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Synthesis and biological evaluation of a new class of multi-target heterocycle piperazine derivatives as potential antipsychotics

Lanchang Gao, Chao Hao, Ru Ma, Jiali Chen, Guisen Zhang, Yin Chen

2021RSC Advances16 citationsDOIOpen Access PDF

Abstract

assessment. An animal behavioral study revealed that compound 3w significantly reverses apomorphine-induced climbing and MK-801-induced hyperactivity, and avoidance behavior in the CAR test, with a high threshold for catalepsy. Moreover, compound 3w demonstrates memory enhancement in a novel object recognition task and low liabilities for weight gain and hyperprolactinemia in a long-term metabolic adverse effects model. Thus, 3w was selected as an antipsychotic candidate for further development.

Topics & Concepts

hERGCatalepsyApomorphineAntipsychoticAtypical antipsychoticDopamine receptor D2PharmacologyReceptorDopaminergicPsychologyChemistryNeuroscienceHaloperidolMedicineDopamineInternal medicinePsychiatrySchizophrenia (object-oriented programming)BiochemistryPotassium channelNeuroscience and Neuropharmacology ResearchPharmacological Receptor Mechanisms and EffectsReceptor Mechanisms and Signaling
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