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Lomerizine dihydrochloride

CAS No. : 101477-54-7

MCE 站：Lomerizine dihydrochloride

产品活性：Lomerizine dihydrochloride 是一种双重的 L- 和 T 型电压门控钙通道 (calcium channel) 拮抗剂。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Lomerizine is an antagonist of L- ａnd T-type voltagegated calcium channels ａnd transient receptor potential channel 5 transient receptor potential channels. Lomerizine is a dual L/T-type channel blocker used for prophylaxis of migraine. To demonstrate the effectiveness of Lomerizine in limiting intracellular [Ca²⁺], its ability to inhibit glutamate-induced death of motor neurons ａnd the associated rise in cytosolic [Ca²⁺] is evaluated. Lomerizine inhibits the low- ａnd high-voltage activated Ca²⁺ currents in dissociated rat brain neurons at a threshold concentration of 0.01 μM ａnd IC₅₀ of 1.9 μM ａnd H₂O₂-induced Ca²⁺ influx in hippocampal neurons is inhibited by 1 μM Lomerizine. Pre-treatment with 1 μM Lomerizine significantly reduces acute death of motor neurons in spinal cord-DRG cultures exposed to 50 μM glutamate, a concentration that kills approximately 40% of motor neurons in the culture by 6 h, ａnd inhibits the rise in cytosolic [Ca²⁺] that occurs with glutamate treatment. 0.5 μM Lomerizine is sufficient to significantly prevent the mitochondrial fragmentation of mitochondria induced by SOD1G93A. Lomerizine increases the cytotoxicity of Adriamycin (ADM) ａnd the apoptosis induced by ADM or Vincristine (VCR) in K562/ADM cells. At the concentration of 3, 10 ａnd 30μM, Lomerizine reduces the IC₅₀ value of ADM from 79.03 μM to 28.14, 8.16 ａnd 3.16 μM, respectively. Lomerizine increases the intracellular accumulation of ADM ａnd inhibits the efflux of Rh123 in K562/ ADM cells. No change in P-gp expression is observed after the treatment of Lomerizine for 72 h. Lomerizine has strong reversal effect on MDR in K562/ADM cells by inhibiting P-gp function.

In Vivo: To determine whether Ca²⁺ signaling molecules mediate NMDA-induced neurotoxicity in p50-deficient mice, the neuroprotective effects of chemical reagents are examined, which act on the Ca²⁺-signaling pathway including CaN activation, on NMDA-induced RGC death. The p50-deficient mice at 2 months of age, showing normal RGC survival, undergo intraperitoneal pretreatments with a NMDA antagonist, MK801 or Memantine; calcium blocker, Lomerizine; ａnd CaN inhibitor, Tacrolimus, daily for 1 week before the injection of 5 nM NMDA. The chronic administration of Lomerizine or Tacrolimus to KO mice for 6 months results in an increase in surviving RGC numbers (p<0.0001). Lomerizine (KB-2796; 0.3 ａnd 1 mg/kg, i.v.) dose-dependently increases cerebral blood flow significantly at 30 min ａnd 15 min, respectively, after its administration. Lomerizine (1 mg/kg, i.v.) significantly attenuates the expression of c-Fos-like immunoreactivity in the ipsilateral frontoparietal cortex.

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