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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
- 15-8월-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- T-type calcium channel blocker; Diphenylpiperazine; Formalin test; Neuropathic pain
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.16, pp.5938 - 5944
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 18
- Number
- 16
- Start Page
- 5938
- End Page
- 5944
- ISSN
- 0968-0896
- 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.
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