The present study demonstrates the application of fMRI technology to neurop
harmacology and the interaction of drug/receptor in the rat brain. Specific
ally, we have observed two different types of fMRI signal changes induced b
y acute i.v. heroin administration in rat brains under conditions of sponta
neous and artificial respiration. Under spontaneous respiration, a global d
ecrease in fMRI signal was observed; under artificial respiration, a region
-specific increase in fMRI signal was identified and the activation sites a
re consistent with the distribution of opiate mu-receptors in rat brain as
previously reported by autoradiography. Both heroin-induced fMRI signal cha
nges were suppressed by pretreatment of naloxone, an opiate mu-receptor ant
agonist, and reversed by injection of naloxone following heroin infusion. T
hese results suggest that fMRI has specific advantages in spatial and tempo
ral resolution for studies of neuropharmacology and drugs of abuse. NeuroRe
port 11:1085-1092 (C) 2000 Lippincott Williams & Wilkins.