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        [3H]2-(2-Benzofuranyl)-2-imidazoline : a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptors

        Author
        Lione, Lisa
        Nutt, D.J.
        Hudson, A.L.
        Attention
        2299/13008
        Abstract
        This is the first study characterising the binding of the new imidazoline I2 receptor selective radioligand [3H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) to rabbit brain membranes. [3H]2-BFI binding was found to be saturable and of high affinity identifying two binding sites with KD1 = 0.27 nM, Bmax = 111.2 fmol mg−1 protein and KD2 = 8.97 nM, Bmax = 268 fmol mg−1 protein. Specific binding represented greater than 90% of total binding. Kinetic studies revealed that the binding was rapid and reversible and also showed [3H]2-BFI interacted with these two sites or two affinity states. In competition binding studies against [3H]2-BFI (0.3-lnM) idazoxan, 2-BFI, cirazoline, guanabenz, naphazoline, amiloride and BU224 (2-(4,5-dihydroimidaz-2-yl-quinoline) displaced with high affinity. In contrast the α2-adrenoceptor antagonists efaroxan and rauwolscine, the I1 site selective drug moxonidine, the monoamine oxidase-A inhibitor clorgyline and the proposed endogenous imidazoline receptor ligand, agmatine, were weak at displacing [3H]2-BFI binding. These findings are consistent with [3H]2-BFI recognising imidazoline receptors of the I2 subtype in rabbit brain
        Publication date
        1996-05
        Published in
        European Journal of Pharmacology
        Published version
        https://doi.org/10.1016/0014-2999(96)00131-8
        Other links
        http://hdl.handle.net/2299/13008
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