The binding affinities at rat A, A, and A adenosine receptors of a wide range of heterocyclic derivatives have been determined. Mono-, bi-, tricyclic and macrocyclic compounds were screened in binding assays, using either [H]PIA or [H]CGS 21680 in rat brain membranes or [I]AB-MECA in CHO cells stably transfected with rat A receptors. Several new classes of adenosine antagonists ( 5-oxoimidazopyrimidines and a pyrazoloquinazoline) were identified. Various sulfonylpiperazines, 11-hydroxytetrahydrocarbazolenine, 4H-pyrido[1,2-a]pyrimidinone, folic acid, and cytochalasin H and J bound to A receptors selectively. Moreover, cytochalasin A, which bound to A adenosine receptors with K value of 1.9 μM, inhibited adenylyl cyclase in rat adipocytes, but not via reversible A receptor binding.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4817726 | PMC |
| http://dx.doi.org/10.1080/07328319608002416 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Inosine exerts dopaminergic neuroprotective effects via mitigation of NLRP3 inflammasome activation.
Neuropharmacology
December 2024
College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongbuk, Republic of Korea. Electronic address:
Neuroinflammation plays a crucial role in the pathogenesis of Parkinson's disease (PD). Transformation of pro-interleukin (IL)-1β into a mature IL-1β via active inflammasome may be related to the progression of PD. Therefore, the modification of inflammasome activity may be a potential therapeutic strategy for PD.
View Article and Find Full Text PDFNetrin-1: Key insights in neural development and disorders.
Tissue Cell
December 2024
Department of Pharmacy, Al-Zahrawi University College, Karbala, Iraq.
Netrin-1, an essential extracellular protein, has gained significant attention due to its pivotal role in guiding axon and cell migration during embryonic development. The fundamental significance of netrin-1 in developmental biology is reflected in its high conservation across different species as a part of the netrin family. The bifunctional nature of netrin-1 demonstrates its functional versatility, as it can function as either a repellent or an attractant according to the context and the expressed receptors on the target cells including the deleted in colorectal cancer (DCC), the uncoordinated-5 (UNC5), DSCAM, Neogenin-1, Adenosine A2b and Draxin receptors.
View Article and Find Full Text PDFReduced adenosine receptor expression in ACS patients with no-flow phenomenon undergoing primary PCI.
Future Cardiol
December 2024
Cardiovascular Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Introduction: Acute coronary syndrome (ACS) patients undergoing primary percutaneous coronary intervention (PPCI) often experience the no-reflow phenomenon (NRP), characterized by reduced myocardial perfusion despite an open coronary artery. Adenosine, a potent vasodilator, is used to aid reperfusion. To elucidate underlying molecular mechanism of this phenomenon, we investigated expression of ADORA2A and ADORA2B genes, encoding adenosine receptors, in ACS patients with NRP and non-NRP.
View Article and Find Full Text PDFActivation of PLCβ enzymes by G and G proteins is a common mechanism to trigger cytosolic Ca increase. We and others reported that G inhibitor FR900358 (FR) can inhibit both and G - and, surprisingly, G -mediated intracellular Ca mobilization. Thus, the G -G -PLCβ-Ca signaling axis depends entirely on the presence of active G , which reasonably explained FR-inhibited G -induced Ca release.
View Article and Find Full Text PDFA bitter taste receptor liganded by oxalic acid inhibits brown planthopper feeding by promoting CREB phosphorylation via the PI3K-AKT signaling pathway.
Int J Biol Macromol
December 2024
School of Life Sciences, Hebei University, Baoding 071002, China. Electronic address:
Insect gustatory receptors play a critical role in modulating feeding behaviors by detecting external nutritional cues through complex biochemical pathways. Bitter taste receptors are essential for insects to identify and avoid toxins. However, the detailed molecular and cellular mechanisms by which these receptors influence insect feeding behavior remain poorly understood.
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!