Delaini F, Perico N, Tagliaferri M, Lupini C, Patino O, Remuzzi G, Garattini S
Mario Negri Institute for Pharmacological Research, Bergamo, Italy.
J Pharmacol Exp Ther. 1988 Jul;246(1):287-93.
Tertatolol is a new beta-blocking agent which induces renal vasodilation in experimental animals and humans and increases glomerular filtration rate (GFR), diuresis and natriuresis. The mechanisms underlying renal effects of tertatolol are not known. Our aims were to establish whether tertatolol influences renal function by a systemic or by an intrarenal effect and to assess whether tertatolol could maintain GFR in chronic renal failure. Tertatolol but not propranolol when given as i.v. bolus injection at the dose of 25 and 50 micrograms/kg. b.w. induces a significant increase in GFR and perfusate flow rate (PFR) in an isolated perfused kidney model [GFR: tertatolol, 25 micrograms/kg; preinjection: 0.477 +/- 0.077 ml/min/g of kidney; 30 min postinjection: 0.996 +/- 0.114 ml/min/g of kidney. Tertatolol (50 micrograms/kg) preinjection: 0.517 +/- 0.040 ml/min/g of kidney; 30 min postinjection: 0.879 +/- 0.035 ml/min/g of kidney. Propranolol (500 micrograms/kg) preinjection: 0.574 +/- 0.045 ml/min/g of kidney; 30 min postinjection: 0.538 +/- 0.029 ml/min/g of kidney. PFR: tertatolol, 25 micrograms/kg, preinjection: 30.00 +/- 0.79 ml/min; 30 min postinjection: 36.20 +/- 2.58 ml/min. Tertatolol (50 micrograms/kg) preinjection: 29.30 +/- 1.44 ml/min; 30 min postinjection: 38.01 +/- 1.87 ml/min. Propranolol (500 micrograms/kg) preinjection: 28.70 +/- 1.04 ml/min; 30 min postinjection: 28.30 +/- 0.91 ml/min]. In the same preparation tertatolol significantly increases urine flow rate and Na+ excretion [urine flow rate: tertatolol (25 micrograms/kg) preinjection: 28.28 +/- 4.10 microliter/min; 60 min postinjection: 38.23 +/- 6.74 microliter/min. Tertatolol (50 micrograms/kg) preinjection: 24.02 +/- 0.63 microliter/min; 60 min postinjection: 33.18 +/- 2.07 microliter/min.(ABSTRACT TRUNCATED AT 250 WORDS)
替他洛尔是一种新型β受体阻滞剂，可在实验动物和人体中诱导肾血管舒张，并增加肾小球滤过率（GFR）、尿量和尿钠排泄。替他洛尔对肾脏作用的潜在机制尚不清楚。我们的目的是确定替他洛尔是通过全身作用还是肾内作用影响肾功能，并评估替他洛尔能否在慢性肾衰竭中维持GFR。以25和50微克/千克体重的剂量静脉推注给药时，替他洛尔而非普萘洛尔可使孤立灌注肾模型中的GFR和灌注液流速（PFR）显著增加[GFR：替他洛尔，25微克/千克；注射前：0.477±0.077毫升/分钟/克肾；注射后30分钟：0.996±0.114毫升/分钟/克肾。替他洛尔（50微克/千克）注射前：0.517±0.040毫升/分钟/克肾；注射后30分钟：0.879±0.035毫升/分钟/克肾。普萘洛尔（500微克/千克）注射前：0.574±0.045毫升/分钟/克肾；注射后30分钟：0.538±0.029毫升/分钟/克肾。PFR：替他洛尔，25微克/千克，注射前：30.00±0.79毫升/分钟；注射后30分钟：36.20±2.58毫升/分钟。替他洛尔（50微克/千克）注射前：29.30±1.44毫升/分钟；注射后30分钟：38.01±1.87毫升/分钟。普萘洛尔（500微克/千克）注射前：28.70±1.04毫升/分钟；注射后30分钟：28.30±0.91毫升/分钟]。在相同的制剂中，替他洛尔可显著增加尿流率和钠排泄[尿流率：替他洛尔（25微克/千克）注射前：28.28±4.10微升/分钟；注射后60分钟：38.23±6.74微升/分钟。替他洛尔（50微克/千克）注射前：24.02±0.63微升/分钟；注射后60分钟：33.18±2.07微升/分钟。（摘要截断于250字）
