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 journalArticle

15 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 languageEnglish
Pages (from-to)5938-5944
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number16
DOIs
Publication statusPublished - 2010 Aug 15

Fingerprint

T-Type Calcium Channels
HEK293 Cells
Clamping devices
Neuralgia
Formaldehyde
Analgesics
Rats
Derivatives

Keywords

  • Diphenylpiperazine
  • Formalin test
  • Neuropathic pain
  • T-type calcium channel blocker

ASJC Scopus subject areas

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

Cite this

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.

In: Bioorganic and Medicinal Chemistry, Vol. 18, No. 16, 15.08.2010, p. 5938-5944.

Research output: Contribution to journalArticle

Kam, Yoo Lim ; Rhee, Hee Kyung ; Rhim, Hyewhon ; Back, Seung Keun ; Na, Heung Sik ; Choo, Hea Young Park. / Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity. In: Bioorganic and Medicinal Chemistry. 2010 ; Vol. 18, No. 16. pp. 5938-5944.
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