NESS-0327

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NESS-0327
JSmol)
  • Clc3cc(Cl)ccc3-n4c2-c1ccc(Cl)cc1CCCc2c(n4)C(=O)NN5CCCCC5
  • InChI=1S/C24H23Cl3N4O/c25-16-7-9-18-15(13-16)5-4-6-19-22(24(32)29-30-11-2-1-3-12-30)28-31(23(18)19)21-10-8-17(26)14-20(21)27/h7-10,13-14H,1-6,11-12H2,(H,29,32) ☒N
  • Key:NCXBPZJQQSNIRA-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

NESS-0327 is a drug used in scientific research which acts as an extremely potent and selective

antagonist of the cannabinoid receptor CB1. It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e. 0.00035nM) and a selectivity of over 60,000x for CB1 over CB2.[1]
Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM[2] and 18.4nM[3]). Also unlike rimonabant, NESS-0327 does not appear to act as an
neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.[4]

See also

References

  1. S2CID 32018707
    .
  2. PMID 12192147
    .
  3. PMID 18512901
    .
  4. PMID 16271359
    .
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