Cyclic Opioid Peptides.

摘要: For decades the opioid receptors have been an attractive therapeutic target for treatment of pain. Since first discovery enkephalin, approximately a dozen endogenous peptides known to produce activity and analgesia, but their therapeutics limited mainly due low blood brain barrier penetration poor resistance proteolytic degradation. One versatile approach overcome these drawbacks is cyclization linear cyclic with constrained topographical structure. Compared parents, analogs exhibit better metabolic stability, lower offtarget toxicity, improved bioavailability. Extensive structure-activity relationship studies uncovered promising compounds pain as well further elucidate structural elements required selective receptor activity. The benefits that come employing can be enhanced through generation polycyclic derivatives. Opioid ligands generally short peptide chain thus realm has yet explored. In this review, brief history designing receptors, including classic ligands, discussed along recent approaches successes receptors. Various scaffolds improve bioavailability are elaborated concluded discourse towards peptides.