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Mu-opioid receptor agonists
Picenadol
Другие языки:

    Picenadol

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    Picenadol
    Picenadol.svg
    Clinical data
    ATC code
    • none
    Identifiers
    • 3-(1,3-dimethyl-4-propylpiperidin-4-yl)phenol
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    Chemical and physical data
    Formula C16H25NO
    Molar mass 247.382 g·mol−1
    3D model (JSmol)
    • OC1=CC=CC([C@@]2(CCN(C[C@@H]2C)C)CCC)=C1
    • InChI=1S/C16H25NO/c1-4-8-16(9-10-17(3)12-13(16)2)14-6-5-7-15(18)11-14/h5-7,11,13,18H,4,8-10,12H2,1-3H3/t13-,16-/m0/s1 checkY
    • Key:RTOHPIRUUAKHOZ-BBRMVZONSA-N checkY
      (verify)

    Picenadol (LY-97435) is a 4-phenylpiperidine derivative that is an opioid analgesic drug developed by Eli Lilly in the 1970s.

    Picenadol is an effective analgesic with similar efficacy to pethidine (meperidine). It has been investigated for some applications such as obstetrics and dentistry, but never commercialised.

    It is unusual in that one enantiomer is a pure μ-opioid agonist, while the other is an antagonist. The (3R,4R) isomer is the agonist, while (3S,4S) is antagonist. This means that the racemic mix of the two enantiomers is a mixed agonist-antagonist, with relatively low abuse potential, and little of the κ-opioid activity that tends to cause problems with other opioid mixed agonist-antagonists such as pentazocine.

    Synthesis

    Picenadol synthesis 1:
    Picenadol synthesis 2:

    See also




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