NESS-0327 (original) (raw)
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.Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM and18.4nM).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.
| Property | Value |
|---|---|
| dbo:abstract | 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.Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM and18.4nM).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. (en) |
| dbo:casNumber | 494844-07-4 |
| dbo:fdaUniiCode | X1BQI2J97I |
| dbo:pubchem | 10435654 |
| dbo:thumbnail | wiki-commons:Special:FilePath/NESS-0327.png?width=300 |
| dbo:wikiPageID | 17302912 (xsd:integer) |
| dbo:wikiPageLength | 4608 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1082425009 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Cannabinoid_receptor dbr:Rimonabant dbc:Cannabinoids dbc:Chloroarenes dbc:Hydrazides dbc:Piperazines dbr:NESS-040C5 dbr:Dissociation_constant dbc:Pyrazoles dbr:Inverse_agonist dbc:CB1_receptor_antagonists dbr:Cannabinoid_receptor_1 dbr:Discovery_and_development_of_Cannabinoid_Receptor_1_Antagonists dbr:Antagonist_(pharmacology) dbr:Neutral_antagonist |
| dbp:c | 24 (xsd:integer) |
| dbp:casNumber | 494844 (xsd:integer) |
| dbp:chemspiderid | 8611079 (xsd:integer) |
| dbp:cl | 3 (xsd:integer) |
| dbp:h | 23 (xsd:integer) |
| dbp:n | 4 (xsd:integer) |
| dbp:o | 1 (xsd:integer) |
| dbp:pubchem | 10435654 (xsd:integer) |
| dbp:smiles | Clc3ccccc3-n4c2-c1ccccc1CCCc2cCNN5CCCCC5 (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | NCXBPZJQQSNIRA-UHFFFAOYSA-N (en) |
| dbp:unii | X1BQI2J97I (en) |
| dbp:verifiedfields | changed (en) |
| dbp:verifiedrevid | 424803248 (xsd:integer) |
| dbp:watchedfields | changed (en) |
| dbp:wikiPageUsesTemplate | dbt:Cannabinoid-stub dbt:Cannabinoids dbt:Drugbox dbt:Reflist dbt:Short_description dbt:Chemspidercite dbt:Drugbankcite dbt:Fdacite dbt:Stdinchicite |
| dcterms:subject | dbc:Cannabinoids dbc:Chloroarenes dbc:Hydrazides dbc:Piperazines dbc:Pyrazoles dbc:CB1_receptor_antagonists |
| gold:hypernym | dbr:Drug |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 yago:WikicatCB1ReceptorAntagonists yago:Adversary109773245 yago:CausalAgent100007347 yago:LivingThing100004258 yago:Object100002684 yago:Organism100004475 yago:Person100007846 yago:PhysicalEntity100001930 yago:YagoLegalActor yago:YagoLegalActorGeo dbo:Drug yago:Whole100003553 umbel-rc:DrugProduct |
| rdfs:comment | 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.Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM and18.4nM).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. (en) |
| rdfs:label | NESS-0327 (en) |
| owl:sameAs | freebase:NESS-0327 yago-res:NESS-0327 wikidata:NESS-0327 dbpedia-sh:NESS-0327 dbpedia-sr:NESS-0327 https://global.dbpedia.org/id/4rhcZ |
| prov:wasDerivedFrom | wikipedia-en:NESS-0327?oldid=1082425009&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/NESS-0327.png |
| foaf:isPrimaryTopicOf | wikipedia-en:NESS-0327 |
| is dbo:wikiPageWikiLink of | dbr:List_of_designer_drugs dbr:List_of_psychedelic_drugs dbr:NESS-040C5 dbr:Cannabinoid_receptor_antagonist |
| is foaf:primaryTopic of | wikipedia-en:NESS-0327 |
