Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.
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.
Park
Hyeung-geun
HG
Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr
Park
Mi-kyung
MK
Choi
Ji-yeon
JY
Choi
Sea-hoon
SH
Lee
Jihye
J
Park
Boon-saeng
BS
Kim
Myoung Goo
MG
Suh
Young-ger
YG
Cho
Hawon
H
Oh
Uhtaek
U
Lee
Jeewoo
J
Kim
Hee-Doo
HD
Park
Young-Ho
YH
Koh
Hyun-Ju
HJ
Lim
Kyung Min
KM
Moh
Joo-Hyun
JH
Jew
Sang-sup
SS
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
D002127:Calcium Isotopes; D007473:Ion Channels; D011955:Receptors, Drug; D013890:Thiourea; D002211:Capsaicin; D002118:Calcium