ニソルジピン 化学特性,用途語,生産方法
外観
うすい黄色～黄色, 結晶性粉末～粉末
溶解性
THF, CH2Cl2に可溶。水に殆ど不溶。メタノール:0.1%完溶エタノールにやや溶けやすく、水にほとんど溶けない。
用途
薬理・生理作用研究用。
用途
カルシウム拮抗剤です。L 型
電位依存性カルシウムチャネルのN 部位に結
合し、細胞内へのカルシウムイオン流入を抑
制する作用を示します。
用途
ニソルジピン（国際一般名、英: Nisoldipine）は、ジヒドロピリジン系カルシウムチャネル拮抗薬の一つ。
血管平滑筋細胞のカルシウムチャネルに作用し、細胞内へのカルシウムの流入を阻害する。高血圧症、狭心症に対し有効である。
効能
血圧降下薬, 血管拡張薬, カルシウムチャネル遮断薬
商品名
バイミカード (バイエル薬品)
説明
Nisoldipine D4 is another long-acting dihydropyridine calcium channel blocker effective in the treatment of hypertension and angina pectoris. It is reported to have little or no cardiodepressive activity and to be more effective than nifedipine in reducing blood pressure in hypertensives. Nisoldipine has also been shown to be effective in the management of congestive heart failure. Reduction in dosage is necessary in patients with hepatic, but not renal impairment.
化学的特性
Nisoldipine D4 is Light Tan Crystals
使用
Labeled Nisoldipine, intended for use as an internal standard for the quantification of Nisoldipine by GC- or LC-mass spectrometry.
定義
ChEBI: A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate,
calcium channel blocker, is used in the treatment of hypertension and angina pectoris.
一般的な説明
In vitro studies show that the effects ofnisoldipine, 1,4-dihydro-2, 6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinecarboxylic acid methyl 2-methylpropyl ester(Sular), on contractile processes are selective, with greaterpotency on vascular smooth muscle than on cardiac muscle.
Nisoldipine is highly metabolized, with five majormetabolites identified. As with most of the dihydropyridines,the cytochrome P450 (CYP) 3A4 isozyme is mainlyresponsible for the metabolism of nisoldipine. The majorbiotransformation pathway appears to involve the hydroxylationof the isobutyl ester side chain. This particular metabolitehas approximately 10% of the activity of the parentcompound.
ニソルジピン 上流と下流の製品情報
原材料
準備製品