NEFAZODONE - CAS 83366-66-9
Catalog number: 83366-66-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
5-HT Receptor
Nefazodone is a selective serotonin 5-HT2 receptor antagonist. It is an antidepressant under the development of Bristol-Myers Squibb. Its sale was discontinued in some countries due to the rare incidence of hepatotoxicity.
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Crystalline Solid
Soluble in DMSO
-20℃ Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Melting Point:
186 - 188℃
Canonical SMILES:
Current Developer:
Bristol-Myers Squibb
1.Different pH-sensitivity patterns of 30 sodium channel inhibitors suggest chemically different pools along the access pathway.
Lazar A1, Lenkey N2, Pesti K3, Fodor L4, Mike A5. Front Pharmacol. 2015 Sep 25;6:210. doi: 10.3389/fphar.2015.00210. eCollection 2015.
The major drug binding site of sodium channels is inaccessible from the extracellular side, drug molecules can only access it either from the membrane phase, or from the intracellular aqueous phase. For this reason, ligand-membrane interactions are as important determinants of inhibitor properties, as ligand-protein interactions. One-way to probe this is to modify the pH of the extracellular fluid, which alters the ratio of charged vs. uncharged forms of some compounds, thereby changing their interaction with the membrane. In this electrophysiology study we used three different pH values: 6.0, 7.3, and 8.6 to test the significance of the protonation-deprotonation equilibrium in drug access and affinity. We investigated drugs of several different indications: carbamazepine, lamotrigine, phenytoin, lidocaine, bupivacaine, mexiletine, flecainide, ranolazine, riluzole, memantine, ritanserin, tolperisone, silperisone, ambroxol, haloperidol, chlorpromazine, clozapine, fluoxetine, sertraline, paroxetine, amitriptyline, imipramine, desipramine, maprotiline, nisoxetine, mianserin, mirtazapine, venlafaxine, nefazodone, and trazodone.
2.Trazodone in the elderly: risk of extrapyramidal acute events.
Sotto Mayor J1, Pacheco AP1, Esperança S1, Oliveira e Silva A1. BMJ Case Rep. 2015 Jul 14;2015. pii: bcr2015210726. doi: 10.1136/bcr-2015-210726.
Trazodone is a second-generation atypical antidepressant exercising selective inhibitory action on the transport of serotonin. It also has an antagonist effect, similar to nefazodone, on the 5HT1 and 5HT2 receptors, probably due to the therapeutic effects of such substances. It is very effective in the treatment of depression, in anxiety and insomnia. Its known side effects mainly occur with prolonged use of daily doses of 150-200 mg. The ability to enhance drowsiness may be associated with some risk in elderly patients. This clinical case illustrates an acute extrapyramidal event induced by a low dose of trazodone.
3.Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2.
Xu W1, Lim J1, Goh CY1, Suen JY1, Jiang Y1, Yau MK1, Wu KC1, Liu L1, Fairlie DP1. J Chem Inf Model. 2015 Oct 26;55(10):2079-84. doi: 10.1021/acs.jcim.5b00500. Epub 2015 Oct 12.
Virtual screening of a drug database identified Carvedilol, Loratadine, Nefazodone and Astemizole as PAR2 antagonists, after ligand docking and molecular dynamics simulations using a PAR2 homology model and a putative binding mode of a known PAR2 ligand. The drugs demonstrated competitive binding and antagonism of calcium mobilization and ERK1/2 phosphorylation in CHO-hPAR2 transfected cells, while inhibiting IL-6 secretion in PAR2 expressing MDA-MB-231 breast cancer cells. This research highlights opportunities for GPCR hit-finding from FDA-approved drugs.
4.Drug-induced liver injury associated with antidepressive psychopharmacotherapy: An explorative assessment based on quantitative signal detection using different MedDRA terms.
Gahr M1, Zeiss R1, Lang D2, Connemann BJ1, Hiemke C3, Schönfeldt-Lecuona C1. J Clin Pharmacol. 2015 Oct 16. doi: 10.1002/jcph.662. [Epub ahead of print]
Drug-induced liver injury is a major problem of pharmacotherapy and is also frequent with antidepressive psychopharmacotherapy. However, there are only few studies using a consistent methodologic approach to study hepatotoxicity of a larger group of antidepressants. We performed a quantitative signal detection analysis using data from the Uppsala Monitoring Centre from the WHO that records adverse drug reaction (ADR)-data from worldwide sources; we retrieved substance- and country-specific (Australia, France, Germany, Italy, Spain, UK, and USA) ADR-data and calculated reporting odds ratios as measures for disproportionality within a case/non-case approach. To allow for identification of agents that cause severe forms of hepatotoxic ADR we used two different terms of the MeDRA ("Drug related hepatic disorders - comprehensive search" [DRHD-CS] and "… - severe events only" [DRHD-SEO]). Distribution of signals was heterogeneous throughout the different datasets and consistent findings were present only for few substances: agomelatine and tianeptine as well as both positive control agents (amineptine, nefazodone) generated signals related to DRHD-CS and DRHD-SEO in all analysed datasets.
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