Diarylimidazolecarboxamides and diaryltriazolecarboxamides related to SR141716 were synthesized and tested for binding to the human CB(1) receptor. Suitably substituted imidazoles are comparably potent to the clinical candidate, whereas the analogous triazoles are less so due to the absence of an additional substituent on the azole ring.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2003.12.068 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Xixin Decoction's novel mechanism for alleviating Alzheimer's disease cognitive dysfunction by modulating amyloid-β transport across the blood-brain barrier to reduce neuroinflammation.
Front Pharmacol
January 2025
Key Research Laboratory for Prevention and Treatment of Cerebrospinal diseases, Shaanxi Provincial Administration of Traditional Chinese Medicine, Xianyang, China.
Purpose: Xixin Decoction (XXD) is a classical formula that has been used to effectively treat dementia for over 300 years. Modern clinical studies have demonstrated its significant therapeutic effects in treating Alzheimer's disease (AD) without notable adverse reactions. Nevertheless, the specific mechanisms underlying its efficacy remain to be elucidated.
View Article and Find Full Text PDFCannabinoid receptor 1 ligands: Biased signaling mechanisms driving functionally selective drug discovery.
Pharmacol Ther
January 2025
Xi'an Key Laboratory for Antiviral and Antimicrobial-Resistant Bacteria Therapeutics Research, Shaanxi University of Science & Technology, Xi'an 710021, China; School of Biological and Pharmaceutical Sciences, Shaanxi University of Science & Technology, Xi'an 710021, China. Electronic address:
G protein-coupled receptors (GPCRs) adopt conformational states that activate or inhibit distinct signaling pathways, including those mediated by G proteins or β-arrestins. Biased signaling through GPCRs may offer a promising strategy to enhance therapeutic efficacy while reducing adverse effects. Cannabinoid receptor 1 (CB1), a key GPCR in the endocannabinoid system, presents therapeutic potential for conditions such as pain, anxiety, cognitive impairment, psychiatric disorders, and metabolic diseases.
View Article and Find Full Text PDFInternational Symposium on Ruminant Physiology: The involvement of the endocannabinoid system in metabolic and inflammatory responses in dairy cows during negative energy balance.
J Dairy Sci
January 2025
Department of Ruminant Science, Institute of Animal Sciences, ARO Volcani Institute, Israel; Department of Animal Science, The Robert H. Smith Faculty of Agriculture, Food and Environment, The Hebrew University of Jerusalem, Rehovot, Israel.
The endocannabinoid system (ECS) is involved in the regulation of energy metabolism, immune function and reproduction in mammals. The ECS is consisted of the endocannabinoid (eCB) ligands, enzymes, and cannabinoid receptors. In mammals, the cannabinoid-1 receptor (CB1/CNR1) is expressed in the central nervous system and in peripheral tissues; and its activation increases anabolic processes.
View Article and Find Full Text PDFMuscarinic cannabinoid suppression of excitation, a novel form of coincidence detection.
Pharmacol Res
January 2025
Gill Institute for Neuroscience, United States; Department of Psychological and Brain Sciences, Indiana University, Bloomington, IN 47405, United States. Electronic address:
Δ-tetrahydrocannabinol (THC), the chief psychoactive ingredient of cannabis, acts in the brain primarily via cannabinoid CB1 receptors. These receptors are implicated in several forms of synaptic plasticity - depolarization-induced suppression of excitation (DSE), metabotropic suppression of excitation (MSE), long term depression (LTD) and activation-dependent desensitization. Cultured autaptic hippocampal neurons express all of these, illustrating the rich functional and temporal heterogeneity of CB1 at a single set of synapses.
View Article and Find Full Text PDFDetermination of the Negative Allosteric Binding Site of Cannabidiol at the CB1 Receptor: A Combined Computational and Site-Directed Mutagenesis Study.
ACS Chem Neurosci
January 2025
National Center for Natural Products Research, University of Mississippi, University, Mississippi 38677, United States.
Cannabinoid receptor 1 (CB1R) has been extensively studied as a potential therapeutic target for various conditions, including pain management, obesity, emesis, and metabolic syndrome. Unlike orthosteric agonists such as Δ-tetrahydrocannabinol (THC), cannabidiol (CBD) has been identified as a negative allosteric modulator (NAM) of CB1R, among its other pharmacological targets. Previous computational and structural studies have proposed various binding sites for CB1R NAMs.
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!