(+)-[3H]SKF 10,047, (+)-[3H]ethylketocyclazocine, mu, kappa, delta and phencyclidine binding sites in guinea pig brain membranes.

Binding of the opiates (+)-[3H]SKF 10,047 [N-allylnormetazocine; (+)-[3H]SKF] and (+)-[3H]ethylketocyclazocine [(+)-[3H]EKC] were compared to mu, kappa and delta and phencyclidine (PCP) receptor binding in guinea pig brain membranes. (+)-[3H]SKF and (+)-[3H]EKC binding were not blocked by naloxone, and had different drug selectivity compared to mu, kappa and delta binding sites. The number of binding sites, drug selectivity and region distribution in brain were similar for (+)-[3H]SKF and (+)-[3H]EKC. Sigma opiates that are associated with psychotomimetic activities, such as pentazocine, cyclazocine, SKF 10,047 and bremazocine, were potent inhibitors of (+)-[3H]SKF and (+)-[3H]EKC binding. Haloperidol was the most potent inhibitor of (+)-[3H]SKF binding. Haloperidol and sigma opiates demonstrated biphasic displacement of [3H]PCP binding, suggesting that [3H]PCP labelled two sites. PCP had a similar affinity for both (+)-[3H]SKF and [3H]PCP binding sites in the presence of 100 mM NaCl. The highest concentrations of (+)-[3H]SKF and (+)-[3H]EKC bindings sites were in the hypothalamus, anterior pituitary, midbrain, pons and medulla.