Cited by 110Adipose Tissue and MetabolismPharmacology and Obesity TreatmentRegulation of Appetite and Obesity

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

Open access
van Baak, Marleen A., Hul, Gabby B. J., Toubro, Søren, Astrup, Arne, Gottesdiener, Keith M., DeSmet, Marina, Saris, Wim H. M.·2002·Clinical Pharmacology & Therapeutics

Abstract

Objective: Our objective was to investigate the thermogenic efficacy of single oral doses of the novel β 3‐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] inhumans. 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 accompanied 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 catecholamine, potassium, orleptin were found. Conclusions: Single‐dose administration of 1000 mg of the novel β 3‐adrenergic receptor agonist L‐796568 increased lipolysis and energy expenditure in overweight men. This is the first study to show such an effect of β 3‐adrenergic receptor agonists in humans without significant evidence for β 2‐adrenergic receptor involvement. Clinical Pharmacology & Therapeutics (2002) 71, 272–279; doi: 10.1067/mcp.2002.122527

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Integrity signals

Registry

Crossref · 10.1067/mcp.2002.122527

Cites

29 of 29 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • One β3 agonist, L-796568, increased lipolysis and energy expenditure in overweight men acutely.

    “One β3 agonist, L-796568, increased lipolysis and energy expenditure in overweight men acutely 142, but its effect seemed to be lost after 28 days of treatment 79,141.”

    From Cellular bioenergetics as a target for obesity therapy (2010) · cites this paper as [142]

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Cites

Flagged first, then by citations

1 of the 30 references couldn’t be matched to a known paper.

Research works printed but not linked: 5

  1. Blaak EE, van Baak MA, Kempen KP, Saris WH. Role of α-and β-adrenoceptors in sympathetically mediated thermogenesis. Am J Physiol 1993;264:E11-7.
  2. Gauthier C, Tavernier G, Charpentier F, Langin D, Le Marec H. Functional β 3 -adrenoceptor in the human heart. J Clin Invest 1996;98:556-62.
  3. Enocksson S, Shimizu M, Lönnqvist F, Nordenström J, Arner P. Demonstration of an in vivo functional β 3 - adrenoceptor in man. J Clin Invest 1995;95:2239-45.
  4. Tavernier G, Barbe P, Galitzky J, Berlan M, Caput D, Lafontan M, et al. Expression of β 3 -adrenoceptor with low lipolytic action in human subcutaneous white adipocytes. J Lipid Res 1996;37:87-97.
  5. Demacker PN, Hymans AG, Jansen AP. Enzymatic and chemical extraction determinations of free fatty acids in serum compared. Clin Chem 1982;28:1765-8.

Cited by

Sorted by citations

Authors
van Baak, M. A., Hul, G. B. J., Toubro, S., Astrup, A., Gottesdiener, K. M., DeSmet, M., & Saris, W. H. M.
Affiliations
  • Nutrition and Toxicology Research Institute (NUTRIM), Department of Human Biology Maastricht University Maastricht The Netherlands
  • Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
Venue
Clinical Pharmacology & Therapeutics
Publisher
Wiley
Published
2002-04
Volume
71
Issue
4
Pages
272-279
ISSN
  • 0009-9236 (ISSN-L)
  • 1532-6535
OpenAlex
W2038927385
Cited by
103
References
30
Citations by year
2024: 1 · 2023: 2 · 2022: 5 · 2021: 5 · 2019: 3 · 2018: 7 · 2017: 7 · 2016: 6 · 2015: 5 · 2014: 4 · 2013: 2 · 2012: 1
FWCI
3.20
Type
journal article
Language
en
Open access
Locations
  • Clinical Pharmacology & Therapeutics (publishedVersion)
  • PubMed (publishedVersion)
  • Research Publications (Maastricht University) (publishedVersion, other-oa)
  • Research Publications (Maastricht University) (submittedVersion, other-oa)
Topics
  • Health Sciences › Medicine › Physiology › Adipose Tissue and Metabolism
  • Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
Keywords
beta3-adrenergic agonists, energy expenditure, thermogenesis, obesity, lipolysis, free fatty acids, plasma glycerol, respiratory quotient, blood pressure, catecholamines, leptin, overweight men
MeSH terms
Benzenesulfonamides, Administration, Oral, Adolescent, Adrenergic beta-Agonists, Adult, Analysis of Variance, Energy Metabolism, Humans, Lipolysis, Middle Aged, Obesity, Sulfonamides, Thiazoles, Cross-Over Studies, Anti-Obesity Agents, Adrenergic beta-3 Receptor Agonists

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review