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Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists
- Li, Fu-Nan;
- Kim, Nam-Jung;
- Paek, Seung-Mann;
- Kwon, Do-Yeon;
- Min, Kyung Hoon;
- 외 6명
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13Citations
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14초록
We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent Ca-45(2+) uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC50 of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described. (C) 2009 Elsevier Ltd. All rights reserved.
키워드
Diarylalkyl amides; TRPV1 antagonists; VANILLOID RECEPTOR-1; NEUROPATHIC PAIN; CAPSAICIN CREAM; POTENT; EXPRESSION; CONVERSION; DISCOVERY; THIOUREAS; NEURONS; CHANNEL
- 제목
- Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists
- 저자
- Li, Fu-Nan; Kim, Nam-Jung; Paek, Seung-Mann; Kwon, Do-Yeon; Min, Kyung Hoon; Jeong, Yeon-Su; Kim, Sun-Young; Park, Young-Ho; Kim, Hee-Doo; Park, Hyeung-Geun; Suh, Young-Ger
- 발행일
- 2009-05
- 유형
- Article
- 권
- 17
- 호
- 10
- 페이지
- 3557 ~ 3567
- 언어
- ENG
- 출판사
- PERGAMON-ELSEVIER SCIENCE LTD
- 발행국가
- 영국
- 분량
- 11 페이지
- ISSN
- E 1464-3391
P 0968-0896