The invention is based on the discovery that nonselective γ-agonists that possess µ receptor-mediated effects in addition to their γ-agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective γ-agonists. The invention includes a number of new compounds having both nonselective γ opioid receptor agonist activity and additional activity at µ opioid receptors.
These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging. The new compounds have relatively low affinity for the δ opioid receptor, and, thus, do not interact significantly with the delta receptor or produce side effects associated with activity at the δ receptor.
URV Reference Number: 6-1072