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| 化学名: | イバブラジン塩酸塩 | | 英語化学名: | Ivabradine hydrochloride | | 别名: | Ivabradine hydrochloride;3-[3-[[(8S)-3,4-Dimethoxy-8-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one hydrochloride;Ivabradine hydrochloride, >=99%;IVABRADINE HYDROCHLORIDE-OTHER COMPOUNDSCONTAINING AN UNFUSED PYRAZOLE RING(WHETHER OR NOT HYDROGENATED)IN THE STRUCTUR;3-[3-[[[(7S)-3,4-Dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one Hydrochloride;Corlentor;S-16257;(7,8-Dimethoxy 3-(3-(((1S)-(4,5-dimethoxybenzocyclobutan-1-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-2H-benzazepin-2-one hydrochloride | | CAS番号: | 148849-67-6 | | 分子式: | C27H37ClN2O5 | | 分子量: | 505.05 | | EINECS: | 638-798-3 | | カテゴリ情報: | Chiral Reagents;Heterocycles;API;Cardiovascular APIs;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors | | Mol File: | 148849-67-6.mol |  |
| 融点 | 193-196?C | | 比旋光度 | 58921 +7.8°; 36521 +27.8° (c = 1% in DMSO) | | 貯蔵温度 | 2-8°C | | 溶解性 | H2O: ≥5mg/mL (warmed) | | 外見 | powder | | 色 | white to beige | | 光学活性 (optical activity) | [α]/D +5 to +9°, c = 1 in DMSO | | Merck | 14,5247 | | InChIKey | HLUKNZUABFFNQS-ZMBIFBSDSA-N | | SMILES | C([C@H]1CC2=CC(OC)=C(OC)C=C12)N(C)CCCN1CCC2=CC(OC)=C(OC)C=C2CC1=O.Cl |&1:1,r| | | CAS データベース | 148849-67-6(CAS DataBase Reference) |
| 主な危険性 | N | | Rフレーズ | 50/53 | | Sフレーズ | 60-61 | | RIDADR | UN 3077 9 / PGIII | | WGK Germany | 3 | | HSコード | 2933.79.1500 |
| | イバブラジン塩酸塩 Usage And Synthesis |
| 外観 | 白色～わずかにうすい褐色、結晶性粉末～粉末 | | 用途 | If チャンネル阻害剤です。心
臓の収縮機能や血圧に影響を及ぼすさず、心
拍数を低下させます。 | | 効能 | 強心薬 | | 説明 | In an effort to develop angina agents without the unwanted negative
inotropic and hypotensive effects associated with b-adrenergic blockers and
calcium channel blockers, a new class of heart-rate reducing compounds that act
specifically on the sinoatrial (SA) node has been explored. These bradycardic
agents interact directly with the pacemaking cell of the SA node and the hyperpolarization-
activated If , the primary pacemaking current. Ivabradine has
evolved as a specific inhibitor of If current through its contact with f-channels on
the intracellular side of the plasma membrane. As a consequence, ivabradine
reduces the speed of diastolic depolarization and decreases heart rate. It has been
approved for the treatment of chronic stable angina and provides a viable
alternative to patients with a contraindication or intolerance of b-blockers. Evaluation
is also underway for the potential treatment of ischemic heart disease.
Using a patch-clamp technique on rabbit sinoatrial node cells, inhibition of If
current ranged from 6% (0.03 mM) – 80% (10 mM).
. | | 化学的特性 | White to Off-White Solid | | Originator | Servier (France) | | 使用 | angina therapeutic | | 使用 | Ivabradine HCl, a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent | | 使用 | Selective bradycardic agent with direct effect on the pacemaker If current of the sinoatrial node. Antianginal | | 使用 | Ivabradine hydrochloride has been used as a potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel (HCN)2 blocker in embryoid body (EB) and rat engineered heart tissue (EHT). | | 定義 | ChEBI: A hydrochloride obtained by combining ivabradine with one molar equivalent of hydrochloric acid. Used to treat patients with angina who have intolerance to beta blockers and/or heart failure. | | brand name | Procoralan | | Biochem/physiol Actions | Ivabradine is used to treat chronic heart failure. | | 臨床応用 | Symptomatic treatment of chronic stable angina pectoris
in patients with sinus rhythm
Treatment of mild to severe chronic heart failure | | 貯蔵 | Store at -20°C |
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