title: Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.
abstract: Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4'-hydroxy-3'-methoxy-phenyl)-propyl]-1,3-diphenethyl-thiourea (8l, IC(50)=0.32 microM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC(50)=0.65 microM) against the vanilloid receptor in a (45)Ca(2+)-influx assay.
authors.affiliation: Research Institute of Pharmaceutical Sciences, 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: Boon-saeng
authors.initials: BS
authors.lastname: Park
authors.forename: Myoung Goo
authors.initials: MG
authors.lastname: Kim
authors.forename: Young-ger
authors.initials: YG
authors.lastname: Suh
authors.forename: Hawon
authors.initials: H
authors.lastname: Cho
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: Hyun-Ju
authors.initials: HJ
authors.lastname: Koh
authors.forename: Kyung Min
authors.initials: KM
authors.lastname: Lim
authors.forename: Joo-Hyun
authors.initials: JH
authors.lastname: Moh
authors.forename: Sang-sup
authors.initials: SS
authors.lastname: Jew
mesh_terms: D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism; D002127:Calcium Isotopes; D002211:Capsaicin / Q000031:analogs & derivatives; D020128:Inhibitory Concentration 50; D007473:Ion Channels / Q000037:antagonists & inhibitors; D009474:Neurons / Q000166:cytology / Q000187:drug effects / Q000502:physiology; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002127:Calcium Isotopes; D007473:Ion Channels; D011955:Receptors, Drug; D013890:Thiourea; D002211:Capsaicin; D002118:Calcium