Molecules, 2017 As a G-protein coupled receptor, the 5-hydroxytryptamine 2A (5-HT2A) receptor is known for its critical role in the cognitive, behavioural and physiological functions, and thus is a primary molecular target to treat psychiatric diseases, including ...
Feng Lin +6 more
doaj +2 more sources
Interaction of arylpiperazine ligands with the hydrophobic part of the 5-HT1A receptor binding site
Bioorganic and Medicinal Chemistry, 2006 A flexible docking of a series of arylpiperazine derivatives with structurally different aryl part to the binding site of a model of human 5-HT1A receptor was exercised.
Vladimir Sukalovic +2 more
exaly +2 more sources
Protective mechanism of arylpiperazine dopaminergic D2ligands on nitric oxide and 6-hydroxydopamine induced SH-SY5Y human neuroblastoma cell death [PDF]
, 2012 U ovom radu je ispitivan uticaj 20 novosintetisanih arilpiperazinskihdopaminergičkih liganada na vijabilnost humanih SH-SY5Y neuroblastomskih ćelijatretiranih donorom azot monoksida (engl. nitric oxide, NO) natrijum nitroprusidom(engl.
Tovilović-Kovačević, Gordana
core +7 more sources
Molecules, 2015 Indole-arylpiperazine derivatives have exhibited good selectivity for the α1A-adrenoceptor, but the structure-activity-binding mechanism relationship remains unclear.
Wei Xu +5 more
doaj +3 more sources
Novel 4,5-Dihydrothiazole-Phenylpiperazine Derivatives: Synthesis, Docking Studies and Pharmacological Evaluation as Serotonergic Agents. [PDF]
ChemMedChemThe 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‐
Andreozzi G +18 more
europepmc +2 more sources
Modeling interactions of α1a adrenergic receptor and different arylpiperazine ligands
, 2012 Molecular modelling studies were undertaken in order to identify key interactions of selected ligands with α1A adrenergic receptor, responsible for their binding and presumably receptor activation. The previously made model of α1A adrenergic receptor was
Senćanski, Milan V. +9 more
core +11 more sources
Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry. [PDF]
ChemistryOpenPiperazine‐based bioactive molecules represent a versatile class of compounds with broad therapeutic potential. Structural modification of the piperazine scaffold governs key structure–activity relationships, enabling antibacterial, antifungal, antitumor, neuroactive, and anti‐inflammatory activities.
Ten A +5 more
europepmc +2 more sources
Molecular Modeling of 5HT2AReceptor – Arylpiperazine Ligands Interactions
Chemical Biology and Drug Design, 2014 In this paper, we report the molecular modeling of the 5HT(2A) receptor and the molecular docking of arylpiperazine-like ligands. The focus of the research was on explaining the effects the ligand structure has on the binding properties of the 5HT(2A ...
Vladimir Sukalovic, Milan Senćanski
exaly +2 more sources
Exploring in silico drug design and pharmacokinetics study for identification of potent antidepressant agents [PDF]
Journal of Chemistry Letters, 2020 In furtherance to our previous study, in silico drug design and pharmacokinetics study were employed on some arylpiperazine derivatives as inhibitors of serotonin transporter (SERT) for identification of potential antidepressant agents.
Sabitu Babatunde Olasupo +3 more
doaj +1 more source
Influence of N–1 substituent properties on binding affinities of arylpiperazines to the binding site of 5-HT1A receptor [PDF]
Journal of the Serbian Chemical Society, 2006 Serotonin receptors (5-HTRs), especially the 5-HT1A subtype, have been the subject of intensive research for the past decade, due to their function in human physiology.
MARIO V. ZLATOVIC +4 more
doaj +3 more sources