Author/Authors :
Jeewoo Lee، نويسنده , , Sang Uk Kang، نويسنده , , Hyun-Kyung Choi، نويسنده , , Jiyoun Lee، نويسنده , , Ju-Ok Lim، نويسنده , , Min-Jung Kil، نويسنده , , Mi-Kyung Jin، نويسنده , , Kang-Pil Kim، نويسنده , , Jong-Hyuk Sung، نويسنده , , Suk-Jae Chung، نويسنده , , Hee-Jin Ha، نويسنده , , Young-Ho Kim، نويسنده , , Larry V Pearce، نويسنده , , Richard Tran، نويسنده , , Daniel J Lundberg، نويسنده , , Yun Wang، نويسنده , , Attila Toth، نويسنده , , Peter M. Blumberg، نويسنده ,
Abstract :
The structural modifications on the B-region of the potent and high affinity vanilloid receptor (VR1) lead ligand N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea were investigated by the replacement of the thiourea with diverse isosteric functional groups. Structure–activity analysis indicated that the A-region in this series was the primary factor in determining the agonistic/antagonistic activities regardless of the B-region. The NC-hydroxy thiourea analogues (12, 13) showed excellent analgesic activities in the acetic acid writhing assay compared to the parent thiourea analogues.
Keywords :
Vanilloid receptor 1 , Antagonist , e-mail: jeewoo@snu.ac.kr , fax: +82-2-888-0649 , Analgesic.* Corresponding author. Tel.: +82-2-880-7846 , TRPV1
