Molecule Details
| InChIKey | QSLMDECMDJKHMQ-UHFFFAOYSA-N |
|---|---|
| Compound Name | Maprotiline |
| Canonical SMILES | CNCCCC12CCC(c3ccccc31)c1ccccc12 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 20 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 6.72 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB00934 |
|---|---|
| Drug Name | Maprotiline |
| CAS Number | 10262-69-8 |
| Groups | approved |
| ATC Codes | N06AA21 |
| Description | Maprotiline is a tetracyclic antidepressant with similar pharmacological properties to tricyclic antidepressants (TCAs). Similar to TCAs, maprotiline inhibits neuronal norepinephrine reuptake, possesses some anticholinergic activity, and does not affect monoamine oxidase activity. It differs from TC... |
Categories: Adrenergic Agents Adrenergic Uptake Inhibitors Agents producing tachycardia Agents that reduce seizure threshold Anthracenes Anticholinergic Agents Antidepressive Agents Antidepressive Agents Indicated for Depression Antidepressive Agents, Second-Generation Antidepressive Agents, Tetracyclic Central Nervous System Agents Central Nervous System Depressants Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 Substrates Drugs that are Mainly Renally Excreted Histamine Antagonists Histamine H1 Antagonists Membrane Transport Modulators Muscarinic Antagonists Nervous System Neurotransmitter Agents Neurotransmitter Uptake Inhibitors Non-Selective Monoamine Reuptake Inhibitors Potential QTc-Prolonging Agents Psychoanaleptics Psychotropic Drugs QTc Prolonging Agents Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin Agents Serotonin Modulators Tricyclics and Other Norepinephrine-reuptake Inhibitors
Cross-references: BindingDB: 50101973 ChEBI: 6690 CHEMBL21731 ChemSpider: 3871 Drugs Product Database (DPD): 2274 Guide to Pharmacology: 2402 IUPHAR: 2402 C07107 D02566 PharmGKB: PA450322 PubChem:4011 PubChem:46508358 RxCUI: 6646 Therapeutic Targets Database: DAP001150 Wikipedia: Maprotiline ZINC: ZINC000001530688
Target Activities (20)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P35367 | HRH1 | Homo sapiens | Human | PF00001 | 8.8 | Ki | ChEMBL |
| P23975 | SLC6A2 | Homo sapiens | Human | PF00209 | 7.5 | Ki | ChEMBL;BindingDB |
| P28223 | HTR2A | Homo sapiens | Human | PF00001 | 7.5 | IC50 | ChEMBL |
| P28335 | HTR2C | Homo sapiens | Human | PF00001 | 7.2 | IC50 | ChEMBL |
| P08912 | CHRM5 | Homo sapiens | Human | PF00001 | 6.9 | IC50 | ChEMBL |
| P08173 | CHRM4 | Homo sapiens | Human | PF00001 | 6.8 | IC50 | ChEMBL |
| P18089 | ADRA2B | Homo sapiens | Human | PF00001 | 6.7 | IC50 | ChEMBL |
| P20309 | CHRM3 | Homo sapiens | Human | PF00001 | 6.7 | IC50 | ChEMBL |
| P41595 | HTR2B | Homo sapiens | Human | PF00001 | 6.6 | IC50 | ChEMBL |
| P25100 | ADRA1D | Homo sapiens | Human | PF00001 | 6.6 | IC50 | ChEMBL |
| P11229 | CHRM1 | Homo sapiens | Human | PF00001 | 6.5 | IC50 | ChEMBL |
| P21728 | DRD1 | Homo sapiens | Human | PF00001 | 6.4 | Ki | ChEMBL |
| P25021 | HRH2 | Homo sapiens | Human | PF00001 | 6.4 | IC50 | ChEMBL |
| P21918 | DRD5 | Homo sapiens | Human | PF00001 | 6.4 | Ki | ChEMBL |
| P18825 | ADRA2C | Homo sapiens | Human | PF00001 | 6.4 | Ki | ChEMBL |
| P35462 | DRD3 | Homo sapiens | Human | PF00001 | 6.3 | Ki | ChEMBL |
| P50406 | HTR6 | Homo sapiens | Human | PF00001 | 6.2 | IC50 | ChEMBL |
| P14416 | DRD2 | Homo sapiens | Human | PF00001 | 6.2 | Ki | ChEMBL |
| P08913 | ADRA2A | Homo sapiens | Human | PF00001 | 6.2 | Ki | ChEMBL |
| P08172 | CHRM2 | Homo sapiens | Human | PF00001 | 6.2 | Ki | ChEMBL |
DrugBank Target Actions (16)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P02763 | P02763 | Alpha-1-acid glycoprotein 1 | binder | carriers |
| P05177 | CYP1A2 | Cytochrome P450 1A2 | substrate | enzymes |
| P10635 | CYP2D6 | Cytochrome P450 2D6 | substrate | enzymes |
| P08172 | CHRM2 | Muscarinic acetylcholine receptor M2 | antagonist | targets |
| P08173 | CHRM4 | Muscarinic acetylcholine receptor M4 | antagonist | targets |
| P08912 | CHRM5 | Muscarinic acetylcholine receptor M5 | antagonist | targets |
| P08913 | ADRA2A | Alpha-2 adrenergic receptors | antagonist | targets |
| P11229 | CHRM1 | Muscarinic acetylcholine receptor M1 | antagonist | targets |
| P20309 | CHRM3 | Muscarinic acetylcholine receptor M3 | antagonist | targets |
| P34969 | HTR7 | 5-hydroxytryptamine receptor 7 | antagonist | targets |
| P35348 | ADRA1A | Alpha-1 adrenergic receptors | antagonist | targets |
| P35367 | HRH1 | Histamine H1 receptor | antagonist | targets |
| P14416 | DRD2 | D(2) dopamine receptor | binder | targets |
| P28223 | HTR2A | 5-hydroxytryptamine receptor 2A | binder | targets |
| P28335 | HTR2C | 5-hydroxytryptamine receptor 2C | binder | targets |
| P23975 | SLC6A2 | Sodium-dependent noradrenaline transporter | inhibitor | targets |