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Brain distribution of the opiate receptor antagonist, cyclofoxy (CF), was evaluated at equilibrium in rats. A combination of i.v. injection and constant i.v. infusion was used to administer CF over a wide dose range (2.4–450 nmol/rat). Kinetic simulations and experimental results showed that this administration schedule accomplishes “true” tissue-blood equilibrium of CF within 60 min. To estimate the receptor-ligand binding parameters, we assumed that the CF concentration at the receptor site is identical to that in plasma water at equilibrium, and can be calculated from measured blood data after corrections for radiolabeled metabolites and plasma protein binding. This assumption was supported by CSF and plasma water measurements at equilibrium. Regional K D , B max , and a nonspecific tissue binding equilibrium constant ( K eq ) were estimated by fitting the tissue and plasma water concentrations to a single receptor model; the estimated values were 1.4–2.9 n M, 15–74 pmol/g of tissue, and 5.2–8.0, respectively. They are in good agreement with previous in vitro measurements (Rothman and McLean, 1988) as well as in vivo estimates from i.v. injection experiments (Sawada et al., 1990 c). The conventional method to estimate the receptor-ligand binding parameters using data from cerebellum to approximate nonspecific tissue binding was found to be unacceptable. Although cerebellum is a brain region with no opiate receptors in rats, small differences in nonspecific tissue binding in different brain regions resulted in significant overestimations of K D  and B max  with this method. Receptor-active and -inactive enantiomers [[ 18 F](-)-CF and [ 3 H](+)-CF)] were simultaneously administered to the same animal and the receptor-bound CF concentration could be accurately measured; this method was used to estimate 5 max  from a single study in a single animal and has potential for direct application in human studies using positron emission tomography.

journal of cerebral blood flow and metabolism

Regional Brain Measurement of Bmax and KD with the Opiate Antagonist Cyclofoxy: Equilibrium Studies in the Conscious Rat