First-Pass Cerebral Extraction of Benzamide-Derivative Radiotracers for SPECT

• Published in: Nuclear medicine and biology Vol. 25; no. 3; pp. 289 - 293
• Main Authors: Bottoncetti, Anna, Pupi, Alberto, Sestini, Stelvio, Pecorale, Andrea, Raspanti, Silvia, Meldolesi, Ugo
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Inc 01.04.1998; Elsevier
• Subjects: Animals; Benzamides - pharmacokinetics; Biological and medical sciences; Brain - blood supply; Brain - diagnostic imaging; Brain - metabolism; Cerebral extraction; Cerebrovascular Circulation; Contrast media. Radiopharmaceuticals; Dopamine Agonists - pharmacokinetics; Iodine Radioisotopes - pharmacokinetics; Male; Medical sciences; Pharmacology. Drug treatments; Pyrrolidines - pharmacokinetics; Radioligand Assay; Radiotracers; Rats; Rats, Sprague-Dawley; Regional Blood Flow; Salicylamides - pharmacokinetics; SPECT; Technetium - pharmacokinetics; Tomography, Emission-Computed, Single-Photon; Cerebral extraction; Radiotracers; SPECT; Radionuclide study; Rat; Ligand; Rodentia; Radioactive tracers; Bioavailability; Experimental study; Photon; Vertebrata; Mammalia; Animal; First pass effect; Benzamide derivatives; Pharmacokinetics; Comparative study; Brain (vertebrata); Emission tomography
• ISSN: 0969-8051; 1872-9614
• DOI: 10.1016/S0969-8051(97)00199-6

Central dopaminergic receptors are widely studied for their importance in the pathophysiology of neurological and psychiatric diseases. We have investigated the cerebral delivery kinetics of three dopaminergic ligands in rats through the use of an indicator fractionation method to measure the tracer’s regional influx rate constant with respect to regional blood flow. The aim is to collect the in vivo kinetic parameters of the radioligand cerebral distribution, which are necessary if, dealing with SPECT and “trapped” tracers, one wishes to analyse data using a graphical approach.