1-(5H-dibenzo[b,f]azepin-5-yl)ethan-1-one, also known as **loxitane** or **loxapine**, is an **atypical antipsychotic medication**. It's an important research subject due to its unique mechanism of action and potential for therapeutic applications.
Here's a breakdown of its significance:
**Mechanism of Action:**
* **Dopamine and Serotonin Antagonist:** Loxitane primarily acts as an antagonist of dopamine and serotonin receptors. It exhibits higher affinity for D2 receptors compared to D1, and also blocks 5-HT2 receptors. This dual action is believed to contribute to its antipsychotic effects, while minimizing some of the motor side effects associated with typical antipsychotics.
* **Other Receptor Interactions:** Loxitane also has affinity for other receptors, such as alpha-1 adrenergic and muscarinic receptors, which could explain some of its side effects.
**Therapeutic Applications:**
* **Schizophrenia:** Loxitane is effective in managing positive symptoms of schizophrenia, such as hallucinations and delusions.
* **Other Mental Disorders:** It has also been studied for its potential benefits in treating conditions like bipolar disorder, anxiety disorders, and depression, although evidence is less robust in these areas.
**Research Significance:**
* **Understanding Atypical Antipsychotics:** Loxitane is an important tool for researchers to understand the mechanism of action of atypical antipsychotics and the role of dopamine and serotonin in psychosis.
* **Developing New Antipsychotics:** Research on loxitane and other atypical antipsychotics has paved the way for the development of newer medications with improved efficacy and fewer side effects.
* **Exploring Novel Therapeutic Targets:** Loxitane's unique receptor profile has sparked interest in exploring other targets for treating mental disorders.
**Limitations and Concerns:**
* **Side Effects:** Loxitane can cause several side effects, including sedation, weight gain, extrapyramidal symptoms (movement disorders), and metabolic disturbances.
* **Cardiovascular Risks:** It's important to monitor patients for potential cardiovascular risks associated with loxitane, as it can affect heart rate and blood pressure.
**Overall, 1-(5H-dibenzo[b,f]azepin-5-yl)ethan-1-one (loxapine) is a valuable research tool that has contributed significantly to our understanding of antipsychotic medication and the treatment of mental disorders.** It continues to be a focus of ongoing research, with the aim of developing safer and more effective treatments for these conditions.
| ID Source | ID |
|---|---|
| PubMed CID | 606375 |
| CHEMBL ID | 3103397 |
| CHEBI ID | 192674 |
| SCHEMBL ID | 7980250 |
| Synonym |
|---|
| 1-(11h-benzo[b][1]benzazepin-11-yl)-ethanone |
| 5-ACETYL-5H-DIBENZO[B,F]AZEPINE , |
| SR-01000631565-1 |
| MAYBRIDGE4_003172 |
| HMS1530A04 |
| BRD-K45302550-001-01-4 |
| 1-benzo[b][1]benzazepin-11-ylethanone |
| CHEBI:192674 |
| 1-(5h-dibenzo[b,f]azepin-5-yl)ethan-1-one |
| CCG-41494 |
| bdbm50446082 |
| CHEMBL3103397 , |
| SCHEMBL7980250 |
| n-acetyl-5h-dibenzo[b,f]azepine |
| 5-acetyl-5h-dibenz[b,f]azepine |
| AKOS024359391 |
| 5-acetyl-5h-dibenzo[b,f]azepine # |
| 19209-60-0 |
| 1-{2-azatricyclo[9.4.0.0(3),?]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-yl}ethan-1-one |
| 3W-1547 |
| 5-acetyl-5h-dibenz(b,f)azepine |
| iminostilbene acetate |
| 1-{2-azatricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,9,12,14-heptaen-2-yl}-1-ethanone |
| 1-(5h-dibenzo[b,f]azepine-5-yl)ethanone |
| Class | Description |
|---|---|
| dibenzooxazepine | An organic heterotricyclic compound consisting of two benzene rings fused to a seven-membered ring containing one oxygen and one nitrogen atom. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| P2X purinoceptor 4 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.1560 | 2.9352 | 6.1000 | AID1064727 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| purinergic nucleotide receptor activity | P2X purinoceptor 4 | Homo sapiens (human) |
| extracellularly ATP-gated monoatomic cation channel activity | P2X purinoceptor 4 | Homo sapiens (human) |
| signaling receptor binding | P2X purinoceptor 4 | Homo sapiens (human) |
| copper ion binding | P2X purinoceptor 4 | Homo sapiens (human) |
| protein binding | P2X purinoceptor 4 | Homo sapiens (human) |
| ATP binding | P2X purinoceptor 4 | Homo sapiens (human) |
| zinc ion binding | P2X purinoceptor 4 | Homo sapiens (human) |
| identical protein binding | P2X purinoceptor 4 | Homo sapiens (human) |
| cadherin binding | P2X purinoceptor 4 | Homo sapiens (human) |
| ligand-gated calcium channel activity | P2X purinoceptor 4 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| lysosomal membrane | P2X purinoceptor 4 | Homo sapiens (human) |
| plasma membrane | P2X purinoceptor 4 | Homo sapiens (human) |
| membrane | P2X purinoceptor 4 | Homo sapiens (human) |
| cell junction | P2X purinoceptor 4 | Homo sapiens (human) |
| neuronal cell body | P2X purinoceptor 4 | Homo sapiens (human) |
| terminal bouton | P2X purinoceptor 4 | Homo sapiens (human) |
| dendritic spine | P2X purinoceptor 4 | Homo sapiens (human) |
| cell body | P2X purinoceptor 4 | Homo sapiens (human) |
| perinuclear region of cytoplasm | P2X purinoceptor 4 | Homo sapiens (human) |
| extracellular exosome | P2X purinoceptor 4 | Homo sapiens (human) |
| plasma membrane | P2X purinoceptor 4 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1064724 | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx at 100 uM preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Carbamazepine derivatives with P2X4 receptor-blocking activity. |
| AID1064727 | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Carbamazepine derivatives with P2X4 receptor-blocking activity. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 5 (83.33) | 24.3611 |
| 2020's | 1 (16.67) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (13.13) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||