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 Source | ID |
|---|---|
| PubMed CID | 57331749 |
| CHEMBL ID | 2019090 |
| SCHEMBL ID | 2745978 |
| MeSH ID | M0577137 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0001 | 0.2753 | 10.0000 | AID655737 |
| Cannabinoid receptor 1 | Homo sapiens (human) | Ki | 4.4247 | 0.0001 | 0.5077 | 9.6000 | AID1127546; AID1638014; AID655735 |
| Cannabinoid receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0240 | 0.0008 | 1.5840 | 9.8000 | AID655738 |
| Cannabinoid receptor 2 | Homo sapiens (human) | Ki | 0.0360 | 0.0000 | 0.4156 | 10.0000 | AID1127545; AID1638013; AID655736 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (39)
Molecular Functions (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cannabinoid receptor activity | Cannabinoid receptor 1 | Homo sapiens (human) |
| protein binding | Cannabinoid receptor 1 | Homo sapiens (human) |
| identical protein binding | Cannabinoid receptor 1 | Homo sapiens (human) |
| G protein-coupled receptor activity | Cannabinoid receptor 1 | Homo sapiens (human) |
| protein binding | Cannabinoid receptor 2 | Homo sapiens (human) |
| cannabinoid receptor activity | Cannabinoid receptor 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (13)
Bioassays (24)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID655753 | Volume of distribution at steady state in cynomolgus monkey at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655738 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655749 | Half life in beagle dog at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655752 | Volume of distribution at steady state in beagle dog at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655754 | Oral bioavailability in rat at 10 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655756 | Oral bioavailability in cynomolgus monkey at 10 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID1638013 | Agonist activity at human CB2 receptor | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID655751 | Volume of distribution at steady state in rat at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655736 | Displacement of [3H]-CP55940 from human recombinant CB2 receptor after 60 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID1127545 | Agonist activity at CB2 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. |
| AID1638014 | Agonist activity at human CB1 receptor | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID655745 | Clearance in rat at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655735 | Displacement of [3H]-CP55940 from human recombinant CB1 receptor after 60 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655747 | Clearance in cynomolgus monkey at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655743 | Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 3 mg/kg, po measured after 30 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655755 | Oral bioavailability in beagle dog at 10 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655742 | Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 1 mg/kg, po measured after 30 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655744 | Antipruritic activity in ICR mouse assessed as inhibition of compound 48/80-induced scratching at 10 mg/kg, po measured after 30 mins | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655748 | Half life in rat at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID1127546 | Agonist activity at CB1 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. |
| AID655746 | Clearance in beagle dog at 3 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655750 | Half life in cynomolgus monkey at 10 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655739 | Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
| AID655737 | Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins | 2012 | Bioorganic & 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 8 (100.00) | 24.3611 |
| 2020's | 0 (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.
| This Compound (12.31) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (12.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (87.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||