{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,18]],"date-time":"2025-10-18T10:53:03Z","timestamp":1760784783569,"version":"build-2065373602"},"reference-count":23,"publisher":"Elsevier BV","issue":"5","license":[{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"published-print":{"date-parts":[[2020,3]]},"DOI":"10.1016\/j.bmcl.2019.126929","type":"journal-article","created":{"date-parts":[[2019,12,26]],"date-time":"2019-12-26T12:39:26Z","timestamp":1577363966000},"page":"126929","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":5,"title":["Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays"],"prefix":"10.1016","volume":"30","author":[{"given":"Albert","family":"Ren","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiuwen","family":"Zhu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Konrad","family":"Feichtinger","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Juerg","family":"Lehman","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michelle","family":"Kasem","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Thomas O.","family":"Schrader","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Amy","family":"Wong","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Huong","family":"Dang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Minh","family":"Le","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"John","family":"Frazer","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"David J.","family":"Unett","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andrew J.","family":"Grottick","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kevin T.","family":"Whelan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michael E.","family":"Morgan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Carleton R.","family":"Sage","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9666-1588","authenticated-orcid":false,"given":"Graeme","family":"Semple","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmcl.2019.126929_b0005","doi-asserted-by":"crossref","first-page":"201","DOI":"10.2174\/1389450053174550","article-title":"Serotonin (5-HT) drugs: effects on appetite expression and use for the treatment of obesity","volume":"6","author":"Halford","year":"2005","journal-title":"Curr Drug Targets"},{"key":"10.1016\/j.bmcl.2019.126929_b0010","doi-asserted-by":"crossref","first-page":"282","DOI":"10.1124\/mi.5.5.8","article-title":"Serotonin 5-HT2C receptor agonists: potential for the treatment of obesity","volume":"5","author":"Miller","year":"2005","journal-title":"Mol Int"},{"key":"10.1016\/j.bmcl.2019.126929_b0015","doi-asserted-by":"crossref","first-page":"309","DOI":"10.1007\/s002130050952","article-title":"Reduced satiating effect of d-fenfluramine in serotonin 5-HT(2C) receptor mutant mice","volume":"143","author":"Vickers","year":"1999","journal-title":"Psychopharmacology"},{"key":"10.1016\/j.bmcl.2019.126929_b0020","doi-asserted-by":"crossref","first-page":"581","DOI":"10.1056\/NEJM199708283370901","article-title":"Valvular heart disease associated with fenfluramine\u2013phentermine","volume":"337","author":"Connolly","year":"1997","journal-title":"New Engl J Med"},{"key":"10.1016\/j.bmcl.2019.126929_h0025","doi-asserted-by":"crossref","first-page":"2836","DOI":"10.1161\/01.CIR.102.23.2836","article-title":"Evidence for possible involvement of 5-HT2B receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications","volume":"102","author":"Rothman","year":"2000","journal-title":"Circulation"},{"key":"10.1016\/j.bmcl.2019.126929_h0030","doi-asserted-by":"crossref","first-page":"710","DOI":"10.1124\/mol.109.058057","article-title":"Parallel functional activity profiling reveals valvulopathogens are potent 5-Hydroxytryptamine2B receptor agonists: implications for drug safety assessment","volume":"76","author":"Huang","year":"2009","journal-title":"Mol Pharm"},{"key":"10.1016\/j.bmcl.2019.126929_h0035","doi-asserted-by":"crossref","first-page":"254","DOI":"10.1177\/107385849900500414","article-title":"Activation is hallucinogenic and antagonism is therapeutic: role of 5-HT2A receptors in atypical antipsychotic drug actions","volume":"5","author":"Roth","year":"1999","journal-title":"Neuroscientist"},{"key":"10.1016\/j.bmcl.2019.126929_h0040","doi-asserted-by":"crossref","first-page":"264","DOI":"10.1124\/pr.115.011478","article-title":"Psychedelics","volume":"68","author":"Nichols","year":"2016","journal-title":"Pharmacol Rev"},{"key":"10.1016\/j.bmcl.2019.126929_h0045","doi-asserted-by":"crossref","first-page":"305","DOI":"10.1021\/jm0709034","article-title":"Discovery and structure -activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity","volume":"51","author":"Smith","year":"2008","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmcl.2019.126929_h0050","doi-asserted-by":"crossref","first-page":"577","DOI":"10.1124\/jpet.107.133348","article-title":"Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization","volume":"325","author":"Thomsen","year":"2008","journal-title":"J Pharmacol Exp