Page last updated: 2024-12-11

hu 210

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID9821569
CHEMBL ID307696
CHEBI ID190326
SCHEMBL ID1517460
MeSH IDM0171822

Synonyms (26)

Synonym
gtpl731
PDSP2_000201
hu-210, solid (air sensitive)
(6ar)-trans-3-(1,1-dimethylheptyl)-6a,7,10,10a-tetrahydro-1-hydroxy-6,6-dimethyl-6h-dibenzo[b,d]pyran-9-methanol
hu 210
hu-210
hu210
CHEMBL307696 ,
(6ar,10ar)-3-(1,1-dimethyl-heptyl)-9-hydroxymethyl-6,6-dimethyl-6a,7,10,10a-tetrahydro-6h-benzo[c]chromen-1-ol
(6ar,10ar)-9-(hydroxymethyl)-6,6-dimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydro-6h-benzo[c]chromen-1-ol
bdbm50067499
(6ar,10ar)-3(1,1-dimethylheptyl)-9-hydroxymethyl)-6,6-dimethyl-6a,7,10,10a-tetrahydro-6h-benzo[c]chromen-1-ol
CHEBI:190326
112830-95-2
(6ar,10ar)-9-(hydroxymethyl)-6,6-dimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydrobenzo[c]chromen-1-ol
(-)-hu-210
unii-191042422p
191042422p ,
6h-dibenzo(b,d)pyran-9-methanol, 3-(1,1-dimethylheptyl)-6a,7,10,10a-tetrahydro-1-hydroxy-6,6-dimethyl-, (6ar,10ar)-
SCHEMBL1517460
AKOS024458716
DTXSID30150188
Q411905
SB16778
hu-210, 0.1mg/ml in methanol
hu-210, 1mg/ml in methanol
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
1-benzopyran
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fatty acid-binding protein, liverMus musculus (house mouse)Ki0.85000.02100.34832.0000AID1802031
Cannabinoid receptor 1Rattus norvegicus (Norway rat)Ki0.00070.00020.566510.0000AID1626943; AID49146
Cannabinoid receptor 1Homo sapiens (human)Ki0.00510.00010.50779.6000AID1127482; AID1416642; AID259614; AID310543; AID416057; AID607138
Cannabinoid receptor 2 Homo sapiens (human)Ki0.00390.00000.415610.0000AID1057093; AID1127483; AID1185845; AID1416639; AID1626945; AID1662649; AID259197; AID310544; AID415513; AID621410
Cannabinoid receptor 2Mus musculus (house mouse)Ki0.00020.00020.07970.7943AID1626944
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.00460.00411.89638.7000AID257800; AID259201
Glutamate receptor 2Rattus norvegicus (Norway rat)EC50 (µMol)0.00460.00411.62517.6000AID257800; AID259201
Glutamate receptor 3Rattus norvegicus (Norway rat)EC50 (µMol)0.00460.00411.17063.5000AID257800; AID259201
Glutamate receptor 4Rattus norvegicus (Norway rat)EC50 (µMol)0.00460.00411.13393.5000AID257800; AID259201
Cannabinoid receptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.00500.00020.19211.9953AID257800
Cannabinoid receptor 1Homo sapiens (human)EC50 (µMol)0.02030.00010.12752.2400AID259615; AID445957
Cannabinoid receptor 2 Homo sapiens (human)EC50 (µMol)0.00260.00030.15173.2800AID1204172; AID259201; AID288422; AID412168; AID445959
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
positive regulation of acute inflammatory response to antigenic stimulusCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
spermatogenesisCannabinoid receptor 1Homo sapiens (human)
axonal fasciculationCannabinoid receptor 1Homo sapiens (human)
response to nutrientCannabinoid receptor 1Homo sapiens (human)
memoryCannabinoid receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentCannabinoid receptor 1Homo sapiens (human)
negative regulation of serotonin secretionCannabinoid receptor 1Homo sapiens (human)
positive regulation of fever generationCannabinoid receptor 1Homo sapiens (human)
negative regulation of fatty acid beta-oxidationCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, GABAergicCannabinoid receptor 1Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 1Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 1Homo sapiens (human)
negative regulation of dopamine secretionCannabinoid receptor 1Homo sapiens (human)
response to nicotineCannabinoid receptor 1Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 1Homo sapiens (human)
response to cocaineCannabinoid receptor 1Homo sapiens (human)
glucose homeostasisCannabinoid receptor 1Homo sapiens (human)
positive regulation of apoptotic processCannabinoid receptor 1Homo sapiens (human)
response to ethanolCannabinoid receptor 1Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 1Homo sapiens (human)
negative regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
positive regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
regulation of insulin secretionCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicCannabinoid receptor 1Homo sapiens (human)
maternal process involved in female pregnancyCannabinoid receptor 1Homo sapiens (human)
regulation of feeding behaviorCannabinoid receptor 1Homo sapiens (human)
regulation of penile erectionCannabinoid receptor 1Homo sapiens (human)
retrograde trans-synaptic signaling by endocannabinoidCannabinoid receptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationCannabinoid receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 1Homo sapiens (human)
response to amphetamineCannabinoid receptor 2 Homo sapiens (human)
inflammatory responseCannabinoid receptor 2 Homo sapiens (human)
immune responseCannabinoid receptor 2 Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 2 Homo sapiens (human)
leukocyte chemotaxisCannabinoid receptor 2 Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicCannabinoid receptor 2 Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 2 Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 2 Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 2 Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 2 Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 2 Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
cannabinoid receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 1Homo sapiens (human)
identical protein bindingCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 2 Homo sapiens (human)
cannabinoid receptor activityCannabinoid receptor 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
mitochondrial outer membraneCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
actin cytoskeletonCannabinoid receptor 1Homo sapiens (human)
growth coneCannabinoid receptor 1Homo sapiens (human)
presynaptic membraneCannabinoid receptor 1Homo sapiens (human)
membrane raftCannabinoid receptor 1Homo sapiens (human)
glutamatergic synapseCannabinoid receptor 1Homo sapiens (human)
GABA-ergic synapseCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
cytoplasmCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 2 Homo sapiens (human)
dendriteCannabinoid receptor 2 Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneCannabinoid receptor 2 Homo sapiens (human)
perikaryonCannabinoid receptor 2 Homo sapiens (human)
endoplasmic reticulumCannabinoid receptor 2 Homo sapiens (human)
plasma membraneCannabinoid receptor 2 Homo sapiens (human)
cytoplasmCannabinoid receptor 2 Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (69)

