[Changes in alpha 2-adrenoceptor binding nature in guinea-pig brain following the development of morphine dependence]

We examined the effect of morphine dependence on alpha 2-adrenoceptors in guinea-pig brain. We also studied the influence of clonidine on the naloxone-induced withdrawal signs. 1. Guinea-pigs were implanted subcutaneously with MS contin (300 mg.kg-1). Two days after implantation, the binding of 3H-UK14304 (alpha 2 selective ligand) to brain membranes prepared from morphine dependent and control animals was determined. Scatchard plot of the saturation binding data revealed an increase in Bmax values and no change in the Kd values from dependent animals. These results indicate that brain alpha 2-adrenoceptors are up-regulated in morphine dependent guinea pigs. 2. Subcutaneous injection of naloxone on the 2 nd day after implantation caused characteristic withdrawal symptoms. Clonidine has been shown to reduce some opiate withdrawal signs in morphine-dependent animals.