Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity.
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.
Kam
Yoo Lim
YL
School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
Rhee
Hee-Kyung
HK
Rhim
Hyewhon
H
Back
Seung Keun
SK
Na
Heung Sik
HS
Choo
Hea-Young Park
HY
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D020747:Calcium Channels, T-Type / Q000378:metabolism*; D006801:Humans; D009437:Neuralgia / Q000188:drug therapy*; D010147:Pain Measurement / Q000187:drug effects; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats
D000700:Analgesics; D020747:Calcium Channels, T-Type; D010879:Piperazines