Antianxiety Agents (Neuroleptics)

An Investigation into Formation of Impurities During Synthesis of Blonanserin

“…18 (2014), 5928-5930 120 mL, layers separated product in aqueous, then adjusted pH 9 with 30 % NaOH Solution then extracted compound with ethylacetate 2 × 500 mL, combined organic layer washed with water, distilled organic layer a white crystalline compound obtained, the crude purified with isopropyl alcohol to get 71.5 g, yield 86 % obtained. To a mixture of potassium iodide 5.5 g, piperazine 18.6 g and 10 g of 2 was heated to 165-170 °C for 8 h, cool to room temperature then water 30 mL and ethylacetate 150 mL was added stirred reaction mass for 15 min separated organic layer then extracted with water using of hydrochloric acid solution 18.5 mL, layers separated product in aqueous, then adjusted pH 9 with 30 % NaOH solution then extracted compound with ethylacetate 2 × 150 mL, combined organic layer washed with water, distilled organic layer a white crystalline compound obtained, the crude purified with ethanol to get yield 8.5 g. 1 During our preliminary optimization studies, we have observed four major impurity in the final product and the molecular weights of these impurities were identified by LC-MS analysis as 339, 461, 383 & 385 and 349 were identified as Des ethyl impurity, di-N-ethylpiperazine impurity, chloro impurity and des-fluoro impurity respectively. The structure was further confirmed through synthesis/isolation from mother liquor, characterization and HPLC spike studies.…”

Sensitive Analysis of Blonanserin, a Novel Antipsychotic Agent, in Human Plasma by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry

“…[1][2][3][4][5][6] It is one of the secondgeneration antipsychotic agents, together with risperidone and olanzapine, it is effective in the treatment of both positive and negative symptoms of schizophrenia without extra-pyramidal symptoms, but has original properties of affinity higher for the dopamine D2 receptor than for the serotonin 5-HT2A receptor. [1][2][3][4]6,7 On the other hand, blonanserin is much less potent in adrenergic-α1, histamine H1 and muscarinic M1 antagonist activities. 6 Such a pharmacological profile shows that blonanserin is more specific to the dopamine D2 and serotonin 5-HT2A receptors with fewer side effects; its excellent effects on schizophrenia have been reported in many reports.…”

A Review of Current Drug Targets and Pharmacology of Antipsychotic Treatment

“…A few agents have recently entered phase III trials; bifeprunex (DU 127090), blonanserin (AD 5423) and asenapine (ORG 5222). Bifeprunex is a mixed dopamine antagonist/serotonin agonist, blonanserin is a D 2 antagonist and a weak antagonist of D 2 , 5HT and noradrenaline uptake systems, and asenapine antagonizes D 2 , 5HT 2A and alpha I adrenergic receptors [60][61][62]. A handful of compounds are in phase I and phase II trials with different targets for drug action.…”