Tertatolol is a beta-blocker with unique renal vasodilatatory effects, mainly at the level of the microcirculation. The mechanisms of this renal vasodilatation are not fully understood but might involve renal 5-HT1A receptor stimulation. It is a potent competitive antagonist of 5-HT1A and 5-HT1B receptors. Tertatolol inhibits human mesangial cell proliferation. Biochemical surveillance did not show any adverse metabolic effects of tertatolol. Tertatolol is rapidly and totally absorbed by the gastro-intestinal tract with a low presystemic metabolism, and the bioavailability is not affected by food intake. It is used as antihypertension agent.