Benzomorphan interactions with acetylcholine receptor complexes from Torpedo.

Benzomorphan interactions with acetylcholine receptor complexes from Torpedo californica electric organ were investigated using radiolabelled probes. All of the benzomorphans had minimal affinity for the acetylcholine binding site. Four benzomorphans (N-allylnormetazocine, cyclazocine, phenazocine and pentazocine) inhibited the binding of tritiated perhydrohistrionicotoxin and phencyclidine to ion channel sites with IC50 values between 0.4 and 5 microM. Two other benzomorphans, ketazocine and ethylketocyclazocine, were much less active. Thus, ion channel affinity is not limited to benzomorphans which stimulate sigma-opiate receptors, and is not a certain indication of psychotomimetic potency.