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5-hydroxytryptamine 2A receptor inverse agonist
An inverse agonist that binds to the same receptor as a 5-hydroxytryptamine 2A receptor agonist, but which induces a pharmacological response opposite to that agonist.
ChEBI ID: 133016
Members (1)
| Member | Definition | Class |
|---|---|---|
| pimavanserin | A member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease. | pimavanserin |
Research
Studies (149)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (6.71) | 29.6817 |
| 2010's | 79 (53.02) | 24.3611 |
| 2020's | 60 (40.27) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 23 (14.47%) | 5.53% |
| Reviews | 38 (23.90%) | 6.00% |
| Case Studies | 5 (3.14%) | 4.05% |
| Observational | 1 (0.63%) | 0.25% |
| Other | 92 (57.86%) | 84.16% |
Protein Targets (17)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 5.3547 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 21.3174 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 37.9083 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 37.9083 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 0.0335 | 5 | 6 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.0009 | 2 | 3 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 0.0464 | 1 | 2 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 0.0464 | 1 | 2 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.0012 | 2 | 3 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 52.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 49.8000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 0.4100 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Kb | 0.0006 | 1 | 1 |