School, Minamikawachi-machi, Tochigi Prefecture, Japan 1 The cardiovascular effects of three single intravenous doses of a Pl-adrenoceptor partial agonist, xamoterol (0.025, 0.05 and 0.1 mg kg-') and placebo were studied in six healthy volunteers at rest using a single-blind design. 2 In addition to heart rate and blood pressure measurements, cardiac contractility was measured by means of M-mode echocardiography and systolic time intervals. Ambulatory 24 h Holter-monitoring of the electrocardiogram was performed. Plasma concentrations of xamoterol were measured. 3 Compared to baseline, xamoterol (0.025 mg kg-) increased heart rate (61 + 3-68 ± 3 beats min-1, means and SEM) and systolic blood pressure (119 ± 3-138 + 5 mm Hg) but decreased pre-ejection period (100 + 4-76 + 5 msec). Stroke volume (88 ± 6-104 + 10 ml), cardiac output (4.8 ± 0.4-6.6 ± 0.6 1 min-'), velocity of circumferential fibre shortening (1.15 ± 0.06-1.50 ± 0.06 circ s-1) were increased by xamoterol. No significant changes were produced by placebo. 4 No dose-dependent effects were seen and maximum effects were produced by 0.025 mg kg-' xamoterol. Significant effects were observed for 2 h. The areas under the plasma concentration curves (AUCO.12) showed a linear dose response.