Smits J F, Zeegers H H, Struyker-Boudier H A
Department of Pharmacology, University of Limburg, Maastricht, The Netherlands.
Arch Int Pharmacodyn Ther. 1989 Mar-Apr;298:164-71.
To investigate the stereospecificity of beta-adrenoceptor blockade and renal vasodilatation by tertatolol, the regional hemodynamic effects of the 2 stereo-isomers of tertatolol (d-tertatolol and l-tertatolol) were compared in conscious spontaneously hypertensive rats. Furthermore, the effects of a combination of d-tertatolol and dl-propranolol were studied. l-Tertatolol and the combination of beta-blockers lowered heart rate and caused an early increase and a late decrease of blood pressure. l-Tertatolol, but not the combination of dl-propranolol and d-tertatolol, decreased renal resistance at 3-4 hr after injection. Injections of d-tertatolol alone did not cause any effect. Since effects of l-tertatolol are fully comparable to effects previously observed with dl-tertatolol, and d-tertatolol was devoid of any effects, both alone and in combination with dl-propranolol, we conclude that both beta-adrenoceptor blockade and renal vasodilatation are stereospecific for the l-isomer of tertatolol.
为研究替他洛尔对β-肾上腺素能受体的阻断作用及肾血管舒张的立体特异性,在清醒的自发性高血压大鼠中比较了替他洛尔的两种立体异构体(d-替他洛尔和l-替他洛尔)的局部血流动力学效应。此外,还研究了d-替他洛尔与dl-普萘洛尔联合用药的效果。l-替他洛尔及β受体阻滞剂联合用药可降低心率,并使血压先升高后降低。l-替他洛尔可降低注射后3 - 4小时的肾血管阻力,而dl-普萘洛尔与d-替他洛尔联合用药则无此作用。单独注射d-替他洛尔未产生任何效应。由于l-替他洛尔的效应与先前观察到的dl-替他洛尔的效应完全相当,且d-替他洛尔单独使用或与dl-普萘洛尔联合使用均无任何效应,我们得出结论,β-肾上腺素能受体阻断和肾血管舒张对替他洛尔的l-异构体均具有立体特异性。