Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects.
A novel non-vanilloid VR1 antagonist consisting of a new vanilloid equivalent exhibits excellent analgesic effects as well as highly potent antagonistic activities in both capsaicin single channel and calcium uptake assays. In addition, the structural requirement for the vanilloid equivalent of the potent VR1 antagonist has also been elucidated.
Suh
Young-Ger
YG
College of Pharmacy, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, South Korea. ygsuh@snu.ac.kr
Lee
Yong-Sil
YS
Min
Kyung-Hoon
KH
Park
Ok-Hui
OH
Seung
Ho-Sun
HS
Kim
Hee-Doo
HD
Park
Hyoung-Geun
HG
Choi
J- Yeon
J
Lee
Jeewoo
J
Kang
Sang-Wook
SW
Oh
Uh-taek
UT
Koo
Jae-yeon
JY
Joo
Yung-Hyup
YH
Kim
Sun-Young
SY
Kim
Jin Kwan
JK
Park
Young Ho
YH
D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010146:Pain / Q000517:prevention & control; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000700:Analgesics; D011955:Receptors, Drug; D002211:Capsaicin