Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.

ABSTRACT: Cholecystokinin (CCK) has been identified as a pronociceptive endogenous peptide which also possesses antiopioid actions. CCK may be upregulated in conditions of chronic pain or during sustained morphine administration resulting in attenuation of opioid-mediated pain relief. These complex interactions between opioids and endogenous CCK receptor systems have suggested the need for a new paradigm in drug design for some states of chronic pain. In these circumstances the rational design of potential drugs for the treatment of these conditions must be based on one ligand for multiple targets. We have designed a single peptide which can interact with delta and mu opioid receptors as agonists and with CCK receptors as antagonists. The ligands were designed based on a model of overlapping pharmac

SUBMITTER: Agnes RS 

PROVIDER: S-EPMC1484468 | biostudies-literature | 2006 May

REPOSITORIES: biostudies-literature