Optimization of HTS hit 1 for NPY Y5 receptor binding affinity, CYP450 inhibition, solubility and metabolic stability led to the identification of some orally available oxygen-linker derivatives for in vivo study. Among them, derivative 4i inhibited food intake induced by the NPY Y5 selective agonist, and chronic oral administration of 4i in DIO mice caused a dose-dependent reduction of body weight gain.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2012.11.005 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Neuropeptide Y in cancer-biological functions and potential clinical implications.
Cancer Metastasis Rev
January 2025
Department of Biochemistry and Molecular and Cellular Biology, Georgetown University Medical Center, BSB 231A, 3900 Reservoir Rd., NW, Washington, DC, 20057, USA.
Neuropeptide Y (NPY) is a sympathetic neurotransmitter widely distributed in the peripheral and central nervous system, affecting many physiological functions. Consequently, dysregulation of the NPY system contributes to numerous pathological disorders, including stress, obesity, and cancer. The pleiotropic functions of NPY in humans are mediated by G protein-coupled receptors (Y1R, Y2R, Y5R), which activate several signaling pathways and thereby regulate cell growth, differentiation, apoptosis, proliferation, angiogenesis, and metabolism.
View Article and Find Full Text PDFDifferential suppression of hippocampal network oscillations by neuropeptide Y.
Neuropharmacology
December 2024
Institute of Physiology and Pathophysiology, Heidelberg University, Im Neuenheimer Feld 326, 69120, Heidelberg, Germany.
Neuropeptide Y (NPY) is the most abundant neuropeptide in the brain. It exerts anxiolytic and anticonvulsive actions, reduces stress and suppresses fear memory. While its effects at the behavioral and cellular levels have been well studied, much less is known about the modulation of physiological activity patterns at the network level.
View Article and Find Full Text PDFTranscriptomic analysis of the HPT axis in a model of oligoasthenozoospermia induced by Adenine in rats.
Exp Mol Pathol
December 2024
College of Traditional Chinese Medicine, Ningxia Medical University, Yinchuan 750000, China; Key Laboratory of Modernization of Minority Medicine, Ministry of Education, Ningxia Medical University, Yinchuan 750000, China. Electronic address:
Male infertility is most commonly caused by oligozoospermia, and its pathogenesis is still poorly understood at the molecular level. This study used RNA sequencing (RNA-Seq) technology to identify candidate genes and regulatory pathways that regulate semen quality in the hypothalamic, pituitary, and testicular tissues of healthy rats and Adenine-induced oligozoospermia model rats. Semen quality testing and histological analysis of testicular tissues were performed on both groups of rats.
View Article and Find Full Text PDFNeuropeptide Y and Pain: Insights from Brain Research.
ACS Pharmacol Transl Sci
December 2024
Department of Pharmacology and Therapeutics, McKnight Brain Institute, College of Medicine, University of Florida, Gainesville, Florida 32610, United States.
Neuropeptide Y (NPY) is a highly conserved neuropeptide with widespread distribution in the central nervous system and diverse physiological functions. While extensively studied for its inhibitory effects on pain at the spinal cord level, its role in pain modulation within the brain remains less clear. This review aims to summarize the complex landscape of supraspinal NPY signaling in pain processing.
View Article and Find Full Text PDFAcute Stress Effects over Time on the Gene Expression and Neurotransmitter Patterns in the Carp () Brain.
Animals (Basel)
November 2024
School of Agricultural, Forest and Food Sciences (HAFL), Bern University of Applied Sciences (BFH), 3052 Zollikofen, Switzerland.
Changes in gene expression in carps' brains over time following acute stressors has not been studied in detail so far. Consequently, a stress trial with juvenile common carp was conducted to investigate transcriptomic differences in four brain parts in response to acute negative stressors and feed reward, focusing on appetite-related genes, serotonergic and dopaminergic pathways, and other involved systems, at 30, 60, and 90 min after treatments. The treatments showed pronounced effects on the gene expression patterns across brain parts compared to control fish.
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!