Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.
A series of acyclic phenethylthiocarbamate derivatives have been synthesized, and their antagonist effect against vanilloid receptor tested. Chain branching led to a significant change in antagonist activity of the parent molecule. Ethyl-branched 1e showed a 6.3 microM of IC(50) value in 45Ca(2+)-influx assay.
Yoon
JungWha
J
College of Pharmacy, Sookmyung Women's University, 53-12 Chungpa-dong, Yongsan-ku, Seoul 140-742, South Korea.
Choi
HyeYoung
H
Lee
Hyun Joo
HJ
Ryu
Chong Hyun
CH
Park
Hyeung-geun
HG
Suh
Young-ger
YG
Oh
Uhtaek
U
Jeong
Yeon Su
YS
Choi
Jin Kyu
JK
Park
Young-Ho
YH
Kim
Hee-Doo
HD
D000818:Animals; D002118:Calcium / Q000378:metabolism; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D009475:Neurons, Afferent / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011955:Receptors, Drug / Q000819:agonists / Q000037:antagonists & inhibitors*; D013116:Spinal Cord / Q000166:cytology; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D011955:Receptors, Drug; D013859:Thiocarbamates; C071423:capsazepine; D002211:Capsaicin; D002118:Calcium