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

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

Issue Date: 2010-08-15

Publisher: PERGAMON-ELSEVIER SCIENCE LTD

Citation: BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.16, pp.5938 - 5944

Abstract: 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.

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

ISSN: 0968-0896

URI: https://pubs.kist.re.kr/handle/201004/131173

DOI: 10.1016/j.bmc.2010.06.082

Appears in Collections:: KIST Article > 2010

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