THE OPIOID RECEPTOR-BINDING OF DEZOCINE, MORPHINE, FENTANYL, BUTORPHANOL AND NALBUPHINE

The ability of morphine, fentanyl, butorphanol, nalbuphine, and dezocine to compete with radiolabeled ligands for binding at the mu1, mu2, kappa1, and delta opioid receptors and the sigma receptor was characterized. In the absence of sodium, the potency of opioid receptor competition at each receptor site was found to be: mu1 - fentanyl > butorphanol > morphine greater-than-or-equal-to dezocine = nalbuphine; mu2 - butorphanol > fentanyl > nalbuphine > morphine = dezocine; kappa1 - butorphanol > nalbuphine > > morphine greater-than-or-equal-to dezocine > fentanyl; and delta - butorphanol > nalbuphine greater-than-or-equal-to dezocine > morphine > fentanyl. For all five compounds, competition at the sigma receptor was weak, with nalbuphine and dezocine having K(i)s of approximately 0.5 muM and the other opioids having K(i)s of greater than 1 muM. Since the presence of 100 mM NaCl during the competitive binding decreased the K(i), to varying degrees, of all five opioids at the mu1 and delta receptors and of some of the opioids at the mu2 and kappa1 receptors, the five compounds studied appear to differ in efficacy at the five receptor sites.