Synthesis and T-type calcium channel blocking activity of novel diphenylpiperazine compounds, and evaluation of in vivo analgesic activity.
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Kam YL, Rhee HK, Rhim H, Back SK, Na HS, Choo HY
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.
- PubMed ID
- 20659804 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Flunarizine Voltage-dependent T-type calcium channel subunit alpha-1G Kd (nM) 530 N/A N/A Details Flunarizine Voltage-dependent T-type calcium channel subunit alpha-1H Kd (nM) 3600 N/A N/A Details Flunarizine Voltage-dependent T-type calcium channel subunit alpha-1I Kd (nM) 840 N/A N/A Details Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1G IC 50 (nM) 1340 N/A N/A Details Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1G IC 50 (nM) 1000 N/A N/A Details Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1H IC 50 (nM) 1000 N/A N/A Details Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1I IC 50 (nM) 1000 N/A N/A Details