Substitution and antagonism in rats trained to discriminate (+)-N-allylnormetazocine from saline.
Journal of Pharmacology and Experimental Therapeutics June 1, 1989 R. Balster
The drug (+)-N-Allylnormetazocine (NANM) binds to two sites in the mammalian brain: a high-affinity site sensitive to haloperidol and a lower-affinity site known as the phencyclidine (PCP) receptor. In rats trained to distinguish (+)-NANM from saline, drugs that bind strongly to the haloperidol-sensitive site did not produce (+)-NANM-like effects, and only haloperidol partially blocked the drug's effects, and only at doses that disrupted behavior. In contrast, PCP-like drugs from various chemical classes fully substituted for (+)-NANM, with their potency matching their affinity for the PCP receptor. The findings indicate that the PCP receptor, not the haloperidol-sensitive site, mediates the discriminative stimulus properties of (+)-NANM.