NESS-0327

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 K_i 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 inverse agonist at higher doses, instead being a purely neutral antagonist which blocks the CB₁ receptor but does not produce any physiological effect of its own.^[4]

CAS Number

• 494844-07-4

PubChem CID

• 10435654

ChemSpider

• 8611079 ^N

UNII

• X1BQI2J97I

Quick facts Identifiers, CAS Number ...

NESS-0327

Identifiers
CAS Number	494844-07-4
PubChem CID	10435654
ChemSpider	8611079 N
UNII	X1BQI2J97I
CompTox Dashboard (EPA)	DTXSID00439851
Chemical and physical data
Formula	C24H23Cl3N4O
Molar mass	489.83 g·mol−1
3D model (JSmol)	Interactive image
SMILES Clc3cc(Cl)ccc3-n4c2-c1ccc(Cl)cc1CCCc2c(n4)C(=O)NN5CCCCC5
InChI 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
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