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

Bioorg Med Chem. 2010 Aug 15;18(16):5938-44. doi: 10.1016/j.bmc.2010.06.082. Epub 2010 Jun 30.

Authors

Yoo Lim Kam¹, 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.

PMID: 20659804
DOI: 10.1016/j.bmc.2010.06.082

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Analgesics / chemical synthesis
Analgesics / chemistry*
Analgesics / pharmacology
Analgesics / therapeutic use*
Animals
Calcium Channels, T-Type / metabolism*
Humans
Neuralgia / drug therapy*
Pain Measurement / drug effects
Piperazines / chemical synthesis
Piperazines / chemistry*
Piperazines / pharmacology
Piperazines / therapeutic use*
Rats

Substances

Analgesics
Calcium Channels, T-Type
Piperazines