SR-144,528

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SR-144,528
Clinical data
ATC code
  • none
Identifiers
  • 5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl]-1H-pyrazole-3-carboxamide
JSmol)
  • CC1=CC=C(C=C1)CN2C(=CC(=N2)C(=O)N[C@H]3[C@]4(CC[C@H](C4)C3(C)C)C)C5=CC(=C(C=C5)Cl)C
  • InChI=1S/C29H34ClN3O/c1-18-6-8-20(9-7-18)17-33-25(21-10-11-23(30)19(2)14-21)15-24(32-33)26(34)31-27-28(3,4)22-12-13-29(27,5)16-22/h6-11,14-15,22,27H,12-13,16-17H2,1-5H3,(H,31,34)/t22-,27-,29+/m1/s1 ☒N
  • Key:SUGVYNSRNKFXQM-XRHWURSXSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

SR144528 is a drug that acts as a potent and highly selective

CB2 receptor inverse agonist, with a Ki of 0.6 nM at CB2 and 400 nM at the related CB1 receptor.[1][2] It is used in scientific research for investigating the function of the CB2 receptor,[3][4][5][6] as well as for studying the effects of CB1 receptors in isolation, as few CB1 agonists that do not also show significant activity as CB2 agonists are available.[7][8][9] It has also been found to be an inhibitor of sterol O-acyltransferase, an effect that appears to be independent from its action on CB2 receptors.[10]

See also

References

  1. PMID 9454810
    .
  2. PMID 9918562
    .
  3. PMID 10915832
    .
  4. S2CID 6447695
    .
  5. S2CID 22671432
    .
  6. PMID 32259074
    .
  7. PMID 10720647
    .
  8. S2CID 2655432
    .
  9. S2CID 10520671
    .
  10. PMID 19338772
    .
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