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The present review addresses the theories which have been advanced to explain experimental observations dealing with insurmountable antagonism and accelerated radioligand dissociation in the presence of an excess unlabelled ligand. We came to the perception that, for each of these phenomena, the...
The present study confirmed our previous assumption on the crucial role of central α 2B -like adrenoceptor subtype in gastric mucosal defense. It was found that beside clonidine, rilmenidine, an α 2 /imidazoline receptor agonist and ST-91, an α 2B -adrenoceptor preferring agonist inhibited the...
The inhibitory effect of clonidine (non-selective α 2 -adrenoceptor agonist) and oxymetazoline (α 2A -adrenoceptor selective agonist) was compared on basal and stimulated gastric motor activity (gastric tone and contractions) using the balloon method in the rat. It was shown that oxymetazoline...
One of the most important clinical pharmacological invention in the last decades the role of adrenoreceptors in urological disease. The disorders of emptying the bladder are associated to the urology. Plant extracts efficacy is low, indicated only in mild symptoms, surgery has to be performed in...
Three-dimensional structure–activity relationship studies of α 2a -adrenoceptor agonists were carried out by Distance Comparison (DISCOthech) and Comparative Molecular Field Analysis (CoMFA) methods to define the pharmacophore and a quantitative model, respectively, of this class of compounds....
G protein-coupled receptors are cell surface receptors that mediate the effects of extracellular signals in the endocrine/paracrine and sensory systems. Experimental evidence is accumulating, which suggest that these receptors form dimers or higher order oligomers. The functional relevance of G...
The gastrointestinal tract is innervated by extrinsic noradrenergic nerves which regulate various digestive functions, including mucosal secretions, bowel propulsion and gut sensations, via activation of α 2 -adrenoceptors. These receptors are mostly involved in the prejunctional modulation of...
Childhood and adolescent depression is an increasingly problematic diagnosis for young people due to a lack of effective treatments for this age group. The symptoms of adult depression can be treated effectively with multiple classes of antidepressant drugs which have been developed over the...
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