Metkefamide

Source: Wikipedia, the free encyclopedia.
Metkefamide
Hepatic[1]
Elimination half-life~60 minutes[3]
Identifiers
  • L-tyrosyl-D-alanylglycyl-L-phenylalanyl-N2-methyl-L-methioninamide
JSmol)
  • O=C(N)[C@@H](N(C(=O)[C@@H](NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C)Cc2ccccc2)C)CCSC
  • InChI=1S/C29H40N6O6S/c1-18(33-28(40)22(30)15-20-9-11-21(36)12-10-20)27(39)32-17-25(37)34-23(16-19-7-5-4-6-8-19)29(41)35(2)24(26(31)38)13-14-42-3/h4-12,18,22-24,36H,13-17,30H2,1-3H3,(H2,31,38)(H,32,39)(H,33,40)(H,34,37)/t18-,22+,23+,24+/m1/s1
  • Key:FWDIKROEWJOQIQ-JMBSJVKXSA-N

Metkefamide (

κ3-opioid receptor.[7][8]

Despite its

pain relief that lasts for hours.[3]

Likely on account of its δ-opioid activity,

sensations of heaviness in the extremities and nasal congestion—though these were not considered to be particularly distressing[9]—and it has also been shown to raise the seizure threshold in animals.[13] In any case, clinical development was not further pursued after phase I clinical studies and metkefamide never reached the pharmaceutical market.[14][15][16]

See also

References

  1. ^
    ISBN 978-0-85404-227-2
    . Retrieved 27 April 2012.
  2. ISBN 978-3-527-32994-6
    . Retrieved 27 April 2012.
  3. ^
    ISBN 978-0-8247-7896-5
    . Retrieved 27 April 2012.
  4. ISBN 978-0-7514-0499-9
    . Retrieved 27 April 2012.
  5. S2CID 3872497
    .
  6. ^
    PMID 6256856
    .
  7. ISBN 978-0-89603-306-1
    . Retrieved 27 April 2012.
  8. PMID 2553920
    .
  9. ^
    S2CID 9618418
    .
  10. PMID 6292609
    .
  11. ISBN 978-0-8247-1995-1
    . Retrieved 27 April 2012.
  12. ISBN 978-0-8247-8346-4
    . Retrieved 27 April 2012.
  13. PMID 6319916
    .
  14. ISBN 978-0-12-040522-0
    . Retrieved 27 April 2012.
  15. ISBN 978-0-7881-8196-2
    . Retrieved 27 April 2012.
  16. ISBN 978-0-412-46630-4
    . Retrieved 26 April 2012.
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