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dc.contributor.authorLione, Lisa
dc.contributor.authorNutt, D.J.
dc.contributor.authorHudson, A.L.
dc.date.accessioned2014-03-04T16:29:03Z
dc.date.available2014-03-04T16:29:03Z
dc.date.issued1996-05
dc.identifier.citationLione , L , Nutt , D J & Hudson , A L 1996 , ' [ 3 H]2-(2-Benzofuranyl)-2-imidazoline : a new selective high affinity radioligand for the study of rabbit brain imidazoline I 2 receptors ' , European Journal of Pharmacology , vol. 304 , no. 1-3 , pp. 221-229 . https://doi.org/10.1016/0014-2999(96)00131-8
dc.identifier.issn0014-2999
dc.identifier.otherPURE: 1491813
dc.identifier.otherPURE UUID: ed337fef-78ab-4295-95db-2913c0784788
dc.identifier.otherScopus: 0030598574
dc.identifier.urihttp://hdl.handle.net/2299/13008
dc.description.abstractThis 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 brainen
dc.language.isoeng
dc.relation.ispartofEuropean Journal of Pharmacology
dc.title[3H]2-(2-Benzofuranyl)-2-imidazoline : a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptorsen
dc.contributor.institutionDepartment of Human and Environmental Sciences
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.contributor.institutionPharmacology and Clinical Science Research
dc.contributor.institutionCardiovascular Pathologies
dc.contributor.institutionDiabetic neuropathies
dc.contributor.institutionTRP Ion channels
dc.description.statusPeer reviewed
rioxxterms.versionofrecordhttps://doi.org/10.1016/0014-2999(96)00131-8
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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