Inhibitors of enkephalin-degrading
enzymes as potential therapeutic agents

by
Patel A, Smith HJ, Sewell RD
Welsh School of Pharmacy,
University of Wales, Cardiff, U.K.
Prog Med Chem 1993; 30:327-78


ABSTRACT

A limited number of enzymes such as membrane metalloendopeptidase (enkephalinase) and angiotensin converting enzyme appear to be involved in deactivation and modulation of circulatory regulatory peptides. Peptides such as the enkephalins are also involved in a large number of physiological processes. This multiplicity of physiological roles has made it difficult to establish the therapeutic role of enkephalin-degrading enzyme inhibitors. Other factors such as difficulty in quantification and thus measurement of processes involved in pain and mental illness have also hindered the process of establishing any therapeutic role of enkephalin-degrading enzyme inhibitors in these conditions. However, they have proved to be useful pharmacological 'tools'. The most likely therapeutic role at present appears to be in the treatment of cardiovascular disorders. As a 'profile' of pharmacological actions of enkephalin-degrading enzymes emerges, it is becoming apparent that bioavailability rather than a high degree of specificity or inhibitory potency may be the most important factor. This may be used to an advantage in future developments by the use of less specific or combined inhibitors in the form of prodrugs, designed to be active at specific sites such as the central nervous system.
Opioids
Morphine
Cannabis
Tramadol
Gabapentin
Fibromyalgia
Hyperalgesia
Delta agonists
Buprenorphine
Enkephalinase
Antidepressants
Opioids for depression?
Imipramine and enkephalin
Enkephalinase inhibitor RB101
Nociceptin receptor antagonists
Depression, opioids and the HPA
Substance P antagonists as antidepressants


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