Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors

Zajdel, Paweł; Marciniec, Krzysztof; Maślankiewicz, Andrzej; Grychowska, Katarzyna; Satała, Grzegorz; Duszyńska, Beata; Lenda, Tomasz; Siwek, Agata; Nowak, Gabriel; Partyka, Anna; Wróbel, Dagmara; Jastrzębska-Więsek, Magdalena; Bojarski, Andrzej J.; Wesołowska, Anna; Pawłowski, Maciej

doi:10.1016/j.ejmech.2012.11.042

Cited by 87 publications

(72 citation statements)

References 22 publications

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“…The tested compounds were synthesized in the Department of Medicinal Chemistry, Jagiellonian University Medical College by Zajdel et al 17,18 The compounds structures were established previously on the basis of CHN elemental analysis and spectral data ( 1 HNMR and mass spectra). Dimethylsulfoxide (DMSO) of high grade purity (99,9%) was obtained from Merck, (Darmstadt, Germany).…”

Section: Tested Compounds and Chemicalsmentioning

confidence: 99%

“…Thus, the present study was designed to evaluate the mutagenic and antimutagenic properties of the newly synthesized quinoline-and isoquinoline-sulfonamide analogs of aripiprazole (1-8) (Table 1) which behave as multimodal dopamine/serotonin agents and display antidepressant, anxiolytic, and/or antipsychotic properties. [17][18][19] Focusing on the application of alternative in vitro and in silico test methods to predict compounds mutagenicity in the present study the Vibrio harveyi assay and OSIRIS Property Explorer software were employed. Additionally, the Ames test was used as the reference.…”

Section: Introductionmentioning

confidence: 99%

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Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

Powroźnik¹,

Słoczyńska²,

Marciniec³

et al. 2016

Adv Pharm Bull

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IntroductionOver the last decades the involvement of reactive oxygen species (ROS) in the molecular mechanisms related to psychiatric disorders such as depression or schizophrenia became evident. [1][2][3] In rat models of depression a decreased activity of antioxidant enzymes such as glutathione peroxidase (GSH-Px) followed by increased lipid peroxidation were observed. [4][5][6] Furthermore, in patients with depression the elevated plasma ROS levels were observed to effectively amplify oxidative stress.

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Section: Tested Compounds and Chemicalsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

Powroźnik¹,

Słoczyńska²,

Marciniec³

et al. 2016

Adv Pharm Bull

Self Cite

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“…Several series of aripiprazole analogs, e.g. quinoline-and isoquinoline -amide and sulfonamide -derivatives of long-chain arylpiperazines (LCAPs) have been explored as potential antipsychotic, antidepressant, and anxiolytic agents (Figure 1) [6][7][8] . Among the currently numerous pharmacological approaches for schizophrenia treatments, considerable attention has been focused on 5-HT 6 antagonists.…”

Section: Introductionmentioning

confidence: 99%

Arylpiperazinylalkyl derivatives of 8-amino-1,3-dimethylpurine-2,6-dione as novel multitarget 5-HT/D receptor agents with potential antipsychotic activity

Chłoń-Rzepa

Bucki

Kołaczkowski

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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(2016) Arylpiperazinylalkyl derivatives of 8-amino-1,3-dimethylpurine-2,6-dione as novel multitarget 5-HT/ D receptor agents with potential antipsychotic activity, Journal of Enzyme Inhibition and Medicinal Chemistry, 31:6, 1048-1062, DOI: 10.3109/14756366.2015 , 31, 34, 39, 41, 43, 45, and 46 in the functional in vitro evaluation for all targeted receptors showed significant partial D 2 agonist, partial 5-HT 1A agonist, and 5-HT 2A antagonist properties. The advantageous in vitro affinity of compound 34 for 5-HT 1A and D 2 receptors has been explained by means of molecular modeling, taking into consideration its partial agonist activity towards the latter one. In behavioral studies, compounds 32 and 34 revealed antipsychotic-like properties, significantly decreasing D-amphetamine-induced hyperactivity in mice.

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“…They produce significant antidepressant activity in mice [26]. In particular, 28 also displays remarkable antipsychotic effects in MK-801-induced hyperlocomotor activity in mice.…”

Section: Modification Of the Spacermentioning

confidence: 99%

4WD to Travel Inside the 5-HT1A Receptor World

Quaglia¹,

Cifani²,

Bello³

et al. 2017

Serotonin - A Chemical Messenger Between All Types of Living Cells

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5-HT 1A receptor is one of the most important members of the numerous families of serotoninergic receptors. Though it was the first 5-HT receptor to be identified and cloned, the knowledge of its activation/transduction mechanisms, mediated effects, and connection with other systems is still uncompleted. For this reason, relevant is the study of the four Ws of the title: first of all "who" this receptor is, then "why" it continues to be a so attractive target after several years after its identification, then "where" is 5-HT 1A receptor expressed within the body, and, finally, "what" effects this receptor can elicit under physiological and pathological conditions. Obviously, more and more potent, safe, and selective "drugs" might be discovered once the responses to these questions are given.

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Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors

Cited by 87 publications

References 22 publications

Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

Preliminary Safety Assessment of New Azinesulfonamide Analogs of Aripiprazole using Prokaryotic Models

Arylpiperazinylalkyl derivatives of 8-amino-1,3-dimethylpurine-2,6-dione as novel multitarget 5-HT/D receptor agents with potential antipsychotic activity

4WD to Travel Inside the 5-HT1A Receptor World

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