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Article: Differential inhibitory effects of melatonin analogs and three naphthalenic ligands on 2-[ 125I]iodomelatonin binding to chicken tissues

TitleDifferential inhibitory effects of melatonin analogs and three naphthalenic ligands on 2-[ 125I]iodomelatonin binding to chicken tissues
Authors
KeywordsIc 50
Melatonin Receptors
Naphthalenic Ligands
Pineal Gland Diurnal Rhythms
Issue Date1997
PublisherBlackwell Munksgaard. The Journal's web site is located at http://www.blackwellpublishing.com/journals/JPI
Citation
Journal Of Pineal Research, 1997, v. 23 n. 3, p. 148-155 How to Cite?
AbstractWe have compared the 50% inhibition values of 2-[ 125I]iodomelatonin ([ 125I]Mel) competition curves by melatonin and 3 naphthalenic ligands, N-[2-(7-methoxy-1-naphthyl) ethyl] cyclobutane carboxamide (S20642), N-propyl N-[2-(7-methoxy-1-naphtyl) ethyl] urea (S20753), and N-[2-(7-methoxy-1-naphthyl) ethyl] crotonamide (S20750), using membrane preparations of four tissues (lung, spleen, brain, and kidney) of the chicken simultaneously. In retired breeders, we have demonstrated that the affinities of S20642 were similar in the lung and spleen. However they were 2-fold lower in the brain and 80-fold lower in the kidney. Similar differential binding affinities to the melatonin receptors were observed in the four tissues of young male chicks. This suggests that age and sex have little influence on the differential inhibitory properties of melatonin and S20642 in the tissues studied. The addition of guanosine 5′-O-thiotriphosphate (GTPγS), which encouraged the uncoupling of melatonin receptor to the G protein complex, lowered the binding affinity of melatonin and S20642 in the tissues studied but their differential affinities in the four tissues were however maintained. The affinities of 5-methoxy-N-cyclopropanoyltryptamine (CPMT) in the kidney were also 5-10-fold lower than those in the lung, spleen, and brain of young male chicks. The distinctive differential affinities of melatonin, S20642, and CPMT for [ 125I]Mel binding sites in the chicken lung, spleen, brain, and kidney indicated that the binding sites in these tissues are heterogeneous. Our study implicated that the naphthalenic ligand S20642 may be a useful melatonin analog to distinguish melatonin receptor subtypes in tissues and a possible drug candidate worthwhile for further investigations. © Munksgaard, Copenhagen.
Persistent Identifierhttp://hdl.handle.net/10722/172377
ISSN
2015 Impact Factor: 9.314
2015 SCImago Journal Rankings: 2.655
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorPang, CSen_US
dc.contributor.authorTang, PLen_US
dc.contributor.authorSong, Yen_US
dc.contributor.authorPang, SFen_US
dc.contributor.authorNg, KWen_US
dc.contributor.authorGuardiolaLemaitre, Ben_US
dc.contributor.authorDelagrange, Pen_US
dc.contributor.authorBrown, GMen_US
dc.date.accessioned2012-10-30T06:22:14Z-
dc.date.available2012-10-30T06:22:14Z-
dc.date.issued1997en_US
dc.identifier.citationJournal Of Pineal Research, 1997, v. 23 n. 3, p. 148-155en_US
dc.identifier.issn0742-3098en_US
dc.identifier.urihttp://hdl.handle.net/10722/172377-
dc.description.abstractWe have compared the 50% inhibition values of 2-[ 125I]iodomelatonin ([ 125I]Mel) competition curves by melatonin and 3 naphthalenic ligands, N-[2-(7-methoxy-1-naphthyl) ethyl] cyclobutane carboxamide (S20642), N-propyl N-[2-(7-methoxy-1-naphtyl) ethyl] urea (S20753), and N-[2-(7-methoxy-1-naphthyl) ethyl] crotonamide (S20750), using membrane preparations of four tissues (lung, spleen, brain, and kidney) of the chicken simultaneously. In retired breeders, we have demonstrated that the affinities of S20642 were similar in the lung and spleen. However they were 2-fold lower in the brain and 80-fold lower in the kidney. Similar differential binding affinities to the melatonin receptors were observed in the four tissues of young male chicks. This suggests that age and sex have little influence on the differential inhibitory properties of melatonin and S20642 in the tissues studied. The addition of guanosine 5′-O-thiotriphosphate (GTPγS), which encouraged the uncoupling of melatonin receptor to the G protein complex, lowered the binding affinity of melatonin and S20642 in the tissues studied but their differential affinities in the four tissues were however maintained. The affinities of 5-methoxy-N-cyclopropanoyltryptamine (CPMT) in the kidney were also 5-10-fold lower than those in the lung, spleen, and brain of young male chicks. The distinctive differential affinities of melatonin, S20642, and CPMT for [ 125I]Mel binding sites in the chicken lung, spleen, brain, and kidney indicated that the binding sites in these tissues are heterogeneous. Our study implicated that the naphthalenic ligand S20642 may be a useful melatonin analog to distinguish melatonin receptor subtypes in tissues and a possible drug candidate worthwhile for further investigations. © Munksgaard, Copenhagen.en_US
dc.languageengen_US
dc.publisherBlackwell Munksgaard. The Journal's web site is located at http://www.blackwellpublishing.com/journals/JPIen_US
dc.relation.ispartofJournal of Pineal Researchen_US
dc.subjectIc 50en_US
dc.subjectMelatonin Receptorsen_US
dc.subjectNaphthalenic Ligandsen_US
dc.subjectPineal Gland Diurnal Rhythmsen_US
dc.titleDifferential inhibitory effects of melatonin analogs and three naphthalenic ligands on 2-[ 125I]iodomelatonin binding to chicken tissuesen_US
dc.typeArticleen_US
dc.identifier.emailNg, KW: kaing@hkucc.hku.hken_US
dc.identifier.authorityNg, KW=rp00765en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1111/j.1600-079X.1997.tb00348.x-
dc.identifier.pmid9406986-
dc.identifier.scopuseid_2-s2.0-0031241103en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0031241103&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume23en_US
dc.identifier.issue3en_US
dc.identifier.spage148en_US
dc.identifier.epage155en_US
dc.identifier.isiWOS:A1997YG06900006-
dc.publisher.placeDenmarken_US
dc.identifier.scopusauthoridPang, CS=7201425191en_US
dc.identifier.scopusauthoridTang, PL=16140906500en_US
dc.identifier.scopusauthoridSong, Y=25960367300en_US
dc.identifier.scopusauthoridPang, SF=7402528719en_US
dc.identifier.scopusauthoridNg, KW=7403178774en_US
dc.identifier.scopusauthoridGuardiolaLemaitre, B=7003761511en_US
dc.identifier.scopusauthoridDelagrange, P=7007022477en_US
dc.identifier.scopusauthoridBrown, GM=35493704500en_US

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