Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor.
Four pyrrolidine derivatives were prepared by the formation of a 5-membered ring based on capsazepine. Among them, the two carbon extended derivatives, 4a (IC(50)=55 microM) and 4b (IC(50)=3 microM), both showed different levels of antagonist activity against the vanilloid receptor in a (45)Ca(2+)-influx assay.
Park
Hyeung geun
Hg
Research Institute of Pharmaceutical Sciences and College of Pharmacy, 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
Suh
Young ger
Yg
Oh
Uhtaek
U
Lee
Jeewoo
J
Kim
Hee Doo
HD
Park
Young Ho
YH
Jeong
Yeon Su
YS
Choi
Jin Kyu
JK
Jew
Sang sup
Ss
D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000737:chemistry; D018360:Crystallography, X-Ray; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D007202:Indicators and Reagents; D011759:Pyrrolidines; D011955:Receptors, Drug; D013890:Thiourea; C071423:capsazepine; D002211:Capsaicin; D002118:Calcium