title: Assessment of i.p. injection of [18F]fallypride for behavioral neuroimaging in rats.
abstract: Great progress has been made toward using small animal PET to assess neurochemical changes during behavior. [(18)F]fallypride (FAL) is a D(2)/D(3) antagonist that is sensitive to changes in endogenous dopamine, and, in theory, could be used to assess changes in dopamine during behavioral paradigms. Tail vein injections of tracer require restraint in awake animals, and catheter implantation is invasive and can cause logistical problems. Thus, administering tracer with i.p. injections (which are well-tolerated by rodents) would be preferable. The purpose of this study was to determine whether i.p. injection of FAL would produce striatal uptake similar to that seen with traditional i.v. tail vein injection protocols. Four male Sprague-Dawley rats underwent i.p. injection of FAL, followed by a 30-min uptake and subsequent dynamic image acquisition on the IndyPET III small animal scanner. Three of these rats also received traditional dynamic scanning with i.v. FAL injection via a tail vein. Two rats that received i.p. injection had moderate striatal uptake, with striatum/cerebellum ratios (SUVR) that were only ∼20% lower than ratios from i.v. scans. Two other rats had little to no uptake; SUVR values were ∼70% lower than i.v. SUVR. These latter two animals showed heavy bone uptake, evidence of defluorination of FAL. The results of this pilot study suggest that it may be possible to achieve striatal uptake of FAL after i.p. injection. However, this was not seen consistently across animals. Future studies are needed to validate, and then to optimize, the use of i.p. FAL for behavioral imaging protocols.
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, R2 E124, 950 W. Walnut St., Indianapolis, IN 46202, USA. kkyoder@iupui.edu
authors.forename: Karmen K
authors.initials: KK
authors.lastname: Yoder
authors.forename: Bruce H
authors.initials: BH
authors.lastname: Mock
authors.forename: Qi-Huang
authors.initials: QH
authors.lastname: Zheng
authors.forename: Brian P
authors.initials: BP
authors.lastname: McCarthy
authors.forename: Amanda A
authors.initials: AA
authors.lastname: Riley
authors.forename: Gary D
authors.initials: GD
authors.lastname: Hutchins
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects* / Q000502:physiology; D001549:Benzamides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001921:Brain / Q000033:anatomy & histology / Q000000981:diagnostic imaging* / Q000187:drug effects; D018492:Dopamine Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D007274:Injections, Intraperitoneal / Q000379:methods; D008297:Male; D049268:Positron-Emission Tomography / Q000379:methods; D011485:Protein Binding / Q000187:drug effects; D011759:Pyrrolidines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors
chemical_list: D001549:Benzamides; D018492:Dopamine Antagonists; C094948:N-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide; D011759:Pyrrolidines