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

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

doi:10.1016/j.bmc.2010.06.082

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

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

Research output: Contribution to journal › Article › peer-review

18 Citations (Scopus)

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.

Original language	English
Pages (from-to)	5938-5944
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	16
DOIs	https://doi.org/10.1016/j.bmc.2010.06.082
Publication status	Published - 2010 Aug 15

Keywords

Diphenylpiperazine
Formalin test
Neuropathic pain
T-type calcium channel blocker

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2010.06.082

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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.",

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AU - Kam, Yoo Lim

AU - Rhee, Hee Kyung

AU - Rhim, Hyewhon

AU - Back, Seung Keun

AU - Na, Heung Sik

AU - Choo, Hea Young Park

PY - 2010/8/15

Y1 - 2010/8/15

N2 - 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.

AB - 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.

KW - Diphenylpiperazine

KW - Formalin test

KW - Neuropathic pain

KW - T-type calcium channel blocker

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IS - 16

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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