{"id":{"repo_id":"buffalo","oai_identifier":"oai:ubir.buffalo.edu:10477/80633"},"canonical_url":"https://search.dev.ndltd.org/etd/buffalo/oai:ubir.buffalo.edu:10477/80633","repository":{"repo_id":"buffalo","name":"Buffalo","base_url":"https://ubir.buffalo.edu/oai/request"},"display":{"title":"The Pharmacological Characterization of Novel Melatonin Receptor Type-Selective Ligands","abstract":"M.S.","abstract_html":"M.S.","abstract_has_math":false,"creators":["Lipinski, Jennie; 0000-0003-2257-8586"],"institution":"State University of New York at Buffalo","degree_name":null,"degree_level":null,"degree_discipline":null,"degree_department":null,"school":null,"contributors":["Dubocovich, Margarita","Pharmacology and Toxicology"],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2019,"date_issued":"2019-10-28T20:52:47Z","date_published":"2019-10-28T20:52:47Z","updated_at":"2026-07-27T19:05:23Z","subjects":["pharmacology","neurosciences"],"languages":["eng"],"rights":["Users of works found in University at Buffalo Institutional Repository (UBIR) are responsible for identifying and contacting the copyright owner for permission to reuse. University at Buffalo Libraries do not manage rights for copyright-protected works and cannot assist with permissions.","Copyright retained by author."],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"http://hdl.handle.net/10477/80633","outbound_label":"Handle","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Dubocovich, Margarita","Pharmacology and Toxicology"]},{"key":"dc:creator","label":"Author","values":["Lipinski, Jennie; 0000-0003-2257-8586"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date","label":"Dc Date","values":["2019-10-28T20:52:47Z","2019","2019-08-06 18:09:45"]},{"key":"dc:publisher","label":"Institution","values":["State University of New York at Buffalo"]},{"key":"dc:type","label":"Dc Type","values":["Text","Thesis"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["pharmacology","neurosciences"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language","label":"Dc Language","values":["eng"]},{"key":"dc:rights","label":"Dc Rights","values":["Users of works found in University at Buffalo Institutional Repository (UBIR) are responsible for identifying and contacting the copyright owner for permission to reuse. University at Buffalo Libraries do not manage rights for copyright-protected works and cannot assist with permissions.","Copyright retained by author."]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["http://hdl.handle.net/10477/80633"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["M.S.","The hormone melatonin is recognized primarily for its role in the regulation of circadian rhythms and sleep-wake cycles, responsible for relaying the signal of darkness. Synthesized and secreted in the pineal gland, melatonin binds to and exerts its effects via two high-affinity GPCRs, MT1 and MT2. The melatonin receptor types exhibit distinct pharmacological profiles, structures and chromosomal localization. The known competitive yet nonselective MT1/MT2 melatonin receptor antagonist, luzindole, has been shown to induce antidepressant-like efficacy in rodent models of behavioral despair through actions at the MT2. Seemingly via the MT1, luzindole has demonstrated effects on the circadian system, significantly delaying the rate of re-entrainment in C3H mouse wheel-running activity following an abrupt advance of dark onset. With minimal discovery of highly specific and selective melatonin receptor ligands, we propose the characterization of newly synthesized, novel melatonin analogues that hold a minimum of 50-fold selectivity for either the MT1 or MT2, with pharmacological profiles comparable to luzindole. Via standard assessment of structure-activity relationships, in vitro competition binding, quantitative receptor autoradiography, and behavioral tests quantifying antidepressant-like efficacy and modulation of circadian rhythms, our goal was to mimic the distinct receptor-mediated behaviors produced by luzindole, with higher efficacy by selectivity."]},{"key":"dc:format","label":"Dc Format","values":["application/pdf"]},{"key":"dc:title","label":"Title","values":["The Pharmacological Characterization of Novel Melatonin Receptor Type-Selective Ligands"]}]}],"canonical_facts":{"dc:contributor":["Dubocovich, Margarita","Pharmacology and Toxicology"],"dc:creator":["Lipinski, Jennie; 0000-0003-2257-8586"],"dc:date":["2019-10-28T20:52:47Z","2019","2019-08-06 18:09:45"],"dc:description":["M.S.","The hormone melatonin is recognized primarily for its role in the regulation of circadian rhythms and sleep-wake cycles, responsible for relaying the signal of darkness. Synthesized and secreted in the pineal gland, melatonin binds to and exerts its effects via two high-affinity GPCRs, MT1 and MT2. The melatonin receptor types exhibit distinct pharmacological profiles, structures and chromosomal localization. The known competitive yet nonselective MT1/MT2 melatonin receptor antagonist, luzindole, has been shown to induce antidepressant-like efficacy in rodent models of behavioral despair through actions at the MT2. Seemingly via the MT1, luzindole has demonstrated effects on the circadian system, significantly delaying the rate of re-entrainment in C3H mouse wheel-running activity following an abrupt advance of dark onset. With minimal discovery of highly specific and selective melatonin receptor ligands, we propose the characterization of newly synthesized, novel melatonin analogues that hold a minimum of 50-fold selectivity for either the MT1 or MT2, with pharmacological profiles comparable to luzindole. Via standard assessment of structure-activity relationships, in vitro competition binding, quantitative receptor autoradiography, and behavioral tests quantifying antidepressant-like efficacy and modulation of circadian rhythms, our goal was to mimic the distinct receptor-mediated behaviors produced by luzindole, with higher efficacy by selectivity."],"dc:format":["application/pdf"],"dc:identifier":["http://hdl.handle.net/10477/80633"],"dc:language":["eng"],"dc:publisher":["State University of New York at Buffalo"],"dc:rights":["Users of works found in University at Buffalo Institutional Repository (UBIR) are responsible for identifying and contacting the copyright owner for permission to reuse. University at Buffalo Libraries do not manage rights for copyright-protected works and cannot assist with permissions.","Copyright retained by author."],"dc:subject":["pharmacology","neurosciences"],"dc:title":["The Pharmacological Characterization of Novel Melatonin Receptor Type-Selective Ligands"],"dc:type":["Text","Thesis"]},"updated_at":"2026-07-27T19:05:23Z"}