Molecule Details
| InChIKey | FIADGNVRKBPQEU-UHFFFAOYSA-N |
|---|---|
| Compound Name | Pizotifen |
| Canonical SMILES | CN1CCC(=C2c3ccccc3CCc3sccc32)CC1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 9 |
| Pfam Stratification | Homologous |
| Avg pChEMBL | 7.99 |
| Source | ChEMBL |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB06153 |
|---|---|
| Drug Name | Pizotifen |
| CAS Number | 15574-96-6 |
| Groups | approved |
| ATC Codes | N02CX01 |
| Description | Pizotifen belongs to the class of antamines and is related to [cyproheptadine].[A32532] It is a potent serotonin and tryptamine antagonist that has been used for migraine prevention for many years. It exhibits weak anticholinergic, antihistamine, and antikinin actions in addition to sedative and app... |
Categories: Adrenergic Antagonists Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists Agents producing tachycardia Agents that produce hypertension Analgesics Analgesics, Non-Narcotic Anticholinergic Agents Antidepressive Agents Antimigraine Agents, Miscellaneous Antimigraine Preparations Central Nervous System Agents Central Nervous System Depressants Histamine Antagonists Histamine H1 Antagonists Muscarinic Antagonists Nervous System Neurotransmitter Agents Peripheral Nervous System Agents Psychotropic Drugs Sensory System Agents Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin 5-HT1 Receptor Antagonists Serotonin 5-HT2 Receptor Antagonists Serotonin 5-HT2A Receptor Antagonists Serotonin 5-HT2C Receptor Antagonists Serotonin Agents Serotonin Receptor Antagonists Sulfur Compounds Thiophenes
Cross-references: BindingDB: 82088 ChEBI: 50212 CHEMBL294951 ChemSpider: 25497 Drugs Product Database (DPD): 12057 PubChem:27400 PubChem:347827758 RxCUI: 8373 Wikipedia: Pizotifen ZINC: ZINC000000001968
Target Activities (9)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P28335 | HTR2C | Homo sapiens | Human | PF00001 | 8.8 | Ki | ChEMBL |
| P11229 | CHRM1 | Homo sapiens | Human | PF00001 | 8.7 | Ki | ChEMBL |
| P41595 | HTR2B | Homo sapiens | Human | PF00001 | 8.7 | Ki | ChEMBL |
| P14416 | DRD2 | Homo sapiens | Human | PF00001 | 8.6 | Ki | ChEMBL |
| P28223 | HTR2A | Homo sapiens | Human | PF00001 | 8.1 | Ki | ChEMBL |
| P34969 | HTR7 | Homo sapiens | Human | PF00001 | 7.6 | Ki | ChEMBL |
| P25100 | ADRA1D | Homo sapiens | Human | PF00001 | 7.1 | Ki | ChEMBL |
| P35348 | ADRA1A | Homo sapiens | Human | PF00001 | 7.1 | Ki | ChEMBL |
| P35368 | ADRA1B | Homo sapiens | Human | PF00001 | 7.1 | Ki | ChEMBL |
DrugBank Target Actions (16)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P36537 | P36537 | UDP-glucuronosyltransferase 2B10 | substrate | enzymes |
| P08172 | CHRM2 | Muscarinic acetylcholine receptor M2 | antagonist | targets |
| P08913 | ADRA2A | Alpha-2A adrenergic receptor | antagonist | targets |
| P11229 | CHRM1 | Muscarinic acetylcholine receptor M1 | antagonist | targets |
| P18089 | ADRA2B | Alpha-2B adrenergic receptor | antagonist | targets |
| P18825 | ADRA2C | Alpha-2C adrenergic receptor | antagonist | targets |
| P20309 | CHRM3 | Muscarinic acetylcholine receptor M3 | antagonist | targets |
| P25100 | ADRA1D | Alpha-1D adrenergic receptor | antagonist | targets |
| P28222 | HTR1B | 5-hydroxytryptamine receptor 1B | antagonist | targets |
| P28223 | HTR2A | 5-hydroxytryptamine receptor 2A | antagonist | targets |
| P28335 | HTR2C | 5-hydroxytryptamine receptor 2C | antagonist | targets |
| P35348 | ADRA1A | Alpha-1A adrenergic receptor | antagonist | targets |
| P35367 | HRH1 | Histamine H1 receptor | antagonist | targets |
| P35368 | ADRA1B | Alpha-1B adrenergic receptor | antagonist | targets |
| P41595 | HTR2B | 5-hydroxytryptamine receptor 2B | antagonist | targets |
| P08908 | HTR1A | 5-hydroxytryptamine receptor 1A | partial agonist | targets |