Rationally designed chimeric peptide of met-enkephalin and FMRFa-[D-Ala2, p-Cl-Phe4]YFa induce multiple opioid receptors mediated antinociception and up-regulate their expression

Vats, Ishwar Dutt; Chaudhary, Snehlata; Sharma, Ahuti; Nath, Mahendra; Pasha, Santosh

doi:10.1016/j.ejphar.2010.02.060

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Development Of Systemically Active Opioid Peptides1

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“…D-Ala 2 and/or Phe( p -Cl) 4 incorporated into YFa to enhance metabolic stability and improve BBB penetration, resulted in enhanced analgesic potency following i.p. administration (see Table 2), but altered the opioid receptor selectivity [21, 22]. Like the parent peptide, these analogs did not produce antinociceptive tolerance.…”

Section: Development Of Systemically Active Opioid Peptidesmentioning

confidence: 99%

Opioid peptides: potential for drug development

Aldrich

McLaughlin

2012

Drug Discovery Today: Technologies

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Opioid receptors are important targets for the treatment of pain and potentially for other disease states (e.g. mood disorders and drug abuse) as well. Significant recent advances have been made in identifying opioid peptide analogs that exhibit promising in vivo activity for treatment of these maladies. This review focuses on the development and evaluation of opioid peptide analogs demonstrating activity after systemic administration, and recent clinical evaluations of opioid peptides for possible therapeutic use.

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Section: Development Of Systemically Active Opioid Peptidesmentioning

confidence: 99%