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.",

keywords = "Diphenylpiperazine, Formalin test, Neuropathic pain, T-type calcium channel blocker",

author = "Kam, \{Yoo Lim\} and Rhee, \{Hee Kyung\} and Hyewhon Rhim and Back, \{Seung Keun\} and Na, \{Heung Sik\} and Choo, \{Hea Young Park\}",

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T1 - Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity

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

UR - https://www.scopus.com/pages/publications/77955471833

U2 - 10.1016/j.bmc.2010.06.082

DO - 10.1016/j.bmc.2010.06.082

M3 - Article

C2 - 20659804

AN - SCOPUS:77955471833

SN - 0968-0896

VL - 18

SP - 5938

EP - 5944

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

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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