1‐Cinnamyl‐4‐(2‐methoxyphenyl)piperazines: Synthesis, Binding Properties, and Docking to Dopamine (D2) and Serotonin (5‐HT1A) Receptors

J Penjišević, V Šukalović, D Andrić… - … der Pharmazie: An …, 2007 - Wiley Online Library
Clinical properties of atypical antipsychotics are based on their interaction with D2
dopamine receptor and serotonin 5‐HT1A and 5‐HT2A receptors. As a part of our research …

Affinity of aporphines for the human 5-HT2A receptor: insights from homology modeling and molecular docking studies

S Pecic, P Makkar, S Chaudhary, BV Reddy… - Bioorganic & medicinal …, 2010 - Elsevier
Analogs of nantenine were docked into a modeled structure of the human 5-HT2A receptor
using ICM Pro, GLIDE, and GOLD docking methods. The resultant docking scores were …

Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors

MR Pullagurla, RB Westkaemper… - Bioorganic & medicinal …, 2004 - Elsevier
A graphics model of the human 5-HT6 receptor was constructed and automated docking
studies were performed. The model suggests that 5-HT6 antagonist arylsulfonyltryptamines …

Synthesis, pharmacophore modeling, and biological evaluation of novel 5H-thiazolo [3, 2-a] pyrimidin-5-one derivatives as 5-HT2A receptor antagonists

FM AWADALLAH - Scientia Pharmaceutica, 2008 - mdpi.com
Abstract Novel 5 H-thiazolo [3, 2-a] pyrimidin-5-one derivatives linked through an ethylene
bridge to various phenylpiperazine groups were prepared for evaluation as 5-HT 2A …

[HTML][HTML] Mechanism Exploration of Arylpiperazine Derivatives Targeting the 5-HT2A Receptor by In Silico Methods

F Lin, F Li, C Wang, J Wang, Y Yang, L Yang, Y Li - Molecules, 2017 - mdpi.com
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 …

Revised Pharmacophore Model for 5-HT2A Receptor Antagonists Derived from the Atypical Antipsychotic Agent Risperidone

UH Shah, SA Gaitonde, JL Moreno… - ACS Chemical …, 2019 - ACS Publications
Pharmacophore models for 5-HT2A receptor antagonists consist of two
aromatic/hydrophobic regions at a given distance from a basic amine. We have previously …

[PDF][PDF] Quantitative prediction of counter attack profiles for (Z)-N, N-dimethyl-2-(perfluorophenyl)-2-(2-phenylhydrazinylidine) acetamide using the GUSAR program

UF Askerova - UNEC Journal of Engineering and Applied Sciences, 2022 - unec-jeas.com
There are a sufficient number of theories about the nature of physiological effect, such us
receptor, neural, biochemical, physicochemical to quantum. All of them are true, because …

2, 5-Disubstituted pyridines: The discovery of a novel series of 5-HT2A ligands

KJ Wilson, MB van Niel, L Cooper, D Bloomfield… - Bioorganic & medicinal …, 2007 - Elsevier
This report describes the effect of replacing the central basic amine present in many known
5-HT2A ligands with an aromatic residue. We targeted the isomeric phenethylpyridines 2 …

Structural determinants for high 5-HT2A receptor affinity of spiro [9, 10-dihydroanthracene]-9, 3′-pyrrolidine (SpAMDA)

S Peddi, BL Roth, RA Glennon… - Bioorganic & medicinal …, 2004 - Elsevier
The synthesis and 5-HT2A receptor affinities of ring altered derivatives of spiro [9, 10-
dihydroanthracene]-9, 3′-pyrrolidine (4), a structurally unique tetracyclic 5-HT2A receptor …

Reformulating a Pharmacophore for 5-HT2A Serotonin Receptor Antagonists

J Younkin, SA Gaitonde, A Ellaithy… - ACS chemical …, 2016 - ACS Publications
Several pharmacophore models have been proposed for 5-HT2A serotonin receptor
antagonists. These typically consist of two aromatic/hydrophobic moieties separated by a …