Chemogenetic modulation of astrocytes and microglia: State‐of‐the‐art and implications in neuroscience

J Bossuyt, Y Van Den Herrewegen, L Nestor, A Buckinx… - Glia, 2023 - Wiley Online Library
Insights into the role astrocytes and microglia play in normal and diseased brain functioning
has expanded drastically over the last decade. Recently, chemogenetic tools have emerged …

Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery

BL Roth, E Lopez, S Beischel, RB Westkaemper… - Pharmacology & …, 2004 - Elsevier
Because psychoactive plants exert profound effects on human perception, emotion, and
cognition, discovering the molecular mechanisms responsible for psychoactive plant actions …

Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors

X Lin, XP Huang, G Chen, R Whaley… - Journal of medicinal …, 2012 - ACS Publications
Of great interest in recent years has been computationally predicting the novel
polypharmacology of drug molecules. Here, we applied an “induced-fit” protocol to improve …

Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to κ-opioid receptors

F Yan, PD Mosier, RB Westkaemper, J Stewart… - Biochemistry, 2005 - ACS Publications
Salvinorin A is a naturally occurring hallucinogenic diterpenoid from the plant Salvia
divinorum that selectively and potently activates κ-opioid receptors (KORs). Salvinorin A is …

[HTML][HTML] A novel antibody targeting the second extracellular loop of the serotonin 5-HT2A receptor inhibits platelet function

JEM Ramirez, AB Alarabi, FT Khasawneh… - International Journal of …, 2022 - mdpi.com
Serotonin (5-hydroxytriptamine or 5-HT) is known to be a weak platelet agonist, and is
involved in thrombus formation. While 5-HT cannot induce platelet aggregation on its own …

5-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1, 3-disubstituted thiourea derivatives

A Bielenica, E Kędzierska, M Koliński, S Kmiecik… - European journal of …, 2016 - Elsevier
A series of 10 thiourea derivatives have been synthesized by the reaction of aromatic amine
with a substituted aryl (compounds 1–3, 6–8) and alkylphenyl (4, 5, 9, 10) isothiocyanates …

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT2A Receptors

AR Blaazer, P Smid, CG Kruse - … : Chemistry Enabling Drug …, 2008 - Wiley Online Library
Agonist activation of central 5‐HT2A receptors results in diverse effects, such as
hallucinations and changes of consciousness. Recent findings indicate that activation of the …

Potential Modes of Interaction of 9-Aminomethyl-9,10-dihydroanthracene (AMDA) Derivatives with the 5-HT2A Receptor: A Ligand Structure-Affinity Relationship …

SP Runyon, PD Mosier, BL Roth… - Journal of medicinal …, 2008 - ACS Publications
The effects of 3-position substitution of 9-aminomethyl-9, 10-dihydroanthracene (AMDA) on
5-HT2A receptor affinity were determined and compared to a parallel series of DOB-like 1 …

Pharmacophore models for metabotropic 5-HT receptor ligands

AJ Bojarski - Current topics in medicinal chemistry, 2006 - ingentaconnect.com
An overview of pharmacophore models, developed for different subtypes of serotonin
receptors belonging to the GPCR family, is presented. Starting with early models for 5-HT1A …

Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28

JW Hulshof, HF Vischer, MHP Verheij… - Bioorganic & medicinal …, 2006 - Elsevier
G-protein coupled receptors encoded by viruses represent an unexplored class of potential
drug targets. In this study, we describe the synthesis and pharmacological characterization …