56296-18-5

Usage

Uses

Used in Pharmaceutical Industry:
11-Piperazinyldibenzo[b,e][1,4]diazepine is used as a DREADD agonist for the activation of hM3Dq, a designer receptor exclusively activated by designer drugs (DREADDs). It selectively binds to hM3Dq DREADDs over endogenous hM3 receptors, making it a valuable tool in the development of targeted drug therapies.
Used in Research Applications:
In the field of neuroscience and pharmacology, 11-Piperazinyldibenzo[b,e][1,4]diazepine is used as a research tool to study the function and modulation of hM3Dq receptors. Its selective binding properties allow for the investigation of receptor signaling pathways and the development of novel therapeutic strategies.
Used in Drug Design and Development:
11-Piperazinyldibenzo[b,e][1,4]diazepine serves as a key component in the design and development of new drugs targeting the hM3Dq receptor. Its unique binding profile can be leveraged to create more effective and selective medications with fewer side effects.
Used in Drug Delivery Systems:
Similar to gallotannin, 11-Piperazinyldibenzo[b,e][1,4]diazepine can be incorporated into drug delivery systems to improve its bioavailability and therapeutic outcomes. Various organic and metallic nanoparticles can be employed as carriers for the compound, enhancing its delivery to target cells and tissues.

Upstream product

• 5814-41-5 5,10-dihydro-11H-dibenzo[b,e][1,4]-diazepin-11-one 
• 27696-24-8 2-(2-aminophenylamino)benzoic acid 
• 609-73-4 o-nitroiodobenzene 
• 110-85-0 piperazine 
• 50373-21-2 11-chloro-5H-dibenzo[b,e][1,4]diazepine 
• 1493-27-2 ortho-nitrofluorobenzene 
• 118-92-3 anthranilic acid 
• 5933-35-7 N-(2-nitrophenyl)anthranilic acid 

Relevant academic research and scientific papers

The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs

Over the past decade, two independent technologies have emerged and been widely adopted by the neuroscience community for remotely controlling neuronal activity: optogenetics which utilize engineered channelrhodopsin and other opsins, and chemogenetics which utilize engineered G protein-coupled receptors (Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)) and other orthologous ligand-receptor pairs. Using directed molecular evolution, two types of DREADDs derived from human muscarinic acetylcholine receptors have been developed: hM3Dq which activates neuronal firing, and hM4Di which inhibits neuronal firing. Importantly, these DREADDs were not activated by the native ligand acetylcholine (ACh), but selectively activated by clozapine N-oxide (CNO), a pharmacologically inert ligand. CNO has been used extensively in rodent models to activate DREADDs, and although CNO is not subject to significant metabolic transformation in mice, a small fraction of CNO is apparently metabolized to clozapine in humans and guinea pigs, lessening the translational potential of DREADDs. To effectively translate the DREADD technology, the next generation of DREADD agonists are needed and a thorough understanding of structure-activity relationships (SARs) of DREADDs is required for developing such ligands. We therefore conducted the first SAR studies of hM3Dq. We explored multiple regions of the scaffold represented by CNO, identified interesting SAR trends, and discovered several compounds that are very potent hM3Dq agonists but do not activate the native human M3 receptor (hM3). We also discovered that the approved drug perlapine is a novel hM3Dq agonist with >10000-fold selectivity for hM3Dq over hM3.

Synthesis of 11-(Piperazin-1-yl)-5H-dibenzo[b,e] [1,4]diazepine on kilo scale

A synthesis of 11-(piperazin-1yl)-5H-dibenzo[b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization. Copyright E-Journal o

AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS

Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

USE OF N-DESMETHYLCLOZAPINE AND RELATED COMPOUNDS AS DOPAMINE STABILIZING AGENTS

Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.

AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS

Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.