Results 41 to 50 of about 605 (157)

Microwave-Assisted Synthesis of Trazodone and Its Derivatives as New 5-HT_1A Ligands: Binding and Docking Studies

Molecules, 2019
Trazodone, a well-known antidepressant drug widely used throughout the world, works as a 5-hydroxytryptamine (5-HT2) and α1-adrenergic receptor antagonist and a serotonin reuptake inhibitor.
Jolanta Jaśkowska, Przemysław Zaręba, Paweł Śliwa, Edyta Pindelska, Grzegorz Satała, Zbigniew Majka   +5 more
doaj   +1 more source

Novel 4,5‐Dihydrothiazole‐Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents

ChemMedChem, Volume 20, Issue 15, August 2, 2025.
The synthesis of a new series of 4,5‐dihydrothiazol‐2‐ylphenylpiperazine derivatives as serotoninergic ligands is described and tested for their affinity toward 5‐HT1A, 5‐HT2A,and 5‐HT2C and selected for further in vivo assays to determine their functional activity. The pharmacological studies highlight that among the developed derivatives, FG‐7 and FG‐
Giorgia Andreozzi, Natalia Karkoszka, Rosa Sparaco, Angela Corvino, Beatrice Severino, Vincenzo Santagada, Elisa Magli, Ewa Gibuła‐Tarłowska, Jolanta H. Kotlińska, Kinga Gawel, Raffaele Capasso, Anna Lesniak, Nataliia Semenko, Agnieszka A. Kaczor, Anna Bielenica, Grażyna Biała, Giuseppe Caliendo, Ewa Kędzierska, Ferdinando Fiorino   +18 more
wiley   +1 more source

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Molecules, 2011
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically ...
William L. Scott, Ziniu Zhou, Martin J. O’Donnell, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Gaël Nomezine, Maciej Pawłowski, Gilles Subra, Katarzyna Grychowska, Joanna Król, Paweł Zajdel   +11 more
doaj   +1 more source

Towards the convergent therapeutic potential of G protein‐coupled receptors in autism spectrum disorders

British Journal of Pharmacology, Volume 182, Issue 14, Page 3044-3067, July 2025.
Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crépieux, Lucie P. Pellissier   +6 more
wiley   +1 more source

The translational value of ligand‐receptor binding kinetics in drug discovery

British Journal of Pharmacology, Volume 181, Issue 21, Page 4117-4129, November 2024.
Abstract The translation of in vitro potency of a candidate drug, as determined by traditional pharmacology metrics (such as EC50/IC50 and KD/Ki values), to in vivo efficacy and safety is challenging. Residence time, which represents the duration of drug‐target interaction, can be part of a more comprehensive understanding of the dynamic nature of drug‐
Hongli Liu, Haoran Zhang, Adriaan P. IJzerman, Dong Guo   +3 more
wiley   +1 more source

An approximate linear solvation energy relationships model based on Snyder's selectivity parameters. Chromatographic behavior of some 1-aralkyl-4-arylpiperazines

, 2008
In order to elucidate the influence of the mobile phase composition on the retention of some 1-aralkyl-4-arylpiperazines, Snyder's selectivity and polarity concept for building a simple linear solvation energy relationships model of chromatographic ...
Andrić, Filip, Živoslav Lj. Tešić, Trifković, Jelena, Milojković-Opsenica, Dušanka, Tešić, Živoslav Lj., Jelena Đ. Trifković, Dusanka M. Milojković-Opsenica, Filip Lj. Andrić   +7 more
core   +1 more source

TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer

Molecular Oncology, Volume 18, Issue 8, Page 1980-2000, August 2024.
The androgen receptor (AR) antagonist TAS3681 is effective against AR mutations, which leads to agonistic activity of AR signal inhibitors, and had an antitumor effect in an AR‐splice variant 7 (AR‐V7)‐positive enzalutamide‐resistant xenograft model. TAS3681 suppresses aberrant AR activation, including AR overexpression and expression of constitutively
Shohei Yoshida, Daisuke Kajiwara, Masanao Seki, Manabu Tayama, Yuki Tanaka, Hiroya Mizutani, Ryoto Fujita, Keisuke Yamamura, Shigeo Okajima, Masanori Asai, Kazuhisa Minamiguchi   +10 more
wiley   +1 more source

Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.

, 1996
A set of 280 5-HT1A receptor ligands were selected from available literature data according to predefined criteria and subjected to three-dimensional quantitative structure-affinity relationship analysis using comparative molecular field analysis.
Gaillard, P., Schambel, P., Carrupt, P.A., Testa, B.   +3 more
core   +2 more sources

Discovery of Bishomo(hetero)arylpiperazines as Novel Multifunctional Ligands Targeting Dopamine D-3 and Serotonin 5-HT1A and 5-HT2A Receptors

, 2010
As a continuation of our efforts to develop innovative ligands for D 3, 5-HT1A, and 5-HT2A receptors with low propensity to block hERG channels, we propose a series bishetero(homo) arylpiperazines 5a-m as novel and potent multifunctional ligands ...
CAMPIANI G., FRANCESCHINI S., FATTORUSSO C., JACOBSEN T. A., BUTINI S., NOVELLINO E., FATTORUSSO, CATERINA, MADSEN K., KUMAR V., BORRELLI G., TROTTA F., Jacobsen T. ., NOVELLINO, ETTORE, Scheel Kruger J., SANDAGER-NIELSEN K., Gemma S. ., PERSICO M., FIORINI I., SCHEEL-KRUGER J., ORTECA N., GEMMA S., Sandager Nielsen K., PERSICO, MARCO, GUARINO E.   +23 more
core   +1 more source

Synthesis of Benzo[b]thiophene Carboxamides Connected to 4‐Arylpiperazines through a Benzylic Spacer: Potential Ligands with 5‐HT_1A Binding Affinity

, 2007
New benzothiophene arylpiperazine derivatives 8 (a-f) were synthesized as potential serotoninergic agents with 5-HT1A receptor affinity. Preparation of the derivatives was performed by treating N-[2-(chloromethyl)phenyl]-4,7-dimethoxybenzo[b]thiophene-2 ...
Acevedo, R., Hernán Pessoa‐Mahana, Pessoa Mahana, C. David, Saitz, Claudio, Claudio Saitz, Ramiro Araya‐Maturana, R. Acevedo, Pessoa Mahana, Hernan, Araya Maturana, Ramiro, C. David Pessoa‐Mahana   +9 more
core   +1 more source