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- Nelotanserin
Nelotanserin API Manufacturers & Suppliers
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Nelotanserin | CAS No: 839713-36-9 | GMP-certified suppliers
A medication that targets neurodegenerative and neuropsychiatric disorders by selectively modulating serotonin receptors to improve sleep quality and reduce psychotic symptoms without typical sedative effects.
Therapeutic categories
Product Snapshot
- Nelotanserin is an oral small molecule compound
- It is primarily investigated for its potential use in treating neuropsychiatric disorders
- The product is currently in the investigational phase and has not received regulatory approval from FDA or EMA
Clinical Overview
The mechanism of action for nelotanserin involves potent blockade of the 5-HT2A receptor, a critical component in central nervous system signaling pathways. By inhibiting this receptor, nelotanserin modulates neurotransmission implicated in sleep regulation and psychotic symptoms. Unlike treatment options that modulate GABA-A receptors, nelotanserin does not engage this pathway, potentially reducing typical sedative or cognitive side effects associated with GABAergic drugs.
Pharmacodynamic data indicate that nelotanserin enhances non-REM sleep—the phase considered most restorative—without suppressing REM or dream sleep. This distinct sleep architecture effect differentiates it from other sedative or hypnotic agents used in related symptom management. Nelotanserin structurally belongs to the phenylpyrazole class, comprising a pyrazole ring bound to a phenyl group, and chemically is classified among amides and benzene derivatives.
Safety and toxicity profiles remain under investigation given its investigational status; however, the selective receptor targeting profile suggests a lower risk of side effects commonly seen with less selective serotonergic or GABAergic agents. As clinical development continues, comprehensive evaluations of tolerability, long-term safety, and drug interactions will inform its clinical utility.
From a procurement perspective, sourcing nelotanserin API requires attention to stringent quality standards due to its investigational use and complex chemical structure. Suppliers should provide certificates of analysis that confirm purity, identity, and compliance with regulatory guidelines for research-grade material. Robust supply chain management is essential to ensure consistency and reliability for ongoing clinical development programs.
Identification & chemistry
| Generic name | Nelotanserin |
|---|---|
| Molecule type | Small molecule |
| CAS | 839713-36-9 |
| UNII | 4ZA73QEW2P |
| DrugBank ID | DB12555 |
Pharmacology
| Summary | Nelotanserin is a selective antagonist of the 5-hydroxytryptamine receptor 2A (5-HT2A), modulating serotonergic signaling in the central nervous system. Its mechanism involves inhibition of 5-HT2A-mediated stimulatory pathways, aiming to alter neural activity without engaging GABA-A receptor systems. This selective targeting underpins its therapeutic potential in disorders linked to serotonin dysregulation. |
|---|---|
| Mechanism of action | Nelotanserin potently and selectively targets the 5-HT2A serotonin receptor, blocking a stimulatory pathway of the central nervous system. This mechanism is not expected to have the side effects of the GABA-A treatments. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 2A | Humans |
Formulation & handling
- Nelotanserin is a small molecule with low aqueous solubility, indicating potential formulation challenges for oral bioavailability. Due to its chemical class and physicochemical properties, it is suitable for oral administration rather than parenteral routes. Attention should be given to solubility enhancement techniques and stability under ambient storage conditions.
Regulatory status
Nelotanserin is a type of Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
