Effect of bunazosin, alpha 1-adrenoceptor blocker, on multidirectional contractile response and localization of bunazosin binding sites in human hypertrophied prostate.

1. Effects of bunazosin, an alpha 1-adrenoceptor blocker, on the contraction induced by norepinephrine in human hypertrophied prostate were examined in vitro. 2. Prostatic specimens showed maximum contraction at 10(-4) M norepinephrine in longitudinal and circumferential directions to the urethra. 3. Bunazosin (10(-7) M) blocked norepinephrine-induced contraction with a parallel shift of the dose-response curve in both directions (pA2: 8.76 +/- 0.15; pA2: 8.90 +/- 0.08, respectively). 4. Serial sections of prostates were also evaluated by autoradiography. The binding sites were diffusely distributed in the interstitium. 5. We concluded that bunazosin affects multidirectional contraction in prostates.

[Influence of indometacin farnesil on blood coagulation. Comparison with indomethacin in normal rats and warfarin induced hypoprothrombinemic rats].

The influence of indometacin farnesil (IMF), a prodrug of indomethacin, on blood coagulation was compared with indomethacin (Ind) in normal rats and warfarin treated rats. In normal rats, 30 mg/kg of Ind very markedly shortened the extrinsic coagulation time and decreased the hematocrit, GOT, GPT and ALP in plasma at 24 hr after administration, but 3 mg/kg of Ind and both 10 and 100 mg/kg of IMF did not influence any parameter. In warfarin treated rats, 2.5 mg/kg of Ind decreased the normal prothrombin level at 48 hr, and 10 mg/kg of Ind prolonged the blood coagulation time, decreased the normal prothrombin level and hematocrit, and increased the PIVKA-II level. Moreover, at 48 hr, 3 of 6 rats in the 10 mg/kg Ind-administered group died due to intestinal bleeding. IMF at all dosages examined did not affect any of the above parameters.