Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity

Kam, Yoo Lim; Rhee, Hee-Kyung; Rhim, Hyewhon; Back, Seung Keun; Na, Heung Sik; Choo, Hea-Young Park

doi:10.1016/j.bmc.2010.06.082

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Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity

Kam, Yoo Lim;
Rhee, Hee-Kyung;
Rhim, Hyewhon;
Back, Seung Keun;
Na, Heung Sik;
외 1명

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18

초록

Novel diphenylpiperazine derivatives were synthesized and evaluated for their inhibitory activity against T-type calcium channel by whole-cell patch clamp recordings on HEK293 cells. Among the test compounds, 2 and 3d were effective in decreasing the response to formalin in both the first and second phases and demonstrated antiallodynic effects in a rat model of neuropathic pain. (C) 2010 Elsevier Ltd. All rights reserved.

키워드

T-type calcium channel blocker; Diphenylpiperazine; Formalin test; Neuropathic pain; CA2+ CHANNELS; PAIN; RAT; MIBEFRADIL; ALLODYNIA; BLOCKERS; MODEL

제목: Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity

저자: Kam, Yoo Lim; Rhee, Hee-Kyung; Rhim, Hyewhon; Back, Seung Keun; Na, Heung Sik; Choo, Hea-Young Park

DOI: 10.1016/j.bmc.2010.06.082

발행일: 2010-08-15

유형: Article

저널명: Bioorganic & Medicinal Chemistry

권: 18

호: 16

페이지: 5938 ~ 5944

언어: ENG

출판사: Pergamon Press Ltd.

발행국가: 영국

분량: 7 페이지

ISSN: E 1464-3391
P 0968-0896