Radioimaging moieties coupled to peptidase-binding moieties...

Details Radioimaging moieties coupled to peptidase-binding moieties... Radioimaging moieties coupled to peptidase-binding moieties...

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 51/04 (2006.01) C07D 207/16 (2006.01) C07D 213/36 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01) G01T 1/161 (2006.01) A61M 36/06 (2006.01)

Patent

CA 2661979

Conjugates, methods and kits are described for imaging tissues and organs that express one or more peptidases. In a preferred embodiment of the invention, a series of di-(2-pyridylmethyl)amine (D) ligands, which can bind M(CO)3 + [M = Tc or Re], were coupled to lisinopril (L). Aliphatic tethers with varying number of methylene groups (3, 4, 5, and 7; D(C4)L, D(C5)L, D(C6)L, and D(C8)L, respectively) were utilized, with in vitro inhibitory activity increasing with increasing number of methylene groups. The D(C8)L conjugate was observed to be significantly more potent than D(C4)L. In vivo specificity for ACE was studied in both tissue distribution and gamma imaging studies, demonstrating localization in tissues with high ACE content. Localization was blocked by pretreatment with lisinopril.

La présente invention concerne des conjugués, des procédés et des trousses permettant d'imager des tissus et des organes exprimant une ou plusieurs peptidases. Dans un mode de réalisation préféré de cette invention, une série de ligands de di-(2-pyridylméthyl)amine (D), qui peuvent lier M(CO)3 + [M = Tc ou Re], est couplée à du lisinopril (L). Des attaches aliphatiques comportant un nombre variable de groupes méthylène (3, 4, 5 et 7; respectivement D(C4)L, D(C5)L, D(C6)L et D(C8)L) sont utilisées, l'activité inhibitrice in vitro augmentant parallèlement à l'augmentation du nombre de groupes méthylène. Le conjugué D(C8)L se révèle être nettement plus puissant que le conjugué D(C4)L. La spécificité in vivo vis à vis de l'enzyme de conversion de l'angiotensine (ACE) étudiée dans des études de distribution tissulaire et d'imagerie gamma démontre une localisation dans des tissus à forte teneur en enzyme de conversion de l'angiotensine, laquelle localisation est bloquée par un prétraitement à base de lisinopril.

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