title: Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
abstract: Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC(50)=31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl)benzamide (3g, IC(50)=31 nM), showed 5-fold higher antagonistic activity than 1 in (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: Ji-Yeon
authors.initials: JY
authors.lastname: Choi
authors.forename: Mi-Hyun
authors.initials: MH
authors.lastname: Kim
authors.forename: Sea-Hoon
authors.initials: SH
authors.lastname: Choi
authors.forename: Mi-Kyung
authors.initials: MK
authors.lastname: Park
authors.forename: Jihye
authors.initials: J
authors.lastname: Lee
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: Hee-Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Yung Hyup
authors.initials: YH
authors.lastname: Joo
authors.forename: Song Seok
authors.initials: SS
authors.lastname: Shin
authors.forename: Jin Kwan
authors.initials: JK
authors.lastname: Kim
authors.forename: Yeon Su
authors.initials: YS
authors.lastname: Jeong
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Koh
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Sang-Sup
authors.initials: SS
authors.lastname: Jew
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D020013:Calcium Signaling / Q000187:drug effects; D005727:Ganglia, Spinal / Q000166:cytology; D020128:Inhibitory Concentration 50; D007473:Ion Channels / Q000819:agonists / Q000037:antagonists & inhibitors*; D008024:Ligands; D009474:Neurons; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels
chemical_list: D001549:Benzamides; D007473:Ion Channels; D008024:Ligands; D011955:Receptors, Drug; D050916:TRPV Cation Channels; C493922:Trpv1 protein, rat