title: Studies of 99mTc-acylplasmins as agents for thrombus detection.
abstract: It has been proposed that acylation at the active site of plasmin is able to prevent its reaction with alpha 2-antiplasmin without affecting the fibrin affinity of the enzyme. To investigate the possibility that 99mTc-labelled acylplasmins are improved thrombus-detecting agents, six acylating agents were synthesised and their reaction with plasmin and the labelling of the products with 99mTc studies. Uptake of 99mTc-acylplasmins in an in vitro thrombus model was complicated by precipitation processes, which may in part account for the rapid blood clearance in rabbits and high liver uptake in mice injected with the compounds. Quantitative measurements using an in vivo rabbit thrombus model demonstrated that guanidinobenzoyl-plasmin exhibited nearly a threefold increase in thrombus uptake compared with non-acylated 99mTc-plasmin. The observed uptake is less than that obtained with 125I-fibrinogen at clinically useful time intervals post-injection but represents a significant advantage over the use of 99mTc-plasmin.
authors.forename: R J
authors.initials: RJ
authors.lastname: Baker
authors.forename: A B
authors.initials: AB
authors.lastname: McLaren
authors.forename: J
authors.initials: J
authors.lastname: Campbell
authors.forename: J C
authors.initials: JC
authors.lastname: Bellen
authors.forename: T R
authors.initials: TR
authors.lastname: Kuchel
mesh_terms: D000215:Acylation; D000818:Animals; D005260:Female; D005341:Fibrinolysin / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008657:Metabolic Clearance Rate; D051379:Mice; D015609:Organotechnetium Compounds; D011817:Rabbits; D011877:Radionuclide Imaging; D013667:Technetium / Q000378:metabolism; D013927:Thrombosis / Q000000981:diagnostic imaging* / Q000378:metabolism
chemical_list: D015609:Organotechnetium Compounds; C034360:technetium Tc 99m plasmin; D013667:Technetium; D005341:Fibrinolysin