Ther"},{"key":"10.1016\/j.bmcl.2019.126929_h0055","doi-asserted-by":"crossref","first-page":"245","DOI":"10.1056\/NEJMoa0909809","article-title":"Multicenter, placebo-controlled trial of lorcaserin for weight management","volume":"363","author":"Smith","year":"2010","journal-title":"N Engl J Med"},{"key":"10.1016\/j.bmcl.2019.126929_b0040","doi-asserted-by":"crossref","first-page":"14","DOI":"10.1016\/j.jpsychires.2014.02.012","article-title":"A 6-week randomized, double-blind, placebo-controlled, comparator referenced trial of vabicaserin in acute schizophrenia","volume":"53","author":"Shen","year":"2014","journal-title":"J Psychiatr Res"},{"key":"10.1016\/j.bmcl.2019.126929_b0045","doi-asserted-by":"crossref","first-page":"328","DOI":"10.1177\/1756285615607726","article-title":"Low-dose fenfluramine in the treatment of neurologic disorders: experience in Dravet syndrome","volume":"8","author":"Schoonjans","year":"2015","journal-title":"Ther Adv Neurol Disord"},{"key":"10.1016\/j.bmcl.2019.126929_b0050","first-page":"669","article-title":"Clemizole and modulators of serotonin signalling suppress seizures in Dravet syndrome","volume":"140","author":"Griffin","year":"2017","journal-title":"Brain"},{"key":"10.1016\/j.bmcl.2019.126929_h0075","doi-asserted-by":"crossref","first-page":"142","DOI":"10.1016\/j.ejphar.2012.02.010","article-title":"5-HT2A receptor activation of the external urethral sphincter and 5-HT2C receptor inhibition of micturition: a study based on pharmacokinetics in the anaesthetized female rat","volume":"682","author":"Mbaki","year":"2012","journal-title":"Eur J Pharmacol"},{"key":"10.1016\/j.bmcl.2019.126929_h0080","doi-asserted-by":"crossref","first-page":"2382","DOI":"10.1002\/nau.23586","article-title":"Effect of a 5-HT2c receptor agonist on urethral closure mechanisms in female rats","volume":"37","author":"Ouchi","year":"2018","journal-title":"Neurourol Urodyn"},{"key":"10.1016\/j.bmcl.2019.126929_h0085","doi-asserted-by":"crossref","first-page":"333","DOI":"10.1016\/j.jphs.2019.02.004","article-title":"Effect of ASP2205 fumarate, a novel 5-HT2C receptor agonist, on urethral closure function in rats","volume":"139","author":"Ishigami","year":"2019","journal-title":"J Pharmacol Sci"},{"key":"10.1016\/j.bmcl.2019.126929_b0060","doi-asserted-by":"crossref","first-page":"862","DOI":"10.1124\/jpet.104.075382","article-title":"WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity","volume":"313","author":"Dunlop","year":"2008","journal-title":"J Pharmacol Exp Ther"},{"key":"10.1016\/j.bmcl.2019.126929_b0065","doi-asserted-by":"crossref","first-page":"673","DOI":"10.1124\/jpet.111.179572","article-title":"Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist","volume":"337","author":"Dunlop","year":"2011","journal-title":"J Pharmacol Exp Ther"},{"key":"10.1016\/j.bmcl.2019.126929_b0070","doi-asserted-by":"crossref","first-page":"1521","DOI":"10.1126\/science.1244142","article-title":"Crystal structure of the 5-HT2B receptor solved using serial femtosecond crystallography in lipidic cubic phase","volume":"342","author":"Liu","year":"2013","journal-title":"Science"},{"key":"10.1016\/j.bmcl.2019.126929_b0075","doi-asserted-by":"crossref","first-page":"99","DOI":"10.1016\/j.bbr.2014.07.016","article-title":"Recent advances in the neuropsychopharmacology of serotonergic hallucinogens","volume":"277","author":"Halberstadt","year":"2015","journal-title":"Behav Brain Res"},{"key":"10.1016\/j.bmcl.2019.126929_b0080","doi-asserted-by":"crossref","first-page":"16044","DOI":"10.1021\/ja508394x","article-title":"A functional selectivity mechanism at the serotonin-2A GPCR involves ligand-dependent conformations of intracellular loop 2","volume":"136","author":"Perez-Aguilar","year":"2014","journal-title":"J Am Chem Soc"},{"key":"10.1016\/j.bmcl.2019.126929_b0085","unstructured":"(a) Koolman H, Braeje W, Mack H, et al. PCT Patent Application WO2014041131. (b) Backfisch G, Bakker MHM, Blaich G, et al. PCT Patent Application WO2015136091. (c) Backfisch G, Bakker MHM, Blaich G, et al. PCT Patent Application WO2015136090."}],"container-title":["Bioorganic &amp; Medicinal Chemistry Letters"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X19309126?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X19309126?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,18]],"date-time":"2025-10-18T07:32:01Z","timestamp":1760772721000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0960894X19309126"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,3]]},"references-count":23,"journal-issue":{"issue":"5","published-print":{"date-parts":[[2020,3]]}},"alternative-id":["S0960894X19309126"],"URL":"https:\/\/doi.org\/10.1016\/j.bmcl.2019.126929","relation":{},"ISSN":["0960-894X"],"issn-type":[{"type":"print","value":"0960-894X"}],"subject":[],"published":{"date-parts":[[2020,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry Letters","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmcl.2019.126929","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2019 Published by Elsevier Ltd.","name":"copyright","label":"Copyright"}],"article-number":"126929"}}