کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5827123 1558917 2015 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Biased agonism at kappa opioid receptors: Implication in pain and mood disorders
ترجمه فارسی عنوان
آگونیستی منفی در گیرنده های کاپا اپیوئید: ناشی از اختلالات درد و خلق
کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
چکیده انگلیسی
The kappa opioid receptor (k receptor) and its endogenous ligand dynorphin have received significant attention due to their involvement in pathophysiology of mood disorders, drug addiction, psychotic disorders and pain. Multiple lines of evidences suggest that the k receptor modulates overlapping neurocircuits connecting brainstem monoaminergic nuclei with forebrain limbic structures and thereby regulates neurobiological effects of stress and psychostimulants. The emerging concept of “biased agonism” (also known as functional selectivity) for G Protein Coupled Receptor (GPCR) ligands have provided new insights into overall response generated by a ligand, which could be exploited for drug discovery. According to this concept, every ligand possesses the unique ability (coded in its structure) that dictates distinct signalling pattern, and consequently beneficial or adverse response. Although still a long way to comprehend the clinical potential of biased GPCR ligands, such ligand could be vital pharmacological probes. This article highlights various lines of evidence, which indicates different ligands of k receptor as “biased”, and their potential implications in mood and pain disorders.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 763, Part B, 15 September 2015, Pages 184-190
نویسندگان
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