シルニジピン  (Synonyms: Cilnidipine; FRC-8653)

Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel^[1][2][3][4]. Antihypertensive effects^[5].

Cilnidipine inhibits the L-type current with an IC₅₀ of 100 nM in neurons pretreated with omegaCgTx plus omegaAgTx^[1].
The IC₅₀ for Cilnidipine in respect of the N-type current is 200 nM^[1].
Cilnidipine dose- and time-dependently inhibits Ba²⁺ currents in A7r5 cells with the IC₅₀ at 10 nM after 10 min^[2].
Cilnidipine dose-dependently inhibits depolarization- and Ca²⁺-induced contractions of rat aortic rings, with an IC₅₀ of 10 nM at 10 min^[2].
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^[3].
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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cilnidipine has potent inhibitory actions on N-type as well as L-type voltage-dependent Ca²⁺-channel in rat dorsal root ganglion neurons^[1].
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^[4].
Cilnidipine and Nimodipine produce comparable beneficial effects in restoring immobilization stress subjected mice^[4].
Oral administration of Cilnidipine (3 mg/kg) markedly lowers both systolic and diastolic blood pressure 1 hr after administration in 2K1C renal hypertensive dogs^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

492.52

C₂₇H₂₈N₂O₇

132203-70-4

Solid

Off-white to light yellow

O=C(C1=C(C)NC(C)=C(C(OC/C=C/C2=CC=CC=C2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OCCOC

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. S Fujii,et al. Effect of cilnidipine, a novel dihydropyridine Ca²⁺-channel antagonist, on N-type Ca²⁺ channel in rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 1997 Mar;280(3):1184-91.  [Content Brief]

  [2]. Matthias Löhn, et al. Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C. J Hypertens. 2002 May;20(5):885-93.  [Content Brief]

  [3]. Young Joo Lee, et al. Cilnidipine mediates a neuroprotective effect by scavenging free radicals and activating the phosphatidylinositol 3-kinase pathway. J Neurochem. 2009 Oct;111(1):90-100.  [Content Brief]

  [4]. Naresh Kumar, et al. Anti-stress effects of cilnidipine and nimodipine in immobilization subjected mice. Physiol Behav. 2012 Mar 20;105(5):1148-55.  [Content Brief]

  [5]. A Takahara, et al. [Antihypertensive effects of repeated oral administration of cilnidipine, a novel calcium antagonist, in 2K1C renal hypertensive dogs]. Nihon Yakurigaku Zasshi. 1995 Oct;106(4):279-87.  [Content Brief]