Page last updated: 2024-11-13

s-777469

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

Description

S-777469: an orally available cannabinoid receptor CB2 agonist as an antipruritic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID57331749
CHEMBL ID2019090
SCHEMBL ID2745978
MeSH IDM0577137

Synonyms (12)

Synonym
bdbm50380892
CHEMBL2019090 ,
s-777469
SCHEMBL2745978
88NI79737I ,
885496-53-7
unii-88ni79737i
Q27269944
MS-27176
CS-0356760
HY-145153
DTXSID301336647

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" In conclusion, these data should be useful for the characterization of the pharmacokinetic properties of S-777469 and the estimation of its pharmacokinetic fate in humans."( Non-clinical evaluation of the metabolism, pharmacokinetics and excretion of S-777469, a new cannabinoid receptor 2 selective agonist.
Hasegawa, H; Kanazu, T; Sekiguchi, K; Takeuchi, M; Yamaguchi, Y, 2014
)
0.84
" Total radioactivity was rapidly and well absorbed in humans, with Cmax of 11,308 ng eq."( The metabolism and pharmacokinetics of [14C]-S-777469, a new cannabinoid receptor 2 selective agonist, in healthy human subjects.
Fukumura, K; Hasegawa, H; Kanazu, T; Sekiguchi, K, 2015
)
0.68

Bioavailability

ExcerptReferenceRelevance
" S-777469 was rapidly and well absorbed, with bioavailability values ranging from 50 to 70% in rats and dogs, almost all drug radioactivity was excreted into the feces via bile within 48 h."( Non-clinical evaluation of the metabolism, pharmacokinetics and excretion of S-777469, a new cannabinoid receptor 2 selective agonist.
Hasegawa, H; Kanazu, T; Sekiguchi, K; Takeuchi, M; Yamaguchi, Y, 2014
)
1.54
" Total radioactivity was rapidly and well absorbed in humans, with Cmax of 11,308 ng eq."( The metabolism and pharmacokinetics of [14C]-S-777469, a new cannabinoid receptor 2 selective agonist, in healthy human subjects.
Fukumura, K; Hasegawa, H; Kanazu, T; Sekiguchi, K, 2015
)
0.68
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cannabinoid receptor 1Homo sapiens (human)IC50 (µMol)2.00000.00010.275310.0000AID655737
Cannabinoid receptor 1Homo sapiens (human)Ki4.42470.00010.50779.6000AID1127546; AID1638014; AID655735
Cannabinoid receptor 2 Homo sapiens (human)IC50 (µMol)0.02400.00081.58409.8000AID655738
Cannabinoid receptor 2 Homo sapiens (human)Ki0.03600.00000.415610.0000AID1127545; AID1638013; AID655736
[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
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 (24)

Assay IDTitleYearJournalArticle
AID655753Volume of distribution at steady state in cynomolgus monkey at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655738Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655749Half life in beagle dog at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655752Volume of distribution at steady state in beagle dog at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655754Oral bioavailability in rat at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655756Oral bioavailability in cynomolgus monkey at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID1638013Agonist activity at human CB2 receptor2019European journal of medicinal chemistry, Mar-01, Volume: 165Benzo[d]thiazol-2(3H)-ones as new potent selective CB
AID655751Volume of distribution at steady state in rat at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655736Displacement of [3H]-CP55940 from human recombinant CB2 receptor after 60 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID1127545Agonist activity at CB2 receptor (unknown origin)2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID1638014Agonist activity at human CB1 receptor2019European journal of medicinal chemistry, Mar-01, Volume: 165Benzo[d]thiazol-2(3H)-ones as new potent selective CB
AID655745Clearance in rat at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655735Displacement of [3H]-CP55940 from human recombinant CB1 receptor after 60 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655747Clearance in cynomolgus monkey at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655743Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 3 mg/kg, po measured after 30 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655755Oral bioavailability in beagle dog at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655742Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 1 mg/kg, po measured after 30 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655744Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 10 mg/kg, po measured after 30 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655748Half life in rat at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID1127546Agonist activity at CB1 receptor (unknown origin)2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
AID655746Clearance in beagle dog at 3 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655750Half life in cynomolgus monkey at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655739Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
AID655737Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.31

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.31 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]