Acute effect of L‐796568, a novel β3‐adrenergic receptor agonist, on energy expenditure in obese men

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Abstract
Objective: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel β3- adrenergic receptor agonist L-796568 ((R)-N-(4-(2-((2-hydroxy-2-(3-pyridinyl)ethyl)amino)ethyl)- phenyl)-4-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)-benzenesulfonamide, dihydrochloride) in humans. Methods: Twelve healthy overweight to obese men participated in this 2-center, 3-period, randomized, placebo-controlled, crossover trial. In each period subjects received 250 mg L-796568, 1000 mg L-796568, or placebo. Energy expenditure and respiratory quotient were determined by indirect calorimetry; blood samples were taken; and ear temperature, heart rate, and blood pressure were measured at baseline and during the 4-hour period after administration. Results: Energy expenditure increased significantly after the 1000-mg dose (about 8%) and this was accom- panied by an increase in plasma glycerol and free fatty acid concentrations. Systolic blood pressure also increased significantly. No changes in heart rate, diastolic blood pressure, ear temperature, plasma cate- cholamine, potassium, or leptin were found. Conclusions: Single-dose administration of 1000 mg of the novel β3-adrenergic receptor agonist L-796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of β3-adrenergic receptor agonists in humans without significant evidence for β2-adrenergic receptor involvement. (Clin Pharmacol Ther 2002;71:272-9.)

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