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초록
A series of novel non-peptide diamide compounds was synthesized and evaluated as antibradykinin agents by utilizing guinea-pig ileum smooth muscle. Among the final compounds, (Z)-4-(4-(bis(4-fluorophenyl) methyl)piperazin-1-yl)-4-oxo-N-(4-phenylbutan-2-yl)but-2-enamide showed most favorable bradykinin inhibitory activity and demonstrated analgesic efficacies in the rat models of inflammatory and neuropathic pain. (C) 2010 Published by Elsevier Ltd.
키워드
Antibradykinin agents; Formalin test; Allodynia; GUINEA-PIG ILEUM; FORMALIN TEST; NEUROPATHIC PAIN; KININ RECEPTORS; NERVE INJURY; MECHANICAL ALLODYNIA; INFLAMMATORY PAIN; OPIOID MODULATION; TACTILE ALLODYNIA; B1 RECEPTORS
- 제목
- Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity
- 저자
- Kam, Yoo Lim; Rhee, Hee-Kyung; Kim, Hwa-Jung; Back, Seung Keun; Na, Heung Sik; Choo, Hea-Young Park
- 발행일
- 2010-03-15
- 유형
- Article
- 권
- 18
- 호
- 6
- 페이지
- 2327 ~ 2336