title: Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents.
abstract: Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca(2+) uptake inhibition in rat DRG neuron with IC(50) between 10 and 100 nM.
authors.affiliation: College of Pharmacy, and Sensory Research Center, CRI, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, Korea. ygsuh@snu.ac.kr
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
authors.forename: Yong-Sil
authors.initials: YS
authors.lastname: Lee
authors.forename: Kyung-Hoon
authors.initials: KH
authors.lastname: Min
authors.forename: Ok-Hui
authors.initials: OH
authors.lastname: Park
authors.forename: Jin-Kwan
authors.initials: JK
authors.lastname: Kim
authors.forename: Ho-Sun
authors.initials: HS
authors.lastname: Seung
authors.forename: Seung-Yong
authors.initials: SY
authors.lastname: Seo
authors.forename: Bo-Young
authors.initials: BY
authors.lastname: Lee
authors.forename: Yeon-Hee
authors.initials: YH
authors.lastname: Nam
authors.forename: Kwang-Ok
authors.initials: KO
authors.lastname: Lee
authors.forename: Hee-Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Hyeung-Geun
authors.initials: HG
authors.lastname: Park
authors.forename: Jeewoo
authors.initials: J
authors.lastname: Lee
authors.forename: Uhtaek
authors.initials: U
authors.lastname: Oh
authors.forename: Ju-Ok
authors.initials: JO
authors.lastname: Lim
authors.forename: Sang-Uk
authors.initials: SU
authors.lastname: Kang
authors.forename: Min-Jung
authors.initials: MJ
authors.lastname: Kil
authors.forename: Jae-Yeon
authors.initials: JY
authors.lastname: Koo
authors.forename: Song Seok
authors.initials: SS
authors.lastname: Shin
authors.forename: Yung-Hyup
authors.initials: YH
authors.lastname: Joo
authors.forename: Jin Kwan
authors.initials: JK
authors.lastname: Kim
authors.forename: Yeon-Su
authors.initials: YS
authors.lastname: Jeong
authors.forename: Sun-Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
mesh_terms: D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism; D005727:Ganglia, Spinal / Q000166:cytology; D066298:In Vitro Techniques; D007473:Ion Channels / Q000037:antagonists & inhibitors*; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D007473:Ion Channels; D050916:TRPV Cation Channels; C493922:Trpv1 protein, rat; D013890:Thiourea; D002118:Calcium