Lee, Byung-Hwan Choi, Min Jung Jo, Mi Na Seo, Hee Jeong Nah, Seung-Yeol Cho, Yong Seo Nam, Ghilsoo Pae, Ae Nim Rhim, Hyewhon Choo, Hyunah 2024-01-20T21:03:47Z 2024-01-20T21:03:47Z 2021-09-03 2009-07-01 0968-0896 https://pubs.kist.re.kr/handle/201004/132323 5-HT3A receptor antagonists have been used mainly for the treatment of nausea and vomiting. These days, the antagonists are of special interest due to their therapeutic potential to treat other diseases such as depression, psychotic disorder, drug abuse, and irritable bowel syndrome. To discover novel 5-HT3A receptor antagonists, we screened our in-house small molecule library, resulting in identifying the quinazolindione derivatives as potent 5-HT3A receptor antagonists. For the purpose of structure-activity relationship study, 24 quinazolindione analogues were biologically evaluated against 5-HT3A receptor. Among those, KKHT10612 shows the best antagonistic effect against 5-HT3A receptor with an IC50 value of 0.8 mu M which is comparable with that of the reference compound, MDL72222, and selectivity over T-type calcium channel as well. (C) 2009 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD 5HT3 RECEPTOR CHANNEL SELECTIVITY EXPRESSION Quinazolindione derivatives as potent 5-HT3A receptor antagonists Article 10.1016/j.bmc.2009.04.029 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.17, no.13, pp.4793 - 4796 BIOORGANIC & MEDICINAL CHEMISTRY 17 13 4793 4796 scie scopus 000266822900057 2-s2.0-66449125846 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article 5HT3 RECEPTOR CHANNEL SELECTIVITY EXPRESSION 5-HT3A Receptor Antagonist Quinazolindione derivatives MDL72222 Calcium channel Serotonin Bemesetron