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Novel Multimodal Salicylamide Derivative with Antidepressant-like, Anxiolytic-like, Antipsychotic-like, and Anti-Amnesic Activity in Mice.
Pharmaceuticals (Basel)
January 2023
Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.
Depression, anxiety, and schizophrenia may coexist in psychiatric patients. Moreover, these disorders are very often associated with cognitive impairments. However, pharmacotherapy of these conditions remains challenging due to limited drug effectiveness or numerous side effects.
View Article and Find Full Text PDFDiscovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Eur J Med Chem
April 2023
Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modeling Laboratory, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki St., PL-20093, Lublin, Poland; School of Pharmacy, University of Eastern Finland, P.O. Box 1627, FI-70211, Kuopio, Finland. Electronic address:
Schizophrenia is a mental disorder with a complex pathomechanism involving many neurotransmitter systems. Among the currently used antipsychotics, classical drugs acting as dopamine D receptor antagonists, and drugs of a newer generation, the so-called atypical antipsychotics, can be distinguished. The latter are characterized by a multi-target profile of action, affecting, apart from the D receptor, also serotonin receptors, in particular 5-HT and 5-HT.
View Article and Find Full Text PDFAntipsychotic- and Anxiolytic-like Properties of a Multimodal Compound JJGW08 in Rodents.
Int J Mol Sci
December 2022
Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.
Schizophrenia is a chronic mental illness, which remains difficult to treat. A high resistance to the available therapies, their insufficient efficacy, and numerous side effects are the reasons why there is an urgent need to develop new antipsychotics. This study aimed to assess the antipsychotic-like effects of JJGW08, a novel arylpiperazine alkyl derivative of salicylamide, in rodents.
View Article and Find Full Text PDFDesign and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties.
Molecules
February 2022
Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.
Long-chain arylpiperazine scaffold is a versatile template to design central nervous system (CNS) drugs that target serotonin and dopamine receptors. Here we describe the synthesis and biological evaluation of ten new arylpiperazine derivatives designed to obtain an affinity profile at serotonin 5-HT, 5-HT, 5-HT receptor, and dopamine D receptor of prospective drugs to treat the core symptoms of autism spectrum disorder (ASD) or psychosis. Besides the structural features required for affinity at the target receptors, the new compounds incorporated structural fragments with antioxidant properties to counteract oxidative stress connected with ASD and psychosis.
View Article and Find Full Text PDFChemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.
Bioorg Med Chem
May 2020
Department of Medicinal Chemistry, Maj Institute of Pharmacology of the Polish Academy of Sciences, 12 Smętna Street, Cracow 31-343, Poland.
In the pharmacotherapy of schizophrenia, there is a lack of effective drugs, and currently used agents cause a large number of side effects. The D, 5-HT, 5-HT receptors are among the most important receptor targets in the treatment of schizophrenia, but antagonism at 5-HT and 5-HT receptors may bring about additional improvement of cognitive functions. However, doubt exists regarding the importance of 5-HTR in the pharmacotherapy.
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