Up-regulation of [3H]DAMGO and [3H]DTLET opioid binding sites in laminae I-II of the spinal cord in intact and deafferented morphine-tolerant rats.

Using quantitative autoradiography and selective opioid ligands, we have measured the effects of morphine-induced tolerance on [3H]DAMGO and [3H]DTLET binding sites in the superficial spinal dorsal horn (laminae I-II) of intact and deafferented rats (unilateral C4-T2 dorsal rhizotomy). In intact rats, the treatment induced an up-regulation of 26% and 39% for [3H]DAMGO and [3H]DTLET binding sites, respectively, without modification of receptor affinity. In deafferented rats, the treatment similarly induced an up-regulation of 31% and 29% for [3H]DAMGO and [3H]DTLET binding sites, respectively, on the contralateral side, and of 21% and 25%, respectively, on the ipsilateral side. These data demonstrate that the up-regulation induced by morphine tolerance is of similar magnitude for both presynaptic (on primary afferent fibers) and postsynaptic (on spinal neurons) opioid binding sites in the rat dorsal horn.