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- Metkefamide 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.".
- Metkefamide atcPrefix "None".
- Metkefamide bioavailability "30.0".
- Metkefamide casNumber "66960-34-7".
- Metkefamide casSupplemental "66960-35-8 (acetate)".
- Metkefamide iupacName "(L)-tyrosyl-(D)-alanylglycyl-(L)-phenylalanyl-N2-methyl-(L)-methioninamide".
- Metkefamide pubchem "5464184".
- Metkefamide thumbnail Metkefamide.svg?width=300.
- Metkefamide wikiPageID "35641157".
- Metkefamide wikiPageRevisionID "599129515".
- Metkefamide atcPrefix "None".
- Metkefamide bioavailability "30".
- Metkefamide c "29".
- Metkefamide casNumber "66960".
- Metkefamide casSupplemental "66960".
- Metkefamide chemspiderid "4576570".
- Metkefamide eliminationHalfLife "3600.0".
- Metkefamide h "40".
- Metkefamide hasPhotoCollection Metkefamide.
- Metkefamide inchi "1".
- Metkefamide inchikey "FWDIKROEWJOQIQ-JMBSJVKXBF".
- Metkefamide iupacName "(L)-tyrosyl-(D)-alanylglycyl-(L)-phenylalanyl-N2-methyl-(L)-methioninamide".
- Metkefamide metabolism Liver.
- Metkefamide molecularWeight "600.73".
- Metkefamide n "6".
- Metkefamide o "6".
- Metkefamide proteinBound "44".
- Metkefamide pubchem "5464184".
- Metkefamide s "1".
- Metkefamide smiles "O=C[C@@H]CCSC".
- Metkefamide stdinchi "1".
- Metkefamide stdinchikey "FWDIKROEWJOQIQ-JMBSJVKXSA-N".
- Metkefamide subject Category:Amides.
- Metkefamide subject Category:Analgesics.
- Metkefamide subject Category:Opioid_peptides.
- Metkefamide type Abstraction100002137.
- Metkefamide type Amide114724264.
- Metkefamide type Amides.
- Metkefamide type Chemical114806838.
- Metkefamide type Compound114818238.
- Metkefamide type Material114580897.
- Metkefamide type Matter100020827.
- Metkefamide type OrganicCompound114727670.
- Metkefamide type Part113809207.
- Metkefamide type Peptide114743046.
- Metkefamide type Peptides.
- Metkefamide type PhysicalEntity100001930.
- Metkefamide type Relation100031921.
- Metkefamide type Substance100019613.
- Metkefamide type Drug.
- Metkefamide type FunctionalSubstance.
- Metkefamide 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.".
- Metkefamide label "Metkefamide".
- Metkefamide sameAs m.0jk_vqc.
- Metkefamide sameAs Q6824163.
- Metkefamide sameAs Q6824163.
- Metkefamide sameAs Metkefamide.
- Metkefamide wasDerivedFrom Metkefamide?oldid=599129515.
- Metkefamide depiction Metkefamide.svg.
- Metkefamide isPrimaryTopicOf Metkefamide.