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In vivo benzodiazepine receptor equilibrium dissociation constant, K D , and maximum number of binding sites, B max , were measured by single photon emission computerized tomography (SPECT) in three baboons. Animals were injected with a bolus followed by a constant i.v. infusion of the high affinity benzodiazepine ligand [ 123 I]iomazenil. Plasma steady-state concentration and receptor–ligand equilibrium were reached within 2 and 3 h, respectively, and were sustained for the duration (4–9 h) of the experiments (n = 15). At the end of the experiments, a receptor saturating dose of flumazenil (0.2 mg/kg) was injected to measure nondisplaceable activity. Experiments were carried out at various levels of specific activity, and Scatchard analysis was performed for derivation of the K D  (0.59 ± 0.09 n M) and B max  (from 126 n M in the occipital region to 68 n M in the striatum). Two animals were killed and [ 125 I]iomazenil B max  and K D  were measured at 22 and 37°C on occipital homogenate membranes. In vitro values of B max  (114 ± 33 n M) and 37°C K D  (0.66 ± 0.16 n M) were in good agreement with in vivo values measured by SPECT. This study demonstrates that SPECT can be used to quantify central neuroreceptors density and affinity.

journal of cerebral blood flow and metabolism

SPECT Quantification of [<sup>123</sup>I]Iomazenil Binding to Benzodiazepine Receptors in Nonhuman Primates: II. Equilibrium Analysis of Constant Infusion Experiments and Correlation with in vitro Parameters

SPECT Quantification of [123I]Iomazenil Binding to Benzodiazepine Receptors in Nonhuman Primates: II. Equilibrium Analysis of Constant Infusion Experiments and Correlation with in vitro Parameters

SPECT Quantification of [¹²³I]Iomazenil Binding to Benzodiazepine Receptors in Nonhuman Primates: II. Equilibrium Analysis of Constant Infusion Experiments and Correlation with in vitro Parameters