Semaglutide lowers body weight in rodents via distributed neural pathways

Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here sh...

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Veröffentlicht in:JCI insight Jg. 5; H. 6
Hauptverfasser: Gabery, Sanaz, Salinas, Casper G., Paulsen, Sarah J., Ahnfelt-Rønne, Jonas, Alanentalo, Tomas, Baquero, Arian F., Buckley, Stephen T., Farkas, Erzsébet, Fekete, Csaba, Frederiksen, Klaus S., Helms, Hans Christian C., Jeppesen, Jacob F., John, Linu M., Pyke, Charles, Nøhr, Jane, Lu, Tess T., Polex-Wolf, Joseph, Prevot, Vincent, Raun, Kirsten, Simonsen, Lotte, Sun, Gao, Szilvásy-Szabó, Anett, Willenbrock, Hanni, Secher, Anna, Knudsen, Lotte Bjerre
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Sprache:Englisch
Veröffentlicht: United States American Society for Clinical Investigation 26.03.2020
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ISSN:2379-3708, 2379-3708
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Abstract Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here show that semaglutide modulated food preference, reduced food intake, and caused weight loss without decreasing energy expenditure. Semaglutide directly accessed the brainstem, septal nucleus, and hypothalamus but did not cross the blood-brain barrier; it interacted with the brain through the circumventricular organs and several select sites adjacent to the ventricles. Semaglutide induced central c-Fos activation in 10 brain areas, including hindbrain areas directly targeted by semaglutide, and secondary areas without direct GLP-1R interaction, such as the lateral parabrachial nucleus. Automated analysis of semaglutide access, c-Fos activity, GLP-1R distribution, and brain connectivity revealed that activation may involve meal termination controlled by neurons in the lateral parabrachial nucleus. Transcriptomic analysis of microdissected brain areas from semaglutide-treated rats showed upregulation of prolactin-releasing hormone and tyrosine hydroxylase in the area postrema. We suggest semaglutide lowers body weight by direct interaction with diverse GLP-1R populations and by directly and indirectly affecting the activity of neural pathways involved in food intake, reward, and energy expenditure.
AbstractList Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here show that semaglutide modulated food preference, reduced food intake, and caused weight loss without decreasing energy expenditure. Semaglutide directly accessed the brainstem, septal nucleus, and hypothalamus but did not cross the blood-brain barrier; it interacted with the brain through the circumventricular organs and several select sites adjacent to the ventricles. Semaglutide induced central c-Fos activation in 10 brain areas, including hindbrain areas directly targeted by semaglutide, and secondary areas without direct GLP-1R interaction, such as the lateral parabrachial nucleus. Automated analysis of semaglutide access, c-Fos activity, GLP-1R distribution, and brain connectivity revealed that activation may involve meal termination controlled by neurons in the lateral parabrachial nucleus. Transcriptomic analysis of microdissected brain areas from semaglutide-treated rats showed upregulation of prolactin-releasing hormone and tyrosine hydroxylase in the area postrema. We suggest semaglutide lowers body weight by direct interaction with diverse GLP-1R populations and by directly and indirectly affecting the activity of neural pathways involved in food intake, reward, and energy expenditure.
Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here show that semaglutide modulated food preference, reduced food intake, and caused weight loss without decreasing energy expenditure. Semaglutide directly accessed the brainstem, septal nucleus, and hypothalamus but did not cross the blood-brain barrier; it interacted with the brain through the circumventricular organs and several select sites adjacent to the ventricles. Semaglutide induced central c-Fos activation in 10 brain areas, including hindbrain areas directly targeted by semaglutide, and secondary areas without direct GLP-1R interaction, such as the lateral parabrachial nucleus. Automated analysis of semaglutide access, c-Fos activity, GLP-1R distribution, and brain connectivity revealed that activation may involve meal termination controlled by neurons in the lateral parabrachial nucleus. Transcriptomic analysis of microdissected brain areas from semaglutide-treated rats showed upregulation of prolactin-releasing hormone and tyrosine hydroxylase in the area postrema. We suggest semaglutide lowers body weight by direct interaction with diverse GLP-1R populations and by directly and indirectly affecting the activity of neural pathways involved in food intake, reward, and energy expenditure.Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here show that semaglutide modulated food preference, reduced food intake, and caused weight loss without decreasing energy expenditure. Semaglutide directly accessed the brainstem, septal nucleus, and hypothalamus but did not cross the blood-brain barrier; it interacted with the brain through the circumventricular organs and several select sites adjacent to the ventricles. Semaglutide induced central c-Fos activation in 10 brain areas, including hindbrain areas directly targeted by semaglutide, and secondary areas without direct GLP-1R interaction, such as the lateral parabrachial nucleus. Automated analysis of semaglutide access, c-Fos activity, GLP-1R distribution, and brain connectivity revealed that activation may involve meal termination controlled by neurons in the lateral parabrachial nucleus. Transcriptomic analysis of microdissected brain areas from semaglutide-treated rats showed upregulation of prolactin-releasing hormone and tyrosine hydroxylase in the area postrema. We suggest semaglutide lowers body weight by direct interaction with diverse GLP-1R populations and by directly and indirectly affecting the activity of neural pathways involved in food intake, reward, and energy expenditure.
Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes. Mechanistic preclinical studies suggest weight loss is mediated through GLP-1 receptors (GLP-1Rs) in the brain. The findings presented here show that semaglutide modulated food preference, reduced food intake, and caused weight loss without decreasing energy expenditure. Semaglutide directly accessed the brainstem, septal nucleus, and hypothalamus but did not cross the blood-brain barrier; it interacted with the brain through the circumventricular organs and several select sites adjacent to the ventricles. Semaglutide induced central c-Fos activation in 10 brain areas, including hindbrain areas directly targeted by semaglutide, and secondary areas without direct GLP-1R interaction, such as the lateral parabrachial nucleus. Automated analysis of semaglutide access, c-Fos activity, GLP-1R distribution, and brain connectivity revealed that activation may involve meal termination controlled by neurons in the lateral parabrachial nucleus. Transcriptomic analysis of microdissected brain areas from semaglutide-treated rats showed upregulation of prolactin-releasing hormone and tyrosine hydroxylase in the area postrema. We suggest semaglutide lowers body weight by direct interaction with diverse GLP-1R populations and by directly and indirectly affecting the activity of neural pathways involved in food intake, reward, and energy expenditure. Semaglutide lowers body weight by direct interaction with diverse neural GLP-1R populations, leading to direct and indirect engagement of brain areas involved in energy balance.
Author Gabery, Sanaz
Salinas, Casper G.
Raun, Kirsten
Paulsen, Sarah J.
Szilvásy-Szabó, Anett
Willenbrock, Hanni
Knudsen, Lotte Bjerre
Nøhr, Jane
Polex-Wolf, Joseph
Fekete, Csaba
Simonsen, Lotte
Frederiksen, Klaus S.
Lu, Tess T.
Ahnfelt-Rønne, Jonas
Baquero, Arian F.
Secher, Anna
Farkas, Erzsébet
Pyke, Charles
Alanentalo, Tomas
John, Linu M.
Buckley, Stephen T.
Prevot, Vincent
Helms, Hans Christian C.
Sun, Gao
Jeppesen, Jacob F.
AuthorAffiliation 4 Inserm, Laboratory of Development and Plasticity of the Neuroendocrine Brain, Jean-Pierre Aubert Research Centre, Lille, France
3 Institute of Experimental Medicine Hungarian Academy of Sciences, Budapest, Hungary
2 Global Research Technologies, Novo Nordisk A/S, Måløv, Denmark, and Seattle, Washington, USA
1 Global Drug Discovery and
AuthorAffiliation_xml – name: 3 Institute of Experimental Medicine Hungarian Academy of Sciences, Budapest, Hungary
– name: 4 Inserm, Laboratory of Development and Plasticity of the Neuroendocrine Brain, Jean-Pierre Aubert Research Centre, Lille, France
– name: 1 Global Drug Discovery and
– name: 2 Global Research Technologies, Novo Nordisk A/S, Måløv, Denmark, and Seattle, Washington, USA
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  givenname: Klaus S.
  surname: Frederiksen
  fullname: Frederiksen, Klaus S.
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  orcidid: 0000-0001-6105-1707
  surname: Helms
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  surname: Knudsen
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/32213703$$D View this record in MEDLINE/PubMed
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2020 American Society for Clinical Investigation 2020 American Society for Clinical Investigation
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Snippet Semaglutide, a glucagon-like peptide 1 (GLP-1) analog, induces weight loss, lowers glucose levels, and reduces cardiovascular risk in patients with diabetes....
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SubjectTerms Ablation
Animals
Area postrema
Blood-brain barrier
Body Weight - drug effects
Brain
Brain - drug effects
Brain stem
c-Fos protein
Cardiovascular diseases
Clinical trials
Diabetes
Diabetes mellitus
Eating - drug effects
Energy expenditure
Energy intake
Energy Metabolism - drug effects
Food
Food intake
Food preferences
Glucagon
Glucagon-like peptide 1
Glucagon-Like Peptide-1 Receptor - drug effects
Glucagon-Like Peptides - pharmacology
Hindbrain
Homeostasis
Hypothalamus
Mice
Neural networks
Neural Pathways - drug effects
Obesity
Parabrachial nucleus
Peptides
Prolactin
Rats
Regulatory approval
Reinforcement
Thyrotropin-releasing hormone
Transcriptomics
Tyrosine 3-monooxygenase
Ventricles (cerebral)
Weight
Weight control
Title Semaglutide lowers body weight in rodents via distributed neural pathways
URI https://www.ncbi.nlm.nih.gov/pubmed/32213703
https://www.proquest.com/docview/3256004058
https://www.proquest.com/docview/2384212103
https://pubmed.ncbi.nlm.nih.gov/PMC7213778
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