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• W2137480040 abstract "It has been suggested that 'clonidine-displacing substance' (CDS) is a putative endogenous substance at imidazoline receptor. CDS was found to recognize not only the imidazoline binding sites but also a 2 -adrenoceptors. However, the information of the functional activities of CDS at the a 2 -adrenoceptor is still limited. The aim of this study was to examine the properties and functions of CDS, in particular, the actions at a 2 -adrenoceptor. In the present study, the methanolic CDS extracts were prepared from bovine brain. CDS activity was determined by the amount of the extract that displaced 50% of [ 3 H]-clonidine binding to bovine cerebral cortex membranes. CDS activity from bovine brain methanolic extract was 4.8±0.5 units/g wet weight. Based on radioligand binding assays, this extract recognized both a 2 -adrenoceptor on bovine cerebral cortex membranes labeled by [ 3 H]-clonidine and non-adrenoceptor imidazoline binding sites on porcine renal cortex membranes labeled by [ 3 H]-idazoxan. The CDS extract was found to be slightly more potent (2 folds) at a 2 -adrenoceptor than at non-adrenoceptor imidazoline binding sites. Functional studies of CDS were examined in the models of a,-adrenoceptor-mediated inhibition of forskolin-stimulated cAMP accumulation in guineapig cerebral cortex slices and in porcine isolated palmar lateral vein. The effects were compared to those of the known a,-adrenoceptor agonists, UK14304 and antagonized by the a 2 -adrenoceptor antagonist, idazoxan. The results from this study showed that bovine brain methanolic CDS extract did not display any activity involving a,-adrenoceptors as predicted from radioligand binding. In conclusion, CDS is able to displace clonidine from a 2 -adrenoceptor but no related biological activity was detected at this sites. Whether the possibility that CDS is an endogenous ligand at a 2 -adrenoceptor and at non-adrenoceptor imidazoline binding sites and possesses any significant activities at these sites remain to be clarified." @default.
• W2137480040 created "2016-06-24" @default.
• W2137480040 creator A5057830661 @default.
• W2137480040 date "2000-01-01" @default.
• W2137480040 modified "2023-09-26" @default.
• W2137480040 title "NO EVIDENCE FOR THE ACTIONS OF 'CLONIDINE-DISPLACING SUBSTANCE' ON ALPHA2-ADRENOCEPTORS" @default.
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