Novel Ligands for the Investigation of Imidazoline Receptors and Their Binding Proteins

摘要: New ligands for imidazoline receptors are described so that these can be more fully explored and understood. BU224, (2-(4,5-dihydroimidaz-2-yl)-quinoline, shows high affinity is selective the imidazoline-2 (I(2)) class of receptors. BU224 was tested in rat Porsolt forced swim paradigm where it found to decrease time spent immobile increase swimming, consistent with an antidepressant profile. tritiated and, radioligand binding studies, label a single population saturable sites affinity. In vitro brain autoradiography [(3)H]BU224 also showed pattern distribution similar known labeling I(2) A new series four 2BFI (2-(benzofuranyl)-2-imidazoline) derivatives were investigated as potential imaging using positron emission tomography (PET). At least two, BU20012 BU20013, retained moderate selectivity penetrated when administered peripherally mouse. has undergone Mannich reaction immobilized diaminodipropyl amine fabricate column, which used isolate protein from rabbit brain; this sequenced identified enzyme creatine kinase.