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
-

Popular posts from this blog

Mobil Contents History Mobil brands Former Mobil brands Lukoil transaction Mobil UK Mobil Australia Mobil New Zealand Mobil Greece Mobil in Japan Mobil in Canada Mobil Egypt See also References External links Navigation menuwww.mobil.com"Mobil Corporation"the original"Our Houston campus""Business & Finance: Socony-Vacuum Corp.""Popular Mechanics""Lubrite Technologies""Exxon Mobil campus 'clearly happening'""Toledo Blade - Google News Archive Search""The Lion and the Moose - How 2 Executives Pulled off the Biggest Merger Ever""ExxonMobil Press Release""Lubricants""Archived copy"the original"Mobil 1™ and Mobil Super™ motor oil and synthetic motor oil - Mobil™ Motor Oils""Mobil Delvac""Mobil Industrial website""The State of Competition in Gasoline Marketing: The Effects of Refiner Operations at Retail""Mobil Travel Guide to become Forbes Travel Guide""Hotel Rankings: Forbes Merges with Mobil"the original"Jamieson oil industry history""Mobil news""Caltex pumps for control""Watchdog blocks Caltex bid""Exxon Mobil sells service station network""Mobil Oil New Zealand Limited is New Zealand's oldest oil company, with predecessor companies having first established a presence in the country in 1896""ExxonMobil subsidiaries have a business history in New Zealand stretching back more than 120 years. We are involved in petroleum refining and distribution and the marketing of fuels, lubricants and chemical products""Archived copy"the original"Exxon Mobil to Sell Its Japanese Arm for $3.9 Billion""Gas station merger will end Esso and Mobil's long run in Japan""Esso moves to affiliate itself with PC Optimum, no longer Aeroplan, in loyalty point switch""Mobil brand of gas stations to launch in Canada after deal for 213 Loblaws-owned locations""Mobil Nears Completion of Rebranding 200 Loblaw Gas Stations""Learn about ExxonMobil's operations in Egypt""Petrol and Diesel Service Stations in Egypt - Mobil"Official websiteExxon Mobil corporate websiteMobil Industrial official websiteeeeeeeeDA04275022275790-40000 0001 0860 5061n82045453134887257134887257

Image
Aera EnergyEssoEsso AustraliaExxonExxon NeftegasHumble OilImperial OilMagnolia Petroleum CompanyMobilMobil Producing NigeriaPetronSeaRiver MaritimeSuperior Oil CompanySyncrudeVacuum Oil CompanyXTO EnergyBaton Rouge RefineryBaytown RefineryMilford HavenExxon Building (New York)Fawley RefineryImperial Oil BuildingMossmorranNanticoke Refinery2010 ExxonMobil oil spill2010 Port Arthur oil spill2013 Mayflower oil spill Exxon Valdez oil spillGreenpoint oil spillSS Atlantic Empress SS Esso Brussels Colony Shale Oil ProjectEast-Prinovozemelsky fieldGoose Creek Oil FieldKearl Oil Sands ProjectKizomba deepwater projectOrmen LangePembina oil fieldPrudhoe Bay Oil FieldSable Offshore Energy ProjectSakhalin-ITengiz FieldTern oilfieldTuapse fieldWest Qurna FieldNational OilSasolSparSpar Express759 Store7-ElevenCircle KCUDaily YamazakiFamilyMartGS25LawsonMinistopParknShopPoplarSparStorywayVanGOemartSparampmBuy the WayBP ConnectCircle K SunkusDaily StopOn the Run7-ElevenBargain BoozeBest-OneBP ConnectB
Read more

Frič See also Navigation menuinternal link

Image
SurnamesCzech-language surnames ‹ The template Infobox surname is being considered for merging. › Frič Origin Language(s) Czechized German (eastern Middle German dialects and Alemannic German) - Thuringian, Upper Saxon, Low Lusatian, Silesian Meaning derived from German: Friedrich Other names Variant(s) Fritsch, Fritzsch, Frycz, Fricz, Fryczyński, Frietsch, Fritsche, Fritzsche; Fritschi (Alemannic), Fritz, Fritze, Fritzel, Fritzl, Fritzke, Fritzen Frič is a Czechized German surname. Notable people with the surname include: Alberto Vojtěch Frič, Czech botanist Antonín Jan Frič (Fritsch) , Czech paleontologist Jaroslav Erik Frič, Czech poet Martin Frič, Czech film director, screenwriter and actor See also Fričovce (Hungarian: Frics ) .mw-parser-output table.dmboxclear:both;margin:0.9em 1em;border-top:1px solid #ccc;border-bottom:1px solid #ccc;background-color:transparent Surname list This page lists people with the surname Frič . If an internal link intending to refer to a specifi
Read more

Identify plant with long narrow paired leaves and reddish stems Planned maintenance scheduled April 17/18, 2019 at 00:00UTC (8:00pm US/Eastern) Announcing the arrival of Valued Associate #679: Cesar Manara Unicorn Meta Zoo #1: Why another podcast?What is this plant with long sharp leaves? Is it a weed?What is this 3ft high, stalky plant, with mid sized narrow leaves?What is this young shrub with opposite ovate, crenate leaves and reddish stems?What is this plant with large broad serrated leaves?Identify this upright branching weed with long leaves and reddish stemsPlease help me identify this bulbous plant with long, broad leaves and white flowersWhat is this small annual with narrow gray/green leaves and rust colored daisy-type flowers?What is this chilli plant?Does anyone know what type of chilli plant this is?Help identify this plant

Image
Apollo command module space walk? prime numbers and expressing non-prime numbers Can a non-EU citizen traveling with me come with me through the EU passport line? Extract all GPU name, model and GPU ram How to deal with a team lead who never gives me credit? Why was the term "discrete" used in discrete logarithm? Why do we bend a book to keep it straight? When do you get frequent flier miles - when you buy, or when you fly? How come Sam didn't become Lord of Horn Hill? At the end of Thor: Ragnarok why don't the Asgardians turn and head for the Bifrost as per their original plan? Is it true that "carbohydrates are of no use for the basal metabolic need"? Using et al. for a last / senior author rather than for a first author How to tell that you are a giant? How to react to hostile behavior from a senior developer? String `!23` is replaced with `docker` in command line How to find out what spells would be useless to a blind NPC sp
Read more