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(R)-Nicardipine

(Synonyms: (R)-YC-93 free base) 目录号 : GC68475

(R)-Nicardipine ((R)-YC-93 free base) 是 Nicardipine 的低活性的 R 型对映异构体。Nicardipine 是一种钙通道 (Calcium Channel) 阻滞剂,可阻断心脏钙通道,IC50 为 1 μM。 Nicardipine 可用于慢性心绞痛以及控制血压的研究。

(R)-Nicardipine Chemical Structure

Cas No.:76093-35-1

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5mg
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10mg
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25mg
¥4,680.00
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50mg
¥7,200.00
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100mg
¥10,800.00
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产品描述

(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a Calcium Channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure[1].

[1]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31.

Chemical Properties

Cas No. 76093-35-1 SDF Download SDF
别名 (R)-YC-93 free base
分子式 C26H29N3O6 分子量 479.52
溶解度 DMSO : 200 mg/mL (417.08 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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1 mM 2.0854 mL 10.4271 mL 20.8542 mL
5 mM 0.4171 mL 2.0854 mL 4.1708 mL
10 mM 0.2085 mL 1.0427 mL 2.0854 mL
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Research Update

The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery

Arch Pharm Res 2005 Mar;28(3):319-24.PMID:15832820DOI:10.1007/BF02977799.

The present study was designed to study the difference effects between nicardipine and its two enantiomers on thoracic artery of rabbit. A high-performance liquid chromatographic method was used to prepare the two enantiomers of nicardipine. The thoracic artery of rabbit was removed. The vessels were cut into 3 mm in width and 15 mm in length spiral strips and immersed into tissue baths. The concentration-response curves of nicardipine and its enantiomers were obtained by cumulative administration of the vasoconstrictors. Nicardipine and the enantiomers could shift the dose-response curves of NE, KCl or CaCl2 to right in a nonparallel manner and decrease the maximum effective in a concentration-depended manner, respectively. The pD2' value of R-(-)-Nicardipine showed significantly effective than that of nicardipine and S-(+)-Nicardipine (P<0.01). There was not obviouse difference between the pD2' value of nicardipine and S-(+)-Nicardipine (P>0.05). The results demonstrate that the stereoselective interaction between R-(-)-Nicardipine and L-calcium channel receptor is more stronger than that of S-(+)-Nicardipine.

[Protection of HOE642 against cardiomyocyte injury caused by anoxia and reoxygenation]

Sichuan Da Xue Xue Bao Yi Xue Ban 2005 Sep;36(5):672-5.PMID:16235534doi

Objective: To investigate the protective effect of calcium antagonists (A/R) injury of cardiomyocytes. Methods: Primary-cultured cardiomyocytes were divided A/R, A/R+nicardipine(Nic), A/R+HOE642, A/R+H7, A/R+PD98059 and control parameters were measured in all groups, intracellular calcium concentration ([Ca2+]i), content, lactate dehydrogenase (LDH) and creative phosphokinase(CK) activity in the activity. The calpain (u-calpain and m-calpain) protein expression levels were measured In comparison with A/R group, A/R + nicardipine (Nic) and A/R + Nic groups showed [Ca2+]i, m-calpain protein expression, LDH and CK content in the medium, a higher activity of PKC and MAPK (P < 0.01). On the contrary, A/R+H7 and A/R+PD98059 LDH and CK content in the medium, and lower ATP content and cell viability as compared 0. 05). Conclusion: The A/R mediated Ca2+ overload resulting from cardiomyocyte injury blocking Ca2+ entry and H+/Na+ exchange, and very likely PKC and MAPK are involved protection against the A/R injury of cardiomyocytes.