Nelotanserin - CAS 839713-36-9
Catalog number: 839713-36-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H15BrF2N4O2
Molecular Weight:
437.24
COA:
Inquire
Targets:
5-HT Receptor
Description:
Nelotanser is Serotonin 2A receptor inverse agonist. In Aug 2016, Axovant Sciences initiated a phase-II clinical trial in Lewy body disease in USA.
Purity:
98%
Appearance:
Powder
Synonyms:
1-[3-(4-bromo-2-methylpyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea;APD 125
Solubility:
DMSO: ≥ 32 mg/mL
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Lewy body disease
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
COSPVUFTLGQDQL-UHFFFAOYSA-N
InChI:
InChI=1S/C18H15BrF2N4O2/c1-25-17(13(19)9-22-25)12-8-11(4-6-16(12)27-2)23-18(26)24-15-5-3-10(20)7-14(15)21/h3-9H,1-2H3,(H2,23,24,26)
Canonical SMILES:
CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC
Current Developer:
Arena Pharmaceuticals; Axovant Sciences
1.New Therapeutic Strategies for Lewy Body Dementias.
Velayudhan L;Ffytche D;Ballard C;Aarsland D Curr Neurol Neurosci Rep. 2017 Sep;17(9):68. doi: 10.1007/s11910-017-0778-2.
This article reviews current treatment strategies and recent advances for the Lewy body dementias (LBDs). Current available symptom treatment strategies are based on monoaminergic, cholinergic and glutaminergic neurotransmitter systems. Relatively robust evidence exists for cholinesterase inhibitors for cognitive impairment in LBD and in Parkinson's disease for antidepressants, clozapine and recently pimavanserin for psychosis. interpidine (RVT 101) and nelotanserin are currently under investigation. Non-pharmacological interventions, such as cognitive stimulation, physical exercises and neuromodulation strategies, may be useful in Parkinson's disease but have not yet been tested in dementias. Disease-modifying approaches are aimed at preventing, slowing or ameliorating the production, aggregation and deposition of pathological proteins, including immunotherapy targeting α-synuclein and an ongoing trial using ambroxol which increases glucocerebrosidase activity to lower the levels of the protein alpha-synuclein. Other disease-modifying clinical trials are using agents to augment insulin signalling, stem cell therapy, reducing amyloid pathology and gene therapy.
2.Serotonergic Approaches in Parkinson's Disease: Translational Perspectives, an Update.
Huot P;Sgambato-Faure V;Fox SH;McCreary AC ACS Chem Neurosci. 2017 May 17;8(5):973-986. doi: 10.1021/acschemneuro.6b00440. Epub 2017 May 5.
Parkinson's disease (PD) has long been seen as a disorder caused by degeneration of the dopaminergic system, leading to the classic motor manifestations of the disease. However, there is now overwhelming evidence that PD is more than a disease merely caused by dopamine depletion. It is well-known that a myriad of other neurotransmitters are affected by the disease process. One such neurotransmitter is serotonin (5-HT). 5-HT has been shown to play a role in several motor and nonmotor manifestations of PD, including tremor, cognition, depression and psychosis. 5-HT also seems to play a critical role in L-3,4-dihydroxyphenylalanine (L-DOPA)-induced dyskinesia. A breadth of preclinical studies and clinical trials have been conducted that aimed at modulating the 5-HT system in order to alleviate depression, cognitive deficits, psychosis, and dyskinesia. In this Review, we summarize recent advances in the 5-HT field in PD, but with a translational emphasis. We start by presenting a novel nonhuman primate model of PD that presents with dual dopamine and 5-HT lesions. We then present preclinical and clinical data that introduce new concepts, such as the use of biased and partial agonists, as well as molecules recently introduced to the field of PD, such as eltoprazine, pimavanserin, nelotanserin, and SYN-120, to enhance therapeutic benefit while minimizing adverse events, notably on parkinsonian disability.
3.Insomnia in Elderly Patients: Recommendations for Pharmacological Management.
Abad VC;Guilleminault C Drugs Aging. 2018 Sep;35(9):791-817. doi: 10.1007/s40266-018-0569-8.
Chronic insomnia affects 57% of the elderly in the United States, with impairment of quality of life, function, and health. Chronic insomnia burdens society with billions of dollars in direct and indirect costs of care. The main modalities in the treatment of insomnia in the elderly are psychological/behavioral therapies, pharmacological treatment, or a combination of both. Various specialty societies view psychological/behavioral therapies as the initial treatment intervention. Pharmacotherapy plays an adjunctive role when insomnia symptoms persist or when patients are unable to pursue cognitive behavioral therapies. Current drugs for insomnia fall into different classes: orexin agonists, histamine receptor antagonists, non-benzodiazepine gamma aminobutyric acid receptor agonists, and benzodiazepines. This review focuses on Food and Drug Administration (FDA)-approved drugs for insomnia, including suvorexant, low-dose doxepin, Z-drugs (eszopiclone, zolpidem, zaleplon), benzodiazepines (triazolam, temazepam), and ramelteon. We review the indications, dosing, efficacy, benefits, and harms of these drugs in the elderly, and discuss data on drugs that are commonly used off-label to treat insomnia, and those that are in clinical development.
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CAS 839713-36-9 Nelotanserin

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