THE aim of this study was to quantitate imidazoline receptors in postm
ortem brains of heroin addicts who died of an opiate overdose. The den
sity of I-2-imidazoline receptors ([H-3]idazoxan binding in the presen
ce of adrenaline) and the immunoreactivity of the related 29/30 kDa im
idazoline receptor protein were decreased (39% and 28%, respectively)
in the frontal cortex. The density of brain I-2-imidazoline receptors
was also decreased in heroin-dependent rats (27%). This novel finding
indicates that opiate addiction induces down-regulation of I-2-imidazo
line receptors in astrocytes, and presumably down-regulation of the fu
nctions associated with these receptors.