An electrostatic interaction related to a favorable position of the distal phenyl ring and a phenylalanine residue in the binding pocket would explain the higher 5-HT1A affinity of a 4-phenyl-1,2,3,6-tetrahydropyridine (THP) analogue compared to the corresponding 4-phenylpiperazine analogue. To explore a possible reinforcement of this interaction to increase the affinity for 5-HT1A receptors, different 4-substituted-phenyl analogues were synthesized and tested. The most important increase of affinity is obtained with two electron-donating methyl groups in positions 3 and 5.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027751 | PMC |
| http://dx.doi.org/10.1021/ml4004843 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
How Do the Valency and Radii of Cations Affect the Rheological Properties of Aqueous Solutions of Zwitterionic and Anionic Surfactant Mixtures?
Langmuir
January 2025
Institute of Chemical Technology and Engineering, Faculty of Chemical Technology, Poznan University of Technology, ul. Berdychowo 4, PL 60-965 Poznan, Poland.
Despite extensive research on the use of salts to enhance micellar growth, numerous questions remain regarding the impact of ionic exchange and molecular structure on charge neutralization. This study looks into how certain cations (Na, Ca, and Mg) affect the structure of a cocamidopropyl betaine CAPB and sodium dodecylbenzenesulfonate SDBS surfactant mixture, aiming toward applications in targeted delivery systems. The mixture consists of a zwitterionic surfactant, cocamidopropyl betaine (CAPB), and an anionic surfactant, sodium dodecylbenzenesulfonate (SDBS), combined in varying molar ratios at a total concentration of 200 mM.
View Article and Find Full Text PDFCharacterization of multiple binding sites on microtubule associated protein 2c recognized by dimeric and monomeric 14-3-3ζ.
FEBS J
January 2025
Central European Institute of Technology, Masaryk University, Brno, Czech Republic.
Microtubule associated protein 2 (MAP2) interacts with the regulatory protein 14-3-3ζ in a cAMP-dependent protein kinase (PKA) phosphorylation dependent manner. Using selective phosphorylation, calorimetry, nuclear magnetic resonance, chemical crosslinking, and X-ray crystallography, we characterized interactions of 14-3-3ζ with various binding regions of MAP2c. Although PKA phosphorylation increases the affinity of MAP2c for 14-3-3ζ in the proline rich region and C-terminal domain, unphosphorylated MAP2c also binds the dimeric 14-3-3ζ via its microtubule binding domain and variable central domain.
View Article and Find Full Text PDFA c-type lectin with dual function of immunology and mineralization from the freshwater oyster ( Lea).
Front Immunol
January 2025
Key Laboratory of Freshwater Aquatic Genetic Resources, Ministry of Agriculture and Rural Affairs, Shanghai Ocean University, Shanghai, China.
Background: Shell and pearl formation in bivalves is a sophisticated biomineralization process that encompasses immunological and mineralization aspects, particularly during shell repair and the initial stages of pearl cultivation when a nucleus is inserted. Here, we describe a novel C-type lectin, HcLec1, isolated and characterized from the freshwater pearl mussel Lea.
Methods: Immune challenge, RNA interference (RNAi) experiments, ELISA, and antibacterial assays were employed to investigate the role of HcLec1 in innate immunity.
Bicarbonate use reduces the photorespiration in Ottelia alismoides adapting to the CO-fluctuated aquatic systems.
Physiol Plant
January 2025
Key Laboratory of Aquatic Botany and Watershed Ecology, Wuhan Botanical Garden, Chinese Academy of Sciences, Wuhan, China.
Underwater CO concentration fluctuates extremely in natural water bodies. Under low CO, the unique CO concentrating mechanism in aquatic plants, bicarbonate use, can suppress photorespiration. However, it remains unknown (1) to what extent bicarbonate use reduces photorespiration, (2) how exactly photorespiration varies between bicarbonate-users and CO-obligate users under CO-fluctuated environments, and (3) what are differences in Rubisco characteristics between these two types of aquatic plants.
View Article and Find Full Text PDFDocking Structures Induced by Substitution Motifs of Softwood Xylan at Various Cellulose Surfaces.
Biomacromolecules
January 2025
BOKU-University, Institute of Physics and Materials Science, Vienna, Peter-Jordan-Straße 82, Vienna 1190, Austria.
To understand xylan-cellulose interactions in softwood, the adsorption behavior of hexameric softwood xylan proxies with various substitutions was analyzed on the three surfaces of a hexagonal cellulose microfibril. The study found that all surfaces could bind xylan motifs, showing equally high affinity for the hydrophilic (110) and hydrophobic (100) surfaces and significantly lower affinity for the hydrophilic (11̅0) surface. Unsubstituted xylose hexamers had the highest affinity and most ordered adsorption structures, while substitutions generally reduced the affinity and regularity.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!