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编 号：F756553
分子式：C32H37F2N3O
分子量：517.65
分子式：C32H37F2N3O
分子量：517.65
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CAS No: 2878598-92-4
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生物活性：
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.
体内研究：
Cav 3.2 inhibitor 2 (1-10 mg/kg; i.p. 30 min before i.pl. Na2S) affects the Na2S-induced pain in vivo.Cav 3.2 inhibitor 2 (10 mg/kg; i.p. 7 days after oxaliplatin treatment) affects oxaliplatin-induced allodynia in vivo.Animal Model:Mice with Na2S intraplantar (i.pl.) administration
Dosage:1, 3 and 10 mg/kg
Administration:Intraperitoneal injection; 1-10 mg/kg 30 min before i.pl. Na2S
Result:Almost completely blocked the Na2S-induced colonic pain and referred hyperalgesia.
Animal Model:Wild-type (WT) or Cav3.2-kockout (KO) C57BL/6 mice with oxaliplatin (OHP) injection
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg on day 7 after oxaliplatin treatment
Result:Attenuated the oxaliplatin-induced allodynia in WT C57BL/6 mice, while showed no effect on KO mice.
体外研究：
Cav 3.2 inhibitor 2 (0.3 μM) shows a produced inhibition of Cav3.2 comparable to that of pimozide.Cav 3.2 inhibitor 2 (1 and 10 μM; 90 min) shows a binding affinity to D2 receptor significantly less than pimozide.Cav 3.2 inhibitor 2 (0.01-10 μM) inhibits T channels isoforms with IC50s of 0.09339, 1.109 and 0.2167 μM for -80mV Cav3.2, -110mV Cav3.2 and Cav3.1, respectively.
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.
体内研究：
Cav 3.2 inhibitor 2 (1-10 mg/kg; i.p. 30 min before i.pl. Na2S) affects the Na2S-induced pain in vivo.Cav 3.2 inhibitor 2 (10 mg/kg; i.p. 7 days after oxaliplatin treatment) affects oxaliplatin-induced allodynia in vivo.Animal Model:Mice with Na2S intraplantar (i.pl.) administration
Dosage:1, 3 and 10 mg/kg
Administration:Intraperitoneal injection; 1-10 mg/kg 30 min before i.pl. Na2S
Result:Almost completely blocked the Na2S-induced colonic pain and referred hyperalgesia.
Animal Model:Wild-type (WT) or Cav3.2-kockout (KO) C57BL/6 mice with oxaliplatin (OHP) injection
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg on day 7 after oxaliplatin treatment
Result:Attenuated the oxaliplatin-induced allodynia in WT C57BL/6 mice, while showed no effect on KO mice.
体外研究：
Cav 3.2 inhibitor 2 (0.3 μM) shows a produced inhibition of Cav3.2 comparable to that of pimozide.Cav 3.2 inhibitor 2 (1 and 10 μM; 90 min) shows a binding affinity to D2 receptor significantly less than pimozide.Cav 3.2 inhibitor 2 (0.01-10 μM) inhibits T channels isoforms with IC50s of 0.09339, 1.109 and 0.2167 μM for -80mV Cav3.2, -110mV Cav3.2 and Cav3.1, respectively.
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