ArticleJournal of medicinal chemistry2012
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Lack of efficacy of a partial adenosine A1 receptor agonist in neuropathic pain models in mice.Purinergic signalling · 2021Article
- Article
- AMolecular neurobiology · 2017Review
- Purinergic Receptor Expression and Potential Association with Human Embryonic Stem Cell-Derived Oligodendrocyte Progenitor Cell Development.Cell journal · 2017Article
- Sustained Elevated Adenosine via ADORA2B Promotes Chronic Pain through Neuro-immune Interaction.Cell reports · 2016Article
- Medicinal chemistry of adenosine, P2Y and P2X receptors.Neuropharmacology · 2016Review
- Article
- Prodrugs of phosphonates and phosphates: crossing the membrane barrier.Topics in current chemistry · 2015Review
- Molecular signatures of mouse TRPV1-lineage neurons revealed by RNA-Seq transcriptome analysis.The journal of pain · 2014Article
- Synthesis of nucleoside phosphate and phosphonate prodrugs.Chemical reviews · 2014Review
- 2,6-Di-chloro-9-(2',3',5'-tri-O-acetyl-β-d-ribo-furanos-yl)-9H-purine.Acta crystallographica. Section E, Structure reports online · 2014Article
- 5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions.Molecules (Basel, Switzerland) · 2012