Assay IDTitleYearJournalArticle
AID1346728Human CB2 receptor (Cannabinoid receptors)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.
AID1346728Human CB2 receptor (Cannabinoid receptors)1996The Journal of pharmacology and experimental therapeutics, Sep, Volume: 278, Issue:3
Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
AID1345070Human GPR55 (GPR18, GPR55 and GPR119)2007British journal of pharmacology, Dec, Volume: 152, Issue:7
The orphan receptor GPR55 is a novel cannabinoid receptor.
AID1346701Human CB1 receptor (Cannabinoid receptors)1995Molecular pharmacology, Sep, Volume: 48, Issue:3
Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
AID1346728Human CB2 receptor (Cannabinoid receptors)1995Molecular pharmacology, Sep, Volume: 48, Issue:3
Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
AID1346701Human CB1 receptor (Cannabinoid receptors)1996The Journal of pharmacology and experimental therapeutics, Sep, Volume: 278, Issue:3
Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
AID310545Selectivity for human CB2 over human CB12007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
AID127832Compound was evaluated in mouse model for cannabimimetic activity, expressed as as effective dose for antinociception (TF)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.
AID1204172Agonist activity at human CB2 receptor transfected in CHO cell membranes after 90 mins by [35S]-GTPgammaS assay2015European journal of medicinal chemistry, Jun-05, Volume: 97New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.
AID607138Binding affinity to CB1 receptor2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.
AID1626939Induction of CB1-related discriminative stimulus effect in squirrel monkey at 0.003 mg/kg, im measured after 24 hrs2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID621410Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in CHO-K1 cells2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells.
AID1626945Displacement of [3H]CP55940 from human CB2 receptor2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1193635Agonist activity at rat cerebellar membrane cannabinoid CB1 receptor assessed as [35S]GTPgammaS binding at 1 uM relative to control2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Loratadine analogues as MAGL inhibitors.
AID1193637Agonist activity at human cannabinoid CB2 receptor introduced into CHO cells assessed as [35S]GTPgammaS binding at 10 nM relative to control2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Loratadine analogues as MAGL inhibitors.
AID259616Maximum stimulation at human CB1 receptor by [35S]GTP-gamma-S assay compared to the basal level2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
AID1632066Toxicity in naive Sprague-Dawley rat assessed as hypothermia at 0.01 mg/kg, ip after 2 to 48 hrs by core temperature test2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID310544Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
AID1626946Effect on response rate in squirrel monkey at 0.003 mg/kg, im2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID259614Displacement of [3H]SR141716A from human CB1 receptor2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
AID1416639Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis2017MedChemComm, Aug-01, Volume: 8, Issue:8
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB
AID1632055Analgesic activity in naive Sprague-Dawley rat assessed as tail flick latency at 0.1 to 10 mg/kg administered through oral gavage up to 48 hrs by tail-flick assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID1185845Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.
AID472421Antagonist activity at human recombinant alpha 2 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
AID1626944Binding affinity to mouse CB2 receptor2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1626941Induction of CB1-related discriminative stimulus effect in squirrel monkey at 0.003 mg/kg, im measured at 36 hrs2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID445959Agonist activity at human recombinant cannabinoid CB2 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
AID1626926Hypothermic activity in sc dosed Sprague-Dawley rat assessed as decrease in rectal body temperature measured over 6 hrs2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID259201Effect on [35S]GTP-gamma-S binding to human CB2 receptor2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
AID310543Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
AID1632065Toxicity in naive Sprague-Dawley rat assessed as motor incoordination at 0.01 mg/kg, ip after 2 to 48 hrs by rotarod test2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID415513Binding affinity to human recombinant CB2 receptor expressed in african green monkey COS cells by radioligand binding assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo.
AID1127484Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID1662649Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK cell membrane2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.
AID1057093Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Development of fluorinated CB(2) receptor agonists for PET studies.
AID127835Compound was evaluated in mouse model for cannabimimetic activity, expressed as effective dose for spontaneous activity(SA)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.
