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Structure-NCS activity studies with the enkephalins

1980; Elsevier BV; Volume: 10; Issue: 3 Linguagem: Inglês

10.1016/0163-7258(80)90032-7

1879-016X

David H. Coy, Abba J. Kastin,

Chemical Synthesis and Analysis

Numerous analogues of the enkephalin pentapeptides have been synthesized and comprehensive structure-activity relationships have been established. Analogues which are considerably more potent analgesics than the natural peptides are common; however, all thus far appear to have addictive properties. The problem of designing peptides which are able to cross the blood-brain barrier has been readily overcome since several analogues have been reported to be more active than morphine after peripheral injection. The existence of multiple opiate receptors is also being exploited in the design of peptides with more specific binding properties. This could result in the development of analgesic analogues with fewer adverse side-effect and peptides with enhanced non-morphinoid activities, such as anti-depressant and anti-schizophrenic effects.