盐酸普奈洛尔
盐酸普奈洛尔 性质
| 熔点 | 196-198 °C(lit.) |
|---|---|
| 储存条件 | Store below +30°C. |
| 溶解度 | 乙醇：10 mg/mL |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 水溶解性 | Soluble to 100 mM in water |
| BRN | 5780490 |
| CAS 数据库 | 13071-11-9(CAS DataBase Reference) |
盐酸普奈洛尔 用途与合成方法
盐酸普奈洛尔为非选择性β-受体阻断药，阻断心肌的β受体，对β1和β2受体均有拮抗作用。减慢心率，,抑制心脏收缩力与传导、循环血量减少、心肌耗氧量降低。
盐酸普奈洛尔临床主要用于治疗多种原因所致的心律失常，也可用于心绞痛高血压嗜铬细胞瘤(手术前准备)等。由于拮抗β2受体可引起支气管痉挛和哮喘，故本品禁用于支气管哮喘的病人。
(R)-Propranolol hydrochloride 是抗肾上腺素受体 (β-adrenoceptor) 拮抗剂普萘洛尔 (HY-B0573) 的活性较低的对映体。Propranolol 是一种非选择性的 β-adrenergic receptor (βAR) 拮抗剂，对 β1AR 和 β2AR 具有高亲和力，Ki 值分别为 1.8 nM 和 0.8 nM。Both isomers of propranolol are capable of preventing adrenaline-induced cardiac arrhythmias in cats anaesthetized with halothane, but the mean dose of (-)-propranolol is 0.09 mg/kg whereas that of (+)-propranolol is 4.2 mg/kg.Both isomers of propranolol are capable of reversing ventricular tachycardia caused by ouabain in anaesthetized cats and dogs. The dose of (-)-propranolol is significantly smaller than that of (+)-propranolol ((R)-Propranolol) in both species.(R)-Propranolol hydrochloride (10 mg/kg) has no antagonistic activity in rats, the cardiac responses to isoprenaline of rat can be blocked by probably much less than 1/100th of that of the (-) isomer in this preparation.