AID1626938Induction of CB1-related discriminative stimulus effect in squirrel monkey assessed as time required for 50% loss of full effect at 0.003 mg/kg, im2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1626918Half life in mouse plasma assessed as esterase-mediated compound hydrolysis at 200 uM by HPLC method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1632067Toxicity in naive Sprague-Dawley rat assessed as immobility at 0.01 mg/kg, ip by after 2 to 48 hrs by catalepsy ring test2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID1127482Binding affinity to human CB1 receptor2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID1626930Hypothermic activity in Sprague-Dawley rat assessed as time required for decrease in rectal body temperature at 0.01 to 1 mg/kg, sc2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1416642Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis2017MedChemComm, Aug-01, Volume: 8, Issue:8
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB
AID1245641Agonist activity at human CB2R expressed in CHO cell membranes at 10 nM by [35S]GTPgammaS binding assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.
AID1632054Analgesic activity in naive Sprague-Dawley rat assessed as increase in tail flick latency at 0.3 mg/kg, ip up to 48 hrs by tail-flick assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID257800Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.
AID1267177Agonist activity at CBR2 (unknown origin) assessed as [35S]GTPgammaS binding at 10 nM by luminescence assay relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists.
AID259615Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assay2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
AID1626943Binding affinity to rat CB1 receptor2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID412168Agonist activity at human CB2 receptor expressed in yeast cells assessed as degradation of FDGlu to fluorescein after 24 hrs2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
AID259200Effect on human CB2 receptor stimulation by [35S]GTP-gamma-S binding at 10 uM (basal value set at 100%)2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
AID127834Compound was evaluated in mouse model for cannabimimetic activity, expressed as as effective dose for hypothermia (rectal temperature, RT)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.
AID259197Displacement of [3H]CP-55940 from human CB2 receptor2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
AID1245639Agonist activity at CB1R in rat cerebellar membranes at 1 uM by [35S]GTPgammaS binding assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.
AID445957Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
AID288422Agonist activity at human recombinant CB2 receptor expressed in Saccharomyces cerevisiae cells2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
AID1433080Hypothermic activity in sc dosed Sprague-Dawley rat assessed as duration of hypothermic effect at 0.3 mg/kg, sc measured after 12 hrs post dose2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Probing the carboxyester side chain in controlled deactivation (-)-δ(8)-tetrahydrocannabinols.
AID474948Antagonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
AID1433075Hypothermic activity in sc dosed Sprague-Dawley rat measured over 6 hrs post dose2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Probing the carboxyester side chain in controlled deactivation (-)-δ(8)-tetrahydrocannabinols.
AID49666Displacement of [3H]CP-55940 binding to Cannabinoid receptor 1 in rat brain membranes1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Derivation of a pharmacophore model for anandamide using constrained conformational searching and comparative molecular field analysis.
AID1626937Induction of CB1-related discriminative stimulus effect in squirrel monkey at 0.003 mg/kg, im measured within 15 mins2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID472422Antagonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx up to 30 uM by whole cell patch clamp assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
AID1127483Binding affinity to human CB2 receptor2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID416057Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity.
AID259617Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
AID49146Binding affinity for the Cannabinoid receptor using [3H]CP-55940 as radioligand1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Enantioselective synthesis and pharmacology of 11-hydroxy-(1'S,2'R)-dimethylheptyl-delta 8-THC.
AID288424Agonist activity at human recombinant CB1 receptor expressed in Saccharomyces cerevisiae cells upto 30 uM2007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
AID1626919Half life in rat plasma assessed as esterase-mediated compound hydrolysis at 200 uM by HPLC method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
AID1632064Analgesic activity in naive Sprague-Dawley rat assessed as tail flick latency at 0.01 mg/kg, ip up to 48 hrs by tail-flick assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Peripherally Selective Cannabinoid 1 Receptor (CB1R) Agonists for the Treatment of Neuropathic Pain.
AID1802031FABP1 Fluorescent Ligand Displacement Assay from Article 10.1021/acs.biochem.6b00446: \\FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.\\2016Biochemistry, 09-20, Volume: 55, Issue:37
FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (16.13)18.2507
2000's10 (32.26)29.6817
2010's15 (48.39)24.3611
2020's1 (3.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.23%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (96.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]