differential modulation of beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists该项受体信号的差分调制跟踪amine-associated受体1受体激动剂.pdfVIP

Differential Modulation of Beta-Adrenergic Receptor Signaling by Trace Amine-Associated Receptor 1 Agonists 1. 1. ¨ 1 ¨ 1 ¨ 3 Gunnar Kleinau , Juliane Pratzka , Daniela Nurnberg , Annette Gruters , Dagmar Fuhrer-Sakel , 1 ¨ 2 ¨ 4 1 Heiko Krude , Josef Kohrle , Torsten Schoneberg , Heike Biebermann * ´ ¨ ´ 1 Institute of Experimental Pediatric Endocrinology, Charite-Universitatsmedizin Berlin, Berlin, Germany, 2 Institute of Experimental Endocrinology, Charite- ¨ ¨ ¨ ¨ Universitatsmedizin Berlin, Berlin, Germany, 3 Klinik fur Endokrinologie, Zentrum fur Innere Medizin, Universitatsklinikum Essen, Essen, Germany, 4 Institute of Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany Abstract Trace amine-associated receptors (TAAR) are rhodopsin-like G-protein-coupled receptors (GPCR). TAAR are involved in modulation of neuronal, cardiac and vascular functions and they are potentially linked with neurological disorders like schizophrenia and Parkinson’s disease. Subtype TAAR1, the best characterized TAAR so far, is promiscuous for a wide set of ligands and is activated by trace amines tyramine (TYR), phenylethylamine (PEA), octopamine (OA), but also by thyronamines, dopamine, and psycho-active drugs. Unfortunately, effects of trace amines on signali