关键词：镇痛药；伤亡；内啡肽；医疗服务
摘 要：Endogenous opiate peptides (enkephalins and endorphins) are more potent and specific than morphine and congeners. Specificity is determined by the 'address segment' while binding is determined by the 'message segment.' Incorporation of carbohydrates into the address segment results in improved biodistribution and enhanced penetration of the blood-brain barrier (BBB). Thus, glycosylation of mu- or delta-selective peptides allows the resulting glycopeptides to be used as potent and safer alternatives to classical opiates such as morphine. Morphine and other muselective agonists are immunosuppressants, while the glycopeptide enkephalins are selective delta- agonists, which are known to be immunostimulants. Hypothesis: Enkephalin transport and penetration of the blood-brain barrier can be determined by reversible binding to membranes, which may be manipulated by altering the amphipathicity of the address segment directly by introduction of hydrophilic sugar moieties, and lipophilic side chains. Conclusion: Glycopeptide analogues of enkephalins are viable drug candidates. Obstacles regarding the synthesis and design of analgesics have been overcome. Further studies are required in order to meet FDA requirements. See attached .pdf file (14 pg and 22 pg reviews) for details.