4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide: a CB1 cannabinoid receptor radioligand for PET imaging [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11995515 |
| CHEMBL ID | 514215 |
| MeSH ID | M0504960 |
| Synonym |
|---|
| 4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-n-(piperidin-1-yl)-1h-pyrazole-3-carboxamide |
| bdbm50267373 |
| CHEMBL514215 , |
| jhu-75528 |
| 7DE9P17E1J , |
| 947696-17-5 |
| unii-7de9p17e1j |
| 1h-pyrazole-3-carboxamide, 4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-n-1-piperidinyl- |
| omar |
| 4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-n-piperidin-1-ylpyrazole-3-carboxamide |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Homo sapiens (human) | Ki | 0.0110 | 0.0001 | 0.5077 | 9.6000 | AID416057 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| mitochondrial outer membrane | Cannabinoid receptor 1 | Homo sapiens (human) |
| plasma membrane | Cannabinoid receptor 1 | Homo sapiens (human) |
| actin cytoskeleton | Cannabinoid receptor 1 | Homo sapiens (human) |
| growth cone | Cannabinoid receptor 1 | Homo sapiens (human) |
| presynaptic membrane | Cannabinoid receptor 1 | Homo sapiens (human) |
| membrane raft | Cannabinoid receptor 1 | Homo sapiens (human) |
| glutamatergic synapse | Cannabinoid receptor 1 | Homo sapiens (human) |
| GABA-ergic synapse | Cannabinoid receptor 1 | Homo sapiens (human) |
| plasma membrane | Cannabinoid receptor 1 | Homo sapiens (human) |
| cytoplasm | Cannabinoid receptor 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID416058 | Octanol-phosphate buffer partition coefficient, log D at pH 7.4 by shake-flask method | 2009 | European 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. |
| AID415907 | Antagonist activity at CB1 receptor in C57/BL6 mouse striatum assessed as blockade of WIN-55212-2 induced inhibition of glutamate release at 3 uM by electrophysiology | 2009 | European 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. |
| AID416057 | Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting | 2009 | European 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (28.57) | 29.6817 |
| 2010's | 5 (71.43) | 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] | ||
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 (12.51) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||