title: Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists.
abstract: A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. (R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC(50) value of 0.05 microM which is 10-fold more potent than capsazepine.
authors.affiliation: College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
authors.forename: Chong Hyun
authors.initials: CH
authors.lastname: Ryu
authors.forename: Mi Jung
authors.initials: MJ
authors.lastname: Jang
authors.forename: Jeong Wha
authors.initials: JW
authors.lastname: Jung
authors.forename: Ju-Hyun
authors.initials: JH
authors.lastname: Park
authors.forename: Hye Young
authors.initials: HY
authors.lastname: Choi
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
authors.forename: Uhtaek
authors.initials: U
authors.lastname: Oh
authors.forename: Hyeung-Geun
authors.initials: HG
authors.lastname: Park
authors.forename: Jeewoo
authors.initials: J
authors.lastname: Lee
authors.forename: Hyun-Joo
authors.initials: HJ
authors.lastname: Koh
authors.forename: Joo-Hyun
authors.initials: JH
authors.lastname: Mo
authors.forename: Yung Hyup
authors.initials: YH
authors.lastname: Joo
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Hee-Doo
authors.initials: HD
authors.lastname: Kim
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013890:Thiourea / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D011955:Receptors, Drug; D013890:Thiourea