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Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds,and evaluation of in vivo analgesic activity
Authors:Yoo Lim Kam  Hee-Kyung Rhee  Hyewhon Rhim  Seung Keun Back  Heung Sik Na  Hea-Young Park Choo
Affiliation:1. School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea;2. Department of Biological Science, Sookmyung Women’s University, Seoul 140-742, Republic of Korea;3. Life Sciences Division, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea;4. Department of Physiology, Korea University College of Medicine, Seoul 136-705, Republic of Korea
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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