Burden D T, Hamilton T C
Eur J Pharmacol. 1976 Jul;38(1):55-61. doi: 10.1016/0014-2999(76)90200-4.
On oral administration, the non-selective beta-adrenoceptor blocking drugs (+/-)-bufuralol, (-)-bufuralol, propanolol, oxprenolol, pindolol and alprenolol produced hypotensive responses in the conscious cat; (+)-bufuralol was without effect. The selective beta-adrenoceptor blocking drugs practolol and atenolol had no effect on blood pressure but tolamolol elicited a hypotensive response. All the drugs tested reduced the tachycardia due to intravenous isoprenaline in the conscious cat; however, not all doses of these drugs reduced blood pressure. (+)-Bufuralol was devoid to beta-adrenoceptive blocking activity. Only tolamolol reduced the pressor response to i.v. phenylephrine in the conscious cat, indicating that alpha-adrenoceptive blocking activity may contribute to its hypotensive action. The results suggest that beta-adrenoceptive blocking activity is necessary for the hypotensive responses of these drugs. However, for the different drugs, there was no correlation between peripheral beta-adrenoceptive blocking activity and hypotensive response.
口服时,非选择性β-肾上腺素受体阻断药(±)-布呋洛尔、(-)-布呋洛尔、普萘洛尔、氧烯洛尔、吲哚洛尔和阿普洛尔可使清醒猫产生降压反应;(+)-布呋洛尔无此作用。选择性β-肾上腺素受体阻断药醋丁洛尔和阿替洛尔对血压无影响,但托拉洛尔可引起降压反应。所有受试药物均可降低清醒猫静脉注射异丙肾上腺素所致的心动过速;然而,并非所有剂量的这些药物均可降低血压。(+)-布呋洛尔无β-肾上腺素受体阻断活性。只有托拉洛尔可降低清醒猫静脉注射去氧肾上腺素的升压反应,表明α-肾上腺素受体阻断活性可能有助于其降压作用。结果提示,β-肾上腺素受体阻断活性是这些药物产生降压反应所必需的。然而,对于不同药物,外周β-肾上腺素受体阻断活性与降压反应之间并无相关性。