Simple quantification of benzodiazepine receptor binding and ligand transport using iodine-123-iomazenil and two SPECT scans.
The feasibility of simplified procedures for the quantification of benzodiazepine receptor binding using [123I]iomazenil and SPECT was assessed.


METHODS
Six normal male volunteers were studied. Following intravenous injection of 111 MBq [123I]iomazenil, serial dynamic SPECT scanning was performed for 120 min and the concentration of lipophilic compounds in the arterial plasma was determined by chloroform extraction. Kinetic parameters were estimated by a curve-fitting procedure using the following four models: three-compartment, four-parameter (K1-k4) (3C4P), three-compartment, three-parameter (fixed K1/k2) (3C3P), three-compartment, two-parameter (fixed K1/k2 and k4) (3C2P) and two-compartment, two-parameter (K1 and k2) (2C2P). Kinetic parameters were also calculated by a table look-up procedure with 3C2P using only two SPECT data acquisitions. Parametric images were generated based on the same procedure.


RESULTS
In all models, the curve-fitting procedure gave similar outcomes for ligand transport (K1) and receptor density parameters (i.e., binding potential or distribution volume). The 3C4P parameters showed significant correlation between k2 and k3, while 3C3P did not show such a correlation, suggesting the stability of 3C3P. The 3C2P provided parameters essentially identical to those with the 3C3P, indicating the suitability of this model, while 2C2P gave similar distribution volume but obviously low K1.


CONCLUSIONS
Table look-up procedures based on the 3C2P model permit quantification of benzodiazepine receptor binding using [123I]iomazenil with two SPECT scans. This method may be of clinical value in the diagnosis of various diseases.
Onishi
Y
Y
Nihon Medi-Physics Co., Ltd., Hyogo, Japan.
Yonekura
Y
Y
Mukai
T
T
Nishizawa
S
S
Tanaka
F
F
Okazawa
H
H
Ishizu
K
K
Fujita
T
T
Shibasaki
H
H
Konishi
J
J
D000328:Adult; D001569:Benzodiazepines / Q000378:metabolism*; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005442:Flumazenil / Q000031:analogs & derivatives*; D006801:Humans; D007457:Iodine Radioisotopes; D008297:Male; D008875:Middle Aged; D011955:Receptors, Drug / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
D007457:Iodine Radioisotopes; D011955:Receptors, Drug; D001569:Benzodiazepines; D005442:Flumazenil; C063038:iomazenil