barrett, H.E. Howell and R. Helliwell, 1994, Melatonin receptors: localization, molecular pharmacology and physiological significance, Neurochem. Int. 24, 101.
29. Mullins, U.L. and A.S. Eison, 1994, Pharmacologic characterization of melatonin-mediated phosphoinositide hydrolysis in pigeon brain, J. Pineal Res. 17, 33.
30. Niles, L.P., Y.W. Wong, R.K. Mishra and G.M. Brown, 1979, Melatonin receptors in brain, Eur. J. Pharmacol. 55, 219.
31. 125I]iodomelatonin labels multiple binding sites in hamster brain, Biochem. Biophys. Res Commun. 147, 949.
32. 125I]Iodomelatonin binding sites in hamster and chick exhibit differential sensitivity to prazosin. J. Pharm. Pharmacol. 41, 356.
33. Pickering, D.S. and L.P. Niles, 1990. Pharmacological characterization of melatonin binding sites in Syrian hamster hypothalamus, Eur. J. Pharmacol. 175, 71.
34. Pickering, D.S. and L.P. Niles, 1992, Expression of nanomolar-affinity binding sites for melatonin in Syrian hamster RPMI 1846 melanoma cells, Cell. Signal. 4, 201.
35. Popova, J.S. and M.L. Dubocovich, 1995, Melatonin receptor-mediated stimulation of phosphoinositide breakdown in chick brain slices, J. Neurochem. 64, 130.
36. Reiter, R.J., 1991, Pineal melatonin: cell biology of its synthesis and of its physiological interactions, Endocr. Rev. 12, 151.
37. Reppert, S.M., D.R. Weaver and T. Ebisawa, 1994, Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses, Neuron 13, 1177.
38. Song, Y., A.M. Poon, P.P. Lee and S.F. Pang, 1993, Putative melatonin receptors in the male guinea pig kidney, J. Pineal Res. 15, 153.
39. Stankov, B., F. Fraschini and R.J. Reiter, 1991, Melatonin binding sites in the central nervous system, Brain Res. 16, 245.
40. Sugden, D., 1991, Aggregation of pigment granules in single cultured Xenopus laevis melanophores by melatonin analogues, Br. J. Pharmacol. 104, 922.
41. Vakkuri, O., J. Leppaluoto and O. Vuolteenaho, 1984, Development and validation of a melatonin radioimmunoassay using radioiodinated melatonin as a tracer, Acta Endocrinol. 106, 152.
42. 2+ in neonatal rat pituitary cells, Endocrinology 130, 701.
43. Viswanathan, M., J.T. Laitinen and J.M. Saavedra, 1990, Expression of melatonin receptors in arteries involved in thermoregulation, Proc. Natl. Acad. Sci. USA 87, 6200.
44. Weisenberg, I., M. Missbach, J.-P. Kahlen, M. Schrader and C. Carlberg, 1995, Transcriptional activation of the nuclear receptor RZRα by the pineal gland hormone melatonin and identification of CGP 52608 as a synthetic ligand, Nucleic Acids Res. 23, 327.
45. 125I]Iodomelatonin binding sites in spleens of birds and mammals, Neurosci. Lett. 125, 175.