产品
编 号：F119615
分子式：C27H28N2O7
分子量：492.52
分子式：C27H28N2O7
分子量：492.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
175
In-stock
10mg
280
In-stock
50mg
640
In-stock
100mg
1040
In-stock
结构图
CAS No: 132203-70-4
产品详情
生物活性：
Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
体内研究：
Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca2+-channel in rat dorsal root ganglion neurons. Administration of Cilnidipine (10 mg/kg) and Nimodipine (10 mg/kg) significantly attenuates the immobilized stress-induced behavioral changes and restored memory deficits along with normalization of the corticosterone levels.Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice.Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs.Animal Model:Swiss albino mice weighing 25±5 g
Dosage:5 and 10 mg/kg
Administration:administered i.p. 30 min prior to immobilization stress
Result:Cilnidipine (10 mg/kg, i.p.) and nimodipine (10 mg/kg, i.p.) 30 min prior to subjecting immobilization stress resulted in significant attenuation of immobilization stress-induced decrease in locomotor activity. Administration with Cilnidipine (5 mg/kg, i.p.) and Nimodipine (5 mg/kg, i.p.) did not show any significant effect on the stressed mice. Administration of Cilnidipine (10 mg/kg, i.p.) and Nimodipine (10 mg/kg, i.p.) in the non-stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.
体外研究：
Cilnidipine inhibits the L-type current with an IC50 of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx.The IC50 for Cilnidipine in respect of the N-type current is 200 nM. Cilnidipine dose- and time-dependently inhibits Ba2+ currents in A7r5 cells with the IC50 at 10 nM after 10 min. Cilnidipine dose-dependently inhibits depolarization- and Ca2+-induced contractions of rat aortic rings, with an IC50 of 10 nM at 10 min. The viability of nPC12 cells show no significant change up to 150?μM Cilnidipine, but it decreases slightly in the cells treated with greater than 200?μM Cilnidipine. Cilnidipine (100 μM, 2 hours) treatment increases the expression of p85aPI3K p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), and decreases levels of cytosolic cytochrome c, activated caspase 3, and cleaved PARP.
Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
体内研究：
Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca2+-channel in rat dorsal root ganglion neurons. Administration of Cilnidipine (10 mg/kg) and Nimodipine (10 mg/kg) significantly attenuates the immobilized stress-induced behavioral changes and restored memory deficits along with normalization of the corticosterone levels.Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice.Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs.Animal Model:Swiss albino mice weighing 25±5 g
Dosage:5 and 10 mg/kg
Administration:administered i.p. 30 min prior to immobilization stress
Result:Cilnidipine (10 mg/kg, i.p.) and nimodipine (10 mg/kg, i.p.) 30 min prior to subjecting immobilization stress resulted in significant attenuation of immobilization stress-induced decrease in locomotor activity. Administration with Cilnidipine (5 mg/kg, i.p.) and Nimodipine (5 mg/kg, i.p.) did not show any significant effect on the stressed mice. Administration of Cilnidipine (10 mg/kg, i.p.) and Nimodipine (10 mg/kg, i.p.) in the non-stressed mice, and vehicle in the stressed mice did not modulate locomotor activity in a significant manner.
体外研究：
Cilnidipine inhibits the L-type current with an IC50 of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx.The IC50 for Cilnidipine in respect of the N-type current is 200 nM. Cilnidipine dose- and time-dependently inhibits Ba2+ currents in A7r5 cells with the IC50 at 10 nM after 10 min. Cilnidipine dose-dependently inhibits depolarization- and Ca2+-induced contractions of rat aortic rings, with an IC50 of 10 nM at 10 min. The viability of nPC12 cells show no significant change up to 150?μM Cilnidipine, but it decreases slightly in the cells treated with greater than 200?μM Cilnidipine. Cilnidipine (100 μM, 2 hours) treatment increases the expression of p85aPI3K p-Akt, p-GSK-3β, and heat shock transcription factor (HSTF-1), and decreases levels of cytosolic cytochrome c, activated caspase 3, and cleaved PARP.
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