A new series of 9-deazaxanthine derivatives with various substituents at the heterocyclic system were synthesized and evaluated for their binding affinities for the four human recombinant adenosine receptors, A(1)-A(3) subtypes. A number of the 9-deazaxanthines derivatives 3a-m showed moderate-to-high affinity for hA(2B) receptors, with compound 3f showing a 32-fold selectivity for A(2B) over A(1) and a 2750-fold selectivity for A(2B) over A(2A).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2010.03.011 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Precise Control of Regioselective and -Alkylation of Benzotriazoles with α-Diazoacetates by Metalloporphyrin.
Inorg Chem
January 2025
School of Chemistry, Sun Yat-Sen University, Guangzhou 510006, China.
Regioselective -alkylation of benzotriazole is highly important to prepare biological materials. Herein, a series of AB-typed porphyrin and metalloporphyrin compounds were prepared. Catalytic results disclosed that Ir(III) pentafluorophenyl-substituted porphyrin promoted selective -alkylation of benzotriazole, and meanwhile, Fe(III) pyridine-substituted porphyrin accelerated -alkylation of benzotriazole.
View Article and Find Full Text PDFPorphyrin based covalent organic frameworks via self-polycondensation for heterogeneous photocatalysis.
J Colloid Interface Sci
December 2024
College of Chemical Engineering and Materials Science, Tianjin University of Science and Technology, Tianjin 300350, PR China; Tianjin Key Laboratory of Multiplexed Identification for Port Hazardous Chemicals, Tianjin 300457, PR China. Electronic address:
A novel porphyrin based covalent organic frameworks (Por-BABN-COF) has been successfully constructed via self-polycondensation of a newly developed AB porphyrin building block possessing two amino groups and two neopentyl acetal at the meso-position. Por-BABN-COF was employed as a heterogeneous photocatalyst for the selective oxidation of sulfides and CO cycloaddition due to its superior light absorption capacity, strong crystallinity and high stability. The high conversion, good selectivity and excellent reusability indicate Por-BABN-COF is a promising photocatalyst for both reactions.
View Article and Find Full Text PDFAdenosine relaxes vagina smooth muscle through the cyclic guanosine monophosphate- and cyclic guanosine monophosphate-dependent pathways.
J Sex Med
January 2025
Andrology and Gender Endocrinology Unit, Department of Experimental Clinical and Biomedical Sciences "Mario Serio", University of Florence, Florence, 50134, Italy.
Background: In males, adenosine (ADO) is known to relax penile smooth muscles, although its role in the vagina is not yet fully elucidated.
Aim: This study investigated the effect of ADO on vagina smooth muscle activity, using a validated female Sprague-Dawley rat model.
Methods: Contractility studies, using noradrenaline-precontracted vaginal strips, tested the effects of ADORA1/3 antagonists and ADORA2A/2B antagonists and agonists.
MRS3997, a dual adenosine A/A receptor agonist, reduces brain ischemic damage and alleviates neuroinflammation in rats.
Neuropharmacology
January 2025
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, Florence, Italy.
The endogenous neuromodulator adenosine is massively released during hypoxic/ischemic insults and differentially modulates post-ischemic damage depending on the expression and recruitment of its four metabotropic receptor subtypes, namely A, A, A and A receptors (ARs, ARs, ARs and ARs). We previously demonstrated, by using a model of transient middle cerebral artery occlusion (tMCAo) in rats, that selective activation of ARs, as well as ARs, ameliorates post-ischemic brain damage in contrast to neuroinflammation. In the present study, we investigated whether the multitarget nucleoside MRS3997, a full agonist at both ARs and ARs, would afford higher neuroprotection in post-ischemic damage.
View Article and Find Full Text PDF8-Aminopurines: A Promising New Direction for Purine-Based Therapeutics.
Hypertension
December 2024
Department of Pharmacology and Chemical Biology (E.K.J., S.P.T., Y.C., L.A.B.), University of Pittsburgh School of Medicine, Pittsburgh, PA.
Research in purinergic pharmacology has yielded major advances in cardiovascular therapeutics such as adenosine for terminating atrioventricular reentrant tachycardia, regadenoson for pharmacological ischemic stress testing, and selective P2Y receptor antagonists for prevention of stroke and myocardial infarction. Mechanistically, these FDA-approved purine-based therapeutics activate or antagonize receptors having endogenous ligands containing the purine nucleobase adenine. Recent discoveries suggest a novel direction for purine-based therapeutics.
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!