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- Q6824163 subject Q16813793.
- Q6824163 subject Q7145142.
- Q6824163 subject Q8248726.
- Q6824163 abstract "Metkefamide (INN; LY-127,623), or metkephamid acetate (USAN), but most frequently referred to simply as metkephamid, is a synthetic opioid pentapeptide and derivative of [Met]enkephalin with the amino acid sequence Tyr-D-Ala-Gly-Phe-(N-Me)-Met-NH2. It behaves as a potent agonist of the δ- and μ-opioid receptors with roughly equipotent affinity, and also has similarly high affinity as well as subtype-selectivity for the κ3-opioid receptor.Despite its peptidic nature, upon systemic administration, metkefamide rapidly penetrates the blood-brain-barrier and disperses into the central nervous system where it produces potent, centrally-mediated analgesic effects, of which have been shown to be dependent on activity at both the μ- and δ-opioid receptors. In addition, on account of modifications to the N- and C-terminals, metkefamide is highly stable against proteolytic degradation relative to many other opioid peptides. As an example, while its parent peptide, [Met]enkephalin, has an in vivo half-life of merely seconds, metkefamide has a half-life of nearly 60 minutes, and upon intramuscular administration, has been shown to provide pain relief that lasts for hours.Likely on account of its δ-opioid activity, clinical trials have found metkefamide to possess less of a tendency for producing many of the undesirable side effects usually associated with conventional opioids such as respiratory depression, tolerance, and physical dependence. However, it has been shown to cause some additional side effects that are considered unusual for standard opioid analgesics like sensations of heaviness in the extremities and nasal congestion—though these were not considered to be particularly distressing—and it has also been shown to raise the seizure threshold in animals. In any case, clinical development was not further pursued after phase I clinical studies and metkefamide never reached the pharmaceutical market.".
- Q6824163 atcPrefix "None".
- Q6824163 bioavailability "30.0".
- Q6824163 casNumber "66960-34-7".
- Q6824163 casSupplemental "66960-35-8 (acetate)".
- Q6824163 iupacName "(L)-tyrosyl-(D)-alanylglycyl-(L)-phenylalanyl-N2-methyl-(L)-methioninamide".
- Q6824163 pubchem "5464184".
- Q6824163 thumbnail Metkefamide.svg?width=300.
- Q6824163 wikiPageWikiLink Q1425425.
- Q6824163 wikiPageWikiLink Q14897645.
- Q6824163 wikiPageWikiLink Q14911924.
- Q6824163 wikiPageWikiLink Q1641494.
- Q6824163 wikiPageWikiLink Q16813793.
- Q6824163 wikiPageWikiLink Q172847.
- Q6824163 wikiPageWikiLink Q173235.
- Q6824163 wikiPageWikiLink Q174211.
- Q6824163 wikiPageWikiLink Q18030283.
- Q6824163 wikiPageWikiLink Q1960495.
- Q6824163 wikiPageWikiLink Q2066956.
- Q6824163 wikiPageWikiLink Q212527.
- Q6824163 wikiPageWikiLink Q221694.
- Q6824163 wikiPageWikiLink Q2622112.
- Q6824163 wikiPageWikiLink Q284398.
- Q6824163 wikiPageWikiLink Q30612.
- Q6824163 wikiPageWikiLink Q310425.
- Q6824163 wikiPageWikiLink Q3160831.
- Q6824163 wikiPageWikiLink Q3245488.
- Q6824163 wikiPageWikiLink Q3269441.
- Q6824163 wikiPageWikiLink Q33123.
- Q6824163 wikiPageWikiLink Q389934.
- Q6824163 wikiPageWikiLink Q417189.
- Q6824163 wikiPageWikiLink Q425105.
- Q6824163 wikiPageWikiLink Q432083.
- Q6824163 wikiPageWikiLink Q47270.
- Q6824163 wikiPageWikiLink Q47273.
- Q6824163 wikiPageWikiLink Q4926095.
- Q6824163 wikiPageWikiLink Q5477806.
- Q6824163 wikiPageWikiLink Q621261.
- Q6824163 wikiPageWikiLink Q7145142.
- Q6824163 wikiPageWikiLink Q7180990.
- Q6824163 wikiPageWikiLink Q7447053.
- Q6824163 wikiPageWikiLink Q7663812.
- Q6824163 wikiPageWikiLink Q824258.
- Q6824163 wikiPageWikiLink Q8248726.
- Q6824163 wikiPageWikiLink Q899107.
- Q6824163 wikiPageWikiLink Q9368.
- Q6824163 atcPrefix "None".
- Q6824163 bioavailability "30".
- Q6824163 casNumber "66960".
- Q6824163 casSupplemental "66960".
- Q6824163 iupacName "(L)-tyrosyl-(D)-alanylglycyl-(L)-phenylalanyl-N2-methyl-(L)-methioninamide".
- Q6824163 pubchem "5464184".
- Q6824163 type ChemicalSubstance.
- Q6824163 type Drug.
- Q6824163 type ChemicalObject.
- Q6824163 type Thing.
- Q6824163 type Q8386.
- Q6824163 comment "Metkefamide (INN; LY-127,623), or metkephamid acetate (USAN), but most frequently referred to simply as metkephamid, is a synthetic opioid pentapeptide and derivative of [Met]enkephalin with the amino acid sequence Tyr-D-Ala-Gly-Phe-(N-Me)-Met-NH2.".
- Q6824163 label "Metkefamide".
- Q6824163 depiction Metkefamide.svg.