Proceedings of the PSK Conference (대한약학회:학술대회논문집)
- 2003.10b
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- Pages.173.2-173.2
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- 2003
N-4-Substituted-benzyl-N'-tert-butylbenzyl Thioureas as Vanilloid Receptor Ligands: Investigation on the Role of Methanesulfonamido group in Antagonistic Activity
- Park, Hyeung-Geun (Seoul National University) ;
- Choi, Je-Yeon (College of Pharmacy, Sookmyung Women's University) ;
- Choi, Sea-Hoon (College of Pharmac, AmorePacific R & D Center) ;
- Park, Mi-Kyung (College of Pharmac, AmorePacific R & D Center) ;
- Lee, Ji-Hye (College of Pharmac, AmorePacific R & D Center) ;
- Suh, Young-Ger (College of Pharmac, AmorePacific R & D Center) ;
- Cho, Ha-Won (College of Pharmac, AmorePacific R & D Center) ;
- Oh, Uh-Taek (College of Pharmac, AmorePacific R & D Center) ;
- Lee, Ji-Youn (College of Pharmac, AmorePacific R & D Center) ;
- Kang, Sang-Uk (College of Pharmac, AmorePacific R & D Center) ;
- Lee, Jee-Woo (College of Pharmac, AmorePacific R & D Center) ;
- Kim, Hee-Doo (College of Pharmac, AmorePacific R & D Center) ;
- Park, Young-Ho (College of Pharmac, AmorePacific R & D Center) ;
- Jeong, Yeon-Su (College of Pharmac, AmorePacific R & D Center) ;
- Choi, Jin-Kyu (College of Pharmac, AmorePacific R & D Center) ;
- Jew, Sang-Sup (College of Pharmac, AmorePacific R & D Center)
- Published : 2003.10.01
Abstract
Vanilloid receptor I (VR1) is a nonselective cation ion channel placed in the plasma membrane of peripheral sensory neurons that is potential target for analgesia A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG. Their structure-activity relationship in reveals that not only the two oxygens and amide hydrogen of sulfonamido group but also the optimal size of methyl in methanesulfonamido group play an integral role for the antagonistic activity on vanilloid receptor.
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