AI Article Synopsis
Article Abstract
A series of imidazo[4,5-b]pyridines with a 7-(3-pyridyl) substituent is described as high affinity CRF receptor ligands. Individual analogues were synthesized from key intermediates obtained via palladium-catalyzed coupling of 3-pyridyl zinc or boronic acid organometallic intermediates with 2-benzyloxy-4-chloro-3-nitropyridine 12.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)00835-1 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Regulation and function of the gill corticotropin-releasing factor system during osmoregulatory disturbances in Atlantic salmon.
J Exp Biol
December 2024
Department of Integrative Biology, University of Guelph, 50 Stone Rd E, Guelph, Ontario, Canada.
While corticosteroids, including cortisol, have conserved osmoregulatory functions, the relative involvement of other stress-related hormones in osmoregulatory processes remains unclear. To address this gap, we initially characterized the gill corticotropin-releasing factor (CRF) system of Atlantic salmon (Salmo salar) and then determined: 1) how it is influenced by osmotic disturbances; 2) whether it is affected by cortisol; and 3) which physiological processes it regulates in the gills. Most CRF system components were expressed in the gills with CRF receptor 2 (crfr2a), CRF binding protein (crfbp1 and crfbp2), and urocortin 2 (ucn2a) being the most abundant.
View Article and Find Full Text PDFDevelopment of a Class A/B Hybrid GPCR System for the Proximity-Assisted Screening of GPCR Ligands.
ACS Chem Biol
December 2024
Department Chemistry and Biochemistry Clemens-Schöpf-Institute, Technical University Darmstadt, Peter-Grünberg Straße 4, Darmstadt 64287, Germany.
Class A G protein-coupled receptors (GPCRs) are key mediators in numerous signaling pathways and important drug targets for several diseases. A major shortcoming in GPCR ligand screening is the detection limit for weak binding molecules, which is especially critical for poorly druggable GPCRs. Here, we present a proximity-based screening system for class A GPCRs, which adopts the natural two-step activation mechanism of class B GPCRs.
View Article and Find Full Text PDFContrastive Functional Connectivity Defines Neurophysiology-informed Symptom Dimensions in Major Depression.
bioRxiv
October 2024
Department of Bioengineering, Lehigh University, Bethlehem, PA, USA.
Background: Major depressive disorder (MDD) is a prevalent psychiatric disorder characterized by substantial clinical and neurobiological heterogeneity. Conventional studies that solely focus on clinical symptoms or neuroimaging metrics often fail to capture the intricate relationship between these modalities, limiting their ability to disentangle the complexity in MDD. Moreover, patient neuroimaging data typically contains normal sources of variance shared with healthy controls, which can obscure disorder-specific variance and complicate the delineation of disease heterogeneity.
View Article and Find Full Text PDFFAAH inhibitor URB597 shows anti-hyperalgesic action and increases brain and intestinal tissues fatty acid amides in a model of CRF agonist mediated visceral hypersensitivity in male rats.
Neurogastroenterol Motil
December 2024
Vatche and Tamar Manoukian Division of Digestive Diseases, Department of Medicine, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, California, USA.
Background And Aims: The endocannabinoid (eCB) system includes ligands (anandamide and 2-arachidonoyl glycerol, 2-AG), receptors and catabolizing enzymes (fatty acid amide hydrolase, FAAH and monoacylglycerol lipase) expressed in both the brain and gut. We investigated whether the FAAH inhibitor, URB597, influenced visceral pain to colorectal distension (CRD) in an acute stress-related model of visceral hypersensitivity induced by the selective corticotropin-releasing factor receptor subtype 1 (CRF) agonist, cortagine.
Methods: Male Sprague-Dawley rats were injected subcutaneously (SC) with URB597 (3 mg/kg) or vehicle and 2 h later, intraperitoneally with cortagine (10 μg/kg) or vehicle.
Want 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!