title: Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor.
abstract: Four pyrrolidine derivatives were prepared by the formation of a 5-membered ring based on capsazepine. Among them, the two carbon extended derivatives, 4a (IC(50)=55 microM) and 4b (IC(50)=3 microM), both showed different levels of antagonist activity against the vanilloid receptor in a (45)Ca(2+)-influx assay.
authors.affiliation: Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr
authors.forename: Hyeung geun
authors.initials: Hg
authors.lastname: Park
authors.forename: Mi kyung
authors.initials: Mk
authors.lastname: Park
authors.forename: Ji yeon
authors.initials: Jy
authors.lastname: Choi
authors.forename: Sea hoon
authors.initials: Sh
authors.lastname: Choi
authors.forename: Jihye
authors.initials: J
authors.lastname: Lee
authors.forename: Young ger
authors.initials: Yg
authors.lastname: Suh
authors.forename: Uhtaek
authors.initials: U
authors.lastname: Oh
authors.forename: Jeewoo
authors.initials: J
authors.lastname: Lee
authors.forename: Hee Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Yeon Su
authors.initials: YS
authors.lastname: Jeong
authors.forename: Jin Kyu
authors.initials: JK
authors.lastname: Choi
authors.forename: Sang sup
authors.initials: Ss
authors.lastname: Jew
mesh_terms: D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000737:chemistry; D018360:Crystallography, X-Ray; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D007202:Indicators and Reagents; D011759:Pyrrolidines; D011955:Receptors, Drug; D013890:Thiourea; C071423:capsazepine; D002211:Capsaicin; D002118:Calcium