Nagatomo T, Hosohata Y, Ohnuki T, Suzuki J
Department of Pharmacology, Niigata College of Pharmacy, Japan.
Nihon Yakurigaku Zasshi. 1997 Jan;109(1):1-12. doi: 10.1254/fpj.109.1.
The non-selective beta-blocker bopindolol, which was developed as a pro-drug, possessed 50-60 times more potent long-acting hypotensive effects on the blood pressure than those of atenolol or propranolol. Because this drug has only a mild partial agonist activity, it did not cause the rapid decrease in heart rate observed with atenolol or propranolol or the increase in heart rate induced by pindolol. These hypotensive effects are due to beta 1-antagonistic effects, not effects on beta 2- or beta 3-adrenoceptors. In addition to these effects, benefits of this drug include the following: slow dissociation rate from beta-adrenoceptors in tissues, high affinity to 5-HT1A subtypes, less clinical effects on lipid metabolism and the inhibition of renin release. It is possible that this drug possesses different pharmacological characteristics from other beta-blockers.
非选择性β受体阻滞剂波吲洛尔是作为前体药物开发的，其长效降压作用比阿替洛尔或普萘洛尔强50至60倍。由于这种药物仅具有轻度的部分激动剂活性，因此它不会引起阿替洛尔或普萘洛尔所观察到的心率快速下降，也不会引起吲哚洛尔诱导的心率增加。这些降压作用是由于β1拮抗作用，而非对β2或β3肾上腺素能受体的作用。除了这些作用外，这种药物的益处还包括：在组织中与β肾上腺素能受体的解离速率缓慢、对5-HT1A亚型具有高亲和力、对脂质代谢的临床影响较小以及抑制肾素释放。这种药物可能具有与其他β受体阻滞剂不同的药理学特性。
