| Compound Information | SONAR Target prediction |
| Name: | Perphenazine |
| Unique Identifier: | LOPAC 01145 |
| MolClass: | Checkout models in ver1.5 and ver1.0 |
| Molecular Formula: | C21ClH26N3OS |
| Molecular Weight: | 377.763 g/mol |
| X log p: | 16.257 (online calculus) |
| Lipinksi Failures | 1 |
| TPSA | 35.02 |
| Hydrogen Bond Donor Count: | 0 |
| Hydrogen Bond Acceptors Count: | 4 |
| Rotatable Bond Count: | 6 |
| Canonical Smiles: | OCCN1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc23)CC1 |
| Class: | Dopamine |
| Action: | Antagonist |
| Selectivity: | DRD2 |
| Generic_name: | Perphenazine |
| Chemical_iupac_name: | 2-[4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl]ethanol |
| Drug_type: | Approved Drug |
| Pharmgkb_id: | PA450882 |
| Kegg_compound_id: | C07427 |
| Drugbank_id: | APRD00429 |
| Melting_point: | 97 oC |
| H2o_solubility: | 28.3 mg/L |
| Logp: | 4.176 |
| Isoelectric_point: | 7.94 |
| Cas_registry_number: | 58-39-9 |
| Mass_spectrum: | http://webbook.nist.gov/cgi/cbook.cgi?Spec=C58399&Index=0&Type=Mass&Large=on |
| Drug_category: | Antipsychotics; Phenothiazines; Dopamine Antagonists; ATC:N05AB03 |
| Indication: | For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults. |
| Pharmacology: | Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and has a greater behavioral potency than other phenothiazine derivatives whose side chains do not contain a piperazine moiety. It is a member of a class of drugs called phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to 15 times as potent as chlorpromazine; that means perphenazine is a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapypramidal side-effects compared to Haloperidol. |
| Mechanism_of_action: | Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor-s action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. |
| Organisms_affected: | Humans and other mammals |
| Found: 24 nonactive as graph: single | with analogs | 1 2 3 4 5 6 7 8 9 10 Next >> [24] |
| Species: | 4932 |
| Condition: | BY4741 |
| Replicates: | 8 |
| Raw OD Value: r im | 0.8515±0.0837439 |
| Normalized OD Score: sc h | 1.0846±0.078614 |
| Z-Score: | 2.6991±1.87038 |
| p-Value: | 0.00865568 |
| Z-Factor: | -2.76755 |
| Fitness Defect: | 4.7495 |
| Bioactivity Statement: | Nonactive |
| ps |
| DBLink | Rows returned: 6 |
| 4748 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol |
| 74835 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol dihydrochloride |
| 168090 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol hydrochloride |
| 213548 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-1,4-dimethyl-2,3,5,6-tetrahydropyrazin-1-yl]ethanol diiodide |
| 213549 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-1,4-dimethyl-2,3,5,6-tetrahydropyrazin-1-yl]ethanol |
| 4282573 | 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-2,3,5,6-tetrahydropyrazin-1-yl]ethanol |
| internal high similarity DBLink | Rows returned: 1 |
| SPE01503934 | 1.0000 |
| active | Cluster 17541 | Additional Members: 13 | Rows returned: 4 |
| SPE01503934 | 0.32258064516129 |
| SPE01500184 | 0 |
| LAT005D03 | 0 |
| LOPAC 00253 | 0 |
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