Repositioning Candidate Details
| Candidate ID: | R0185 |
| Source ID: | DB00543 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Amoxapine |
| Synonyms: | 2-Chloro-11-(1-piperazinyl)dibenz(b,f)(1,4)oxazepine; Amoxapine; Desmethylloxapin |
| Molecular Formula: | C17H16ClN3O |
| SMILES: | ClC1=CC2=C(OC3=CC=CC=C3N=C2N2CCNCC2)C=C1 |
| Structure: |
|
| DrugBank Description: | Amoxapine, the <i>N</i>-demethylated derivative of the antipsychotic agent loxapine, is a dibenzoxazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amoxapine does not affect mood or arousal, but may cause sedation. In depressed individuals, amoxapine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H<sub>1</sub> receptors, α<sub>1</sub>-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amoxapine may be used to treat neurotic and reactive depressive disorders, endogenous and psychotic depression, and mixed symptoms of depression and anxiety or agitation. |
| CAS Number: | 14028-44-5 |
| Molecular Weight: | 313.781 |
| DrugBank Indication: | For the relief of symptoms of depression in patients with neurotic or reactive depressive disorders as well as endogenous and psychotic depressions. May also be used to treat depression accompanied by anxiety or agitation. |
| DrugBank Pharmacology: | Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class, chemically distinct from the dibenzodiazepines, dibenzocycloheptenes, and dibenzoxepines. It has a mild sedative component to its action. The mechanism of its clinical action in man is not well understood. In animals, amoxapine reduced the uptake of nor-epinephirine and serotonin and blocked the response of dopamine receptors to dopamine. Amoxapine is not a monoamine oxidase inhibitor. Clinical studies have demonstrated that amoxapine has a more rapid onset of action than either amitriptyline or imipramine |
| DrugBank MoA: | Amoxapine acts by decreasing the reuptake of norepinephrine and serotonin (5-HT). |
| Targets: | Sodium-dependent noradrenaline transporter inhibitor; Sodium-dependent serotonin transporter inhibitor; Dopamine D2 receptor antagonist; Dopamine D1 receptor antagonist; Alpha-2A adrenergic receptor antagonist; Alpha-1A adrenergic receptor antagonist; Muscarinic acetylcholine receptor M1 antagonist; Gamma-aminobutyric acid receptor subunit alpha-1 antagonist; 5-hydroxytryptamine receptor 2A antagonist; 5-hydroxytryptamine receptor 2C antagonist; 5-hydroxytryptamine receptor 6 antagonist; 5-hydroxytryptamine receptor 7 antagonist; Dopamine D3 receptor antagonist; Dopamine D4 receptor antagonist; Histamine H1 receptor antagonist; Alpha-1 adrenergic receptors antagonist; Muscarinic acetylcholine receptor antagonist; 5-hydroxytryptamine receptor 2B antagonist; 5-hydroxytryptamine receptor 3A antagonist; 5-hydroxytryptamine receptor 1A antagonist; 5-hydroxytryptamine receptor 1B antagonist; Alpha-2 adrenergic receptors antagonist; Histamine H4 receptor binder; GABA(A) Receptor binder; Sodium-dependent dopamine transporter binder |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I17 | 1596 | Mental depression | Mental depression | disease of mental health/ cognitive disorder/ mood disorder | Details |
| I11 | 5295 | Intestinal disease | A gastrointestinal system disease that is located_in the intestine. http://en.wikipedia.org/wiki/Human_gastrointestinal_tract | disease of anatomical entity/gastrointestinal system disease | Details |