title: Pharmacokinetic analysis of benzodiazepine receptor binding of [123I]iomazenil in human brain.
abstract: OBJECTIVE
  The purpose of this study is to evaluate the central benzodiazepine (BZP) receptor binding of iomazenil (IMZ) by pharmacokinetic analysis and to establish a methodology for the diagnosis of CNS disorders with abnormalities in BZP receptor binding.
  
  
  METHODS
  BZP receptor binding of IMZ was analyzed kinetically using plasma concentration-time profiles and dynamic single photon emission computed tomography (SPECT) data obtained after the intravenous administration of IMZ to patients with neuropsychiatric disease. The analysis was based on a 3-compartmental model including the processes of both blood-brain barrier (BBB) transport and BZP receptor binding.
  
  
  RESULTS
  Hydrolized metabolite of IMZ was detected in plasma, indicating the need for separation by HPLC. The BBB influx clearance and the receptor binding potential of IMZ in the medial temporal region was reduced in the epileptic patient.
  
  
  CONCLUSIONS
  Our findings suggest the possibility of detecting the epileptic focus by using our method.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Ito
authors.forename: T
authors.initials: T
authors.lastname: Momose
authors.forename: H
authors.initials: H
authors.lastname: Kotaki
authors.forename: Y
authors.initials: Y
authors.lastname: Kojima
authors.forename: K
authors.initials: K
authors.lastname: Yamamoto
authors.forename: M
authors.initials: M
authors.lastname: Katashima
authors.forename: Y
authors.initials: Y
authors.lastname: Sawada
authors.forename: Y
authors.initials: Y
authors.lastname: Sasaki
authors.forename: T
authors.initials: T
authors.lastname: Iga
mesh_terms: D001812:Blood-Brain Barrier; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D001927:Brain Diseases / Q000000981:diagnostic imaging / Q000378:metabolism*; D005442:Flumazenil / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D006801:Humans; D007275:Injections, Intravenous; D007457:Iodine Radioisotopes; D011963:Receptors, GABA-A / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D007457:Iodine Radioisotopes; D011963:Receptors, GABA-A; D005442:Flumazenil; C063038:iomazenil