دورية أكاديمية
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In Vitro Activation of Human Adrenergic Receptors and Trace Amine-Associated Receptor 1 by Phenethylamine Analogues Present in Food Supplements.

التفاصيل البيبلوغرافية
العنوان: In Vitro Activation of Human Adrenergic Receptors and Trace Amine-Associated Receptor 1 by Phenethylamine Analogues Present in Food Supplements.
المؤلفون: Pinckaers NET; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands.; Research Institute of Nutrition and Translational Research in Metabolism (NUTRIM), Maastricht University, 6200 MD Maastricht, The Netherlands., Blankesteijn WM; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands.; School for Cardiovascular Diseases (CARIM), Maastricht University, 6200 MD Maastricht, The Netherlands., Mircheva A; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands., Shi X; Research Service, Veterans Affairs Portland Health Care System, Portland, OR 97239, USA.; Department of Psychiatry, Oregon Health and Science University, Portland, OR 97239, USA., Opperhuizen A; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands.; Office for Risk Assessment and Research, Netherlands Food and Consumer Product Safety Authority, 3540 AA Utrecht, The Netherlands., Schooten FV; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands.; Research Institute of Nutrition and Translational Research in Metabolism (NUTRIM), Maastricht University, 6200 MD Maastricht, The Netherlands., Vrolijk MF; Department of Pharmacology and Toxicology, Maastricht University, 6200 MD Maastricht, The Netherlands.; Research Institute of Nutrition and Translational Research in Metabolism (NUTRIM), Maastricht University, 6200 MD Maastricht, The Netherlands.
المصدر: Nutrients [Nutrients] 2024 May 22; Vol. 16 (11). Date of Electronic Publication: 2024 May 22.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Publishing Country of Publication: Switzerland NLM ID: 101521595 Publication Model: Electronic Cited Medium: Internet ISSN: 2072-6643 (Electronic) Linking ISSN: 20726643 NLM ISO Abbreviation: Nutrients Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI Publishing
مواضيع طبية MeSH: Phenethylamines*/pharmacology , Receptors, G-Protein-Coupled*/metabolism , Receptors, G-Protein-Coupled*/agonists , Dietary Supplements*, Humans ; Receptors, Adrenergic/metabolism ; HEK293 Cells
مستخلص: Pre-workout supplements are popular among sport athletes and overweight individuals. Phenethylamines (PEAs) and alkylamines (AA) are widely present in these supplements. Although the health effects of these analogues are not well understood yet, they are hypothesised to be agonists of adrenergic (ADR) and trace amine-associated receptors (TAARs). Therefore, we aimed to pharmacologically characterise these compounds by investigating their activating properties of ADRs and TAAR1 in vitro . The potency and efficacy of the selected PEAs and AAs was studied by using cell lines overexpressing human ADRα 1A /α 1B /α 1D /α 2a /α 2B /β 1 /β 2 or TAAR1. Concentration-response relationships are expressed as percentages of the maximal signal obtained by the full ADR agonist adrenaline or the full TAAR1 agonist phenethylamine. Multiple PEAs activated ADRs (EC 50 = 34 nM-690 µM; E max = 8-105%). Almost all PEAs activated TAAR1 (EC 50 = 1.8-92 µM; E max = 40-104%). Our results reveal the pharmacological profile of PEAs and AAs that are often used in food supplements. Several PEAs have strong agonistic properties on multiple receptors and resemble potencies of the endogenous ligands, indicating that they might further stimulate the already activated sympathetic nervous system in exercising athletes via multiple mechanisms. The use of supplements containing one, or a combination of, PEA(s) may pose a health risk for their consumers.
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معلومات مُعتمدة: n.a. The Dutch Ministry of Agriculture, Nature and Food Quality
فهرسة مساهمة: Keywords: adrenaline; adrenergic receptors; alkylamine analogues; food supplements; phenethylamine analogues; trace amine-associated receptor 1
المشرفين على المادة: 0 (Phenethylamines)
0 (Receptors, G-Protein-Coupled)
XMC8VP6RI2 (Trace amine-associated receptor 1)
327C7L2BXQ (phenethylamine)
0 (Receptors, Adrenergic)
تواريخ الأحداث: Date Created: 20240619 Date Completed: 20240619 Latest Revision: 20240625
رمز التحديث: 20240626
مُعرف محوري في PubMed: PMC11174489
DOI: 10.3390/nu16111567
PMID: 38892500
قاعدة البيانات: MEDLINE
الوصف
تدمد:2072-6643
DOI:10.3390/nu16111567