Document Detail


Enkephalinase inhibitors: potential agents for the management of pain.
MedLine Citation:
PMID:  18855623     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Management of acute and chronic pain has always been a key area of clinical research. Enkephalinase inhibitors (EIs) seem to be promising as therapeutic agents having antinociceptive action. They additionally possess anticraving, antidiarrhoeal and antidepressant actions. The antinociceptive action of EIs has been reported for over a decade however, their therapeutic potential is yet to be effectively explored. EIs may be broadly classified as endogenous and those that are obtained synthetically. Endogenous EIs include peptides like spinorphin and opiorphin. And compounds like RB 101, RB 120, RB 3007 constitute the synthetically obtained EIs. Endogenous and synthetic inhibitors enkephalin degrading enzymes have been studied in vivo using standard animal models. The potential EI targets appear to be APN (Aminopeptidase N), NEP (Neutral endopeptidase), DPP-III (Dipeptidyl peptidase). EIs possess the advantage that they lack the opioid side effects. This article reviews the mechanisms by which EIs act and elucidates the pathways involved.
Authors:
V Thanawala; V J Kadam; R Ghosh
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current drug targets     Volume:  9     ISSN:  1873-5592     ISO Abbreviation:  Curr Drug Targets     Publication Date:  2008 Oct 
Date Detail:
Created Date:  2008-10-15     Completed Date:  2009-05-22     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100960531     Medline TA:  Curr Drug Targets     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  887-94     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Bharati Vidyapeeth's College of Pharmacy, Sector 8, CBD Belapur, Navi Mumbai, Maharashtra, India.
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MeSH Terms
Descriptor/Qualifier:
Animals
Disease Management
Drug Delivery Systems / methods
Humans
Neprilysin / antagonists & inhibitors*,  metabolism
Pain / drug therapy*,  enzymology*
Pain Measurement / drug effects,  methods
Protease Inhibitors / administration & dosage*
Chemical
Reg. No./Substance:
0/Protease Inhibitors; EC 3.4.24.11/Neprilysin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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