title: Myocardial extraction of teboroxime: effects of teboroxime interaction with blood.
abstract: The isolated perfused rat heart preparation was used to determine whether the interaction of blood with either 99mTc-teboroxime, 99mTc-sestamibi or 201TI affects the extraction of these myocardial perfusion agents. Hearts were retrogradely perfused at 72 cm H2O with Krebs-Henseleit buffer equilibrated with O2:CO2 (95:5). The hearts were paced at 5 Hz. Single-pass extraction of 99mTc-teboroxime (96% +/- 1%) was greater than that of 99mTc-sestamibi (15% +/- 1%) or 201TI (30% +/- 5%). Extraction of the hydroxide form of 99mTc-teboroxime was only 43% +/- 4%. When arterial blood obtained from rats administered 99mTc-teboroxime was injected into the perfused heart, extraction of 99mTc-teboroxime decreased progressively as its time in circulation was lengthened. Similar experiments using either 99mTc-sestamibi or 201TI showed that extraction of these agents was neither affected by the presence of blood nor residence in circulation. For 99mTc-teboroxime, extraction was 99.5% +/- 0.5%, 57% +/- 13%, 20% +/- 2% at 1, 5, and 60 min postinjection, respectively. In separate experiments, HPLC analysis of blood at 5, 15 and 60 min postinjection indicated that only 34% +/- 4%, 13% +/- 2%, and 2% +/- 1%, respectively, of the total 99mTc-teboroxime was free and was associated with extraction values of 44% +/- 7%, 28% +/- 5%, and 19% +/- 3%, respectively. The percentage of this free radioactivity that converted from the chloro to the hydroxide form was 9% +/- 2%, 6% +/- 2%, and 2% +/- 1%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
authors.affiliation: Department of Radiopharmaceuticals, Bristol-Myers Squibb Pharmaceutical Research Institute, New Brunswick, NJ 08903.
authors.forename: W L
authors.initials: WL
authors.lastname: Rumsey
authors.forename: K C
authors.initials: KC
authors.lastname: Rosenspire
authors.forename: A D
authors.initials: AD
authors.lastname: Nunn
mesh_terms: D000818:Animals; D003326:Coronary Circulation; D008297:Male; D009206:Myocardium / Q000378:metabolism*; D015609:Organotechnetium Compounds / Q000097:blood / Q000493:pharmacokinetics*; D010091:Oximes / Q000097:blood / Q000493:pharmacokinetics*; D010477:Perfusion; D051381:Rats; D011919:Rats, Inbred Strains; D017256:Technetium Tc 99m Sestamibi; D013794:Thallium Radioisotopes / Q000097:blood / Q000493:pharmacokinetics; D013997:Time Factors
chemical_list: D015609:Organotechnetium Compounds; D010091:Oximes; D013794:Thallium Radioisotopes; C072256:technetium Tc 99m-OH(CDO)3 MEB; D017256:Technetium Tc 99m Sestamibi; C060156:technetium Tc 99m teboroxime