Comparison of "selective" opiate receptor antagonists on the isolated mouse vas deferens.

The selectivity and relative potencies of opiate receptor antagonists were compared on the mouse vas deferens preparation. ICI-174864 was found to be a highly selective antagonist at delta opiate receptors equal in potency to naltrexone in blocking the actions of delta agonists. Although less potent than naltrexone, beta-funaltrexamine (beta-FNA) and Mr-1452, like naltrexone, were less selective in that they blocked the actions of mu, delta and kappa agonists. The relative potencies of beta-FNA and Mr-1452 in antagonizing the three types of agonists also were similar to naltrexone.