Identification of an imidazoline binding protein: Creatine kinase and an imidazoline-2 binding site
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چکیده
منابع مشابه
Identification of an imidazoline binding protein: Creatine kinase and an imidazoline-2 binding site
Drugs that bind to imidazoline binding proteins have major physiological actions. To date, three subtypes of such proteins, I(1), I(2) and I(3), have been proposed, although characterisations of these binding proteins are lacking. I(2) binding sites are found throughout the brain, particularly dense in the arcuate nucleus of the hypothalamus. Selective I(2) ligands demonstrate antidepressant-li...
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Monoamine oxidase B (MAO-B) was recently identified as a member of the family of imidazoline binding proteins. To localize the imidazoline binding domain on MAO-B, we labeled the domain with the imidazoline photoaffinity adduct [125I]2-(3-azido-4-iodophenoxy)methylimidazoline in rat and human liver and visualized labeled peptides by autoradiography/sodium dodecyl sulfate-polyacrylamide gel elec...
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Over the past few years, a vast amount of research has shed light on the pharmacology of imidazoline binding sites (I-BS). To date, at least three classes of imidazoline binding sites have been characterised in accordance to their localisation, drug selectivity, proposed signalling pathways and functional roles. The existence of these sites raises the question as to whether an endogenous modula...
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Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided pa...
متن کاملEffects of the imidazoline binding site ligands, idazoxan and efaroxan, on the viability of insulin-secreting BRIN-BD11 cells.
CONTEXT Certain imidazoline drugs stimulate insulin secretion acutely but their longer term effects on the viability of pancreatic beta-cells are less well characterised. Indeed, some reports have suggested that imidazolines can be toxic to beta-cells while others have reported protective effects against other cytotoxic agents. OBJECTIVE In order to address these discrepancies, the effects of...
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ژورنال
عنوان ژورنال: Brain Research
سال: 2009
ISSN: 0006-8993
DOI: 10.1016/j.brainres.2009.04.044