Bioavailability of Endomorphins and the Blood-brain Barrier- A Review

Author(s): Renata Perlikowska, Anna Janecka

Journal Name: Medicinal Chemistry

Volume 10 , Issue 1 , 2014

Become EABM
Become Reviewer
Call for Editor


Opioid peptides have the potential to be pharmaceutical agents for the treatment of pain because they modulate nociceptive pathways at supraspinal, spinal and peripheral levels. Unfortunately, peptides are generally hydrophilic compounds and therefore unable to cross the blood-brain barrier (BBB) by passive diffusion to reach the central nervous system (CNS) in an amount sufficient to activate appropriate receptors. Endomorphins (EMs) belong to the class of endogenous opioids eliciting the strongest analgesic effect, but only after direct administration to the CNS. Extensive research is in progress to better understand the relationships between EM structure and bioavailability. This article deals with the recent investigations that allow the design of stable and neuroactive EM analogs with enhanced brain passage and uptake.

Keywords: Opioid peptides, opioid receptors, analgesia, bioavailability, passive diffusion, peptide permeability.

open access plus

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2014
Published on: 26 December, 2013
Page: [2 - 17]
Pages: 16
DOI: 10.2174/15734064113099990040

Article Metrics

PDF: 73