Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists.
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.
Ryu
Chong Hyun
CH
College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Republic of Korea.
Jang
Mi Jung
MJ
Jung
Jeong Wha
JW
Park
Ju-Hyun
JH
Choi
Hye Young
HY
Suh
Young-Ger
YG
Oh
Uhtaek
U
Park
Hyeung-Geun
HG
Lee
Jeewoo
J
Koh
Hyun-Joo
HJ
Mo
Joo-Hyun
JH
Joo
Yung Hyup
YH
Park
Young-Ho
YH
Kim
Hee-Doo
HD
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
D011955:Receptors, Drug; D013890:Thiourea