Opioid peptides and their receptors

The three agonists, methionine-enkephalin, leucine-enkephalin and beta-endorphin have different pharmacological patterns. It may be of particular importance that they vary in their relative affinities to the enkephalin and naltrexone binding sites in the brain; the former are probably related to delta-receptors prevalent in the mouse vas deferens and the later to mu-receptors prevalent in the guinea-pig. It is possible that mu-receptors are more important for the mediation of analgesic effects than delta-receptors. An understanding of the pharmacokinetics of the opioid peptides will be of basic importance for the design of enkephalin analogues suitable for use as analgesics in man.