NESS-0327 See also References Navigation menu104356548611079X1BQI2J97IDTXSID00439851Interactive image(verify)10.1124/jpet.103.0499241266368910.1248/cpb.50.110910.1021/jm800077810.1016/j.ejphar.2005.09.05816271359eexpanding ite

AlkylamidesCaryophylleneCBCCBCVCBDCBDVCBGCBGMCBGVCBLCBDLCBNCBVEpigallocatechin gallateGallocatecholPerrottetineneSerinolamide ATHCTHC-C4THCATHCVYangonin8,11-DiOH-THC11-COOH-THC11-OH-THCA-40174A-41988A-42574Ajulemic acidAM-087AM-411AM-855AM-905AM-906AM-919AM-926AM-938AM-2389AM-4030AMG-1AMG-3AMG-36AMG-41Dexanabinol (HU-211)DMHPDronabinolHHCHU-210HU-243JWH-051JWH-133JWH-139JWH-161JWH-229JWH-359KM-233L-759,633L-759,656Levonantradol (CP 50,5561)MenabitanNabazenilNabidrox (Canbisol)NabiloneNabitanNaboctateO-224O-581O-774O-806O-823O-1057O-1125O-1191O-1238O-2048O-2113O-2365O-2372O-2373O-2383O-2426O-2484O-2545O-2694O-2715O-2716O-3223O-3226ParahexylPirnabineTHC-O-acetateTHC-O-phosphateCannabicyclohexanolCBD-DMHCP 47,497(C6)-CP 47,497(C9)-CP 47,497CP 55,244CP 55,940HU-308HU-320HU-331HU-336HU-345HU-446HU-465HU-910HUF-101NonabineO-1376O-1422O-1601O-1656O-1657O-1660O-1663O-1871SPA-229Tinabinol1-Butyl-3-(2-methoxybenzoyl)indole1-Butyl-3-(4-methoxybenzoyl)indole1-Pentyl-3-(2-methoxybenzoyl)indoleAM-630AM-679AM-694AM-1241AM-2233GW-405,833 (L-768,242)PravadolineRCS-4WIN 54,461AM-1220AM-1221AM-1235AM-2201AM-2232CHM-081EAM-2201FUB-JWH-018JWH-007JWH-015JWH-018JWH-019JWH-073JWH-081JWH-098JWH-116JWH-122JWH-149JWH-164JWH-182JWH-193JWH-198JWH-200JWH-210JWH-398JWH-424MAM-1220MAM-2201NE-CHMIMOTHJ-018THJ-2201WIN 55,212-2JWH-175JWH-176JWH-184JWH-185JWH-192JWH-194JWH-195JWH-196JWH-197JWH-199CannabipiperidiethanoneJWH-167JWH-203JWH-249JWH-250JWH-251JWH-302RCS-85F-ADBICA5F-NNE15F-PCN5F-SDB-006AB-FUBICAAB-PICAADBICAADB-FUBICAAPICACUMYL-BICACUMYL-PICACUMYL-5F-PICAFDU-NNE1MDMB-CHMICAMMB-2201MN-25NNE1PX-1Org 28312Org 28611SDB-006STS-1355F-PB-22FDU-PB-22FUB-PB-22QUCHIC (BB-22)QUPIC (PB-22)NM-22015Br-UR-1445Cl-UR-144A-796,260A-834,735FUB-144UR-144XLR-11XLR-125Cl-APINACA5F-ADB5F-ADB-PINACA5F-AMB5F-APINACA5F-CUMYL-PINACA5F-EMB-PINACAAB-CHMINACAAB-FUBINACAAB-FUBINACA 2-fluorobenzyl isomerAB-PINACAADB-CHMINACAADB-FUBINACAADB-PINACAAdamantyl-THPINACAADSB-FUB-187AMB-CHMINACAAMB-FUBINACAAPINACA (AKB48)APP-FUBINACACUMYL-4CN-BINACACUMYL-PINACACUMYL-THPINACAEMB-FUBINACAFUB-APINACAMDMB-FUBINACAMDMB-CHMINACAMN-18PX-2PX-3FAB-144JWH-030JWH-147JWH-307JWH-369JWH-370AM-883AM-1346ACEAACPAMethanandamide (AM-356)O-585O-689O-1812O-1860O-18615F-AB-FUPPYCAAB-CHFUPYCA4-HTMPIPO5F-PY-PICA5F-PY-PINACA5F-3-pyridinoylindoleA-836,339A-955,840Abnormal cannabidiolAB-001BzODZ-EPyrAM-1248AM-1714AZ-11713908BAY 38-7271BAY 59-3074BIM-018CB-13CB-86CBS-0550CUMYL-4CN-B7AICA5F-CUMYL-P7AICACUMYL-PEGACLONEFUBIMINAGSK-554,418AGW-842,166XJTE 7-31LASSBio-881LBP-1LeelamineMDA-7MDA-19MEPIRAPIMNESS-040C5NMP-7O-889O-1269O-1270O-1399O-1602O-2220OlorinabPF-03550096PSB-SB-1202PTI-1PTI-2QMPSBS-444,823SER-601TedalinabURB-447VSN-16WIN 56,0984-Nonylphenylboronic acidAM-404Arachidonoyl serotoninArvanilBIA 10-2474Biochanin ACAY-10401CAY-10429GenisteinGuineesineIDFPJNJ 1661010JNJ-42165279JZL184JZL195KaempferolLY-2183240MK-4409O-1624O-2093Oleoylethanolamide (OEA)OlvanilPalmitoylethanolamide (PEA)PF-04457845PF-622PF-750PF-3845PHOPURB-447URB-597URB-602URB-754VDM-11


CannabinoidsCB1 receptor antagonistsHydrazidesChloroarenesPyrazolesPiperazinesCannabinoid stubs


antagonistcannabinoid receptorCB1rimonabantKiinverse agonistneutral antagonist





















NESS-0327
NESS-0327.png
Legal status
Legal status


  • CA: Schedule II

Identifiers

PubChem CID
  • 10435654
ChemSpider

  • 8611079 ☒N
UNII
  • X1BQI2J97I

CompTox Dashboard (EPA)
  • DTXSID00439851 Edit this at Wikidata
Chemical and physical data
Formula
C24H23Cl3N4O
Molar mass489.824 g/mol g·mol−1
3D model (JSmol)
  • Interactive image

.mw-parser-output .noboldfont-weight:normal
 ☒N☑Y (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 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]



See also


  • Discovery and development of Cannabinoid Receptor 1 Antagonists

  • NESS-040C5


References




  1. ^ Ruiu, S; Pinna, GA; Marchese, G; Mussinu, JM; Saba, P; Tambaro, S; Casti, P; Vargiu, R; Pani, L (Jul 2003). "Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor". Journal of Pharmacology and Experimental Therapeutics. 306 (1): 363–70. doi:10.1124/jpet.103.049924. PMID 12663689..mw-parser-output cite.citationfont-style:inherit.mw-parser-output .citation qquotes:"""""""'""'".mw-parser-output .citation .cs1-lock-free abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/6/65/Lock-green.svg/9px-Lock-green.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .citation .cs1-lock-limited a,.mw-parser-output .citation .cs1-lock-registration abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/d/d6/Lock-gray-alt-2.svg/9px-Lock-gray-alt-2.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .citation .cs1-lock-subscription abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/a/aa/Lock-red-alt-2.svg/9px-Lock-red-alt-2.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registrationcolor:#555.mw-parser-output .cs1-subscription span,.mw-parser-output .cs1-registration spanborder-bottom:1px dotted;cursor:help.mw-parser-output .cs1-ws-icon abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/4/4c/Wikisource-logo.svg/12px-Wikisource-logo.svg.png")no-repeat;background-position:right .1em center.mw-parser-output code.cs1-codecolor:inherit;background:inherit;border:inherit;padding:inherit.mw-parser-output .cs1-hidden-errordisplay:none;font-size:100%.mw-parser-output .cs1-visible-errorfont-size:100%.mw-parser-output .cs1-maintdisplay:none;color:#33aa33;margin-left:0.3em.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration,.mw-parser-output .cs1-formatfont-size:95%.mw-parser-output .cs1-kern-left,.mw-parser-output .cs1-kern-wl-leftpadding-left:0.2em.mw-parser-output .cs1-kern-right,.mw-parser-output .cs1-kern-wl-rightpadding-right:0.2em


  2. ^ Stoit, A.R.; Lange, J.H.M.; den Hartog, A.P.; Ronken, E.; Tipker, K.; van Stuivenberg, H.H.; Dijksman, J.A.R.; Wals, H.C.; Kruse, C.G. (2002). "Design, Synthesis and Biological Activity of Rigid Cannabinoid CB1 Receptor Antagonists". Chem. Pharm. Bull. 50 (8): 1109–1113. doi:10.1248/cpb.50.1109.


  3. ^ Zhang, Y.; Burgess, J.P.; Brackeen, M.; Gilliam, A.; Mascarella, S.W.; Page, K.; Seltzman, H.H.; Thomas, B.F. (2008). "Conformationally Constrained Analogues of N -(Piperidinyl)-5-(4-Chlorophenyl)-1-(2,4- Dichlorophenyl)-4-Methyl-1 H -Pyrazole-3-Carboxamide (SR141716): Design, Synthesis, Computational Analysis, And Biological Evaluations". J. Med. Chem. 51 (12): 3526–3539. doi:10.1021/jm8000778.


  4. ^ Tambaro, S; Mongeau, R; Dessi, C; Pani, L; Ruiu, S (Nov 2005). "Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors". European Journal of Pharmacology. 525 (1–3): 150–3. doi:10.1016/j.ejphar.2005.09.058. PMID 16271359.









Cannabinoid stubs, Cannabinoids, CB1 receptor antagonists, Chloroarenes, Hydrazides, Piperazines, PyrazolesUncategorized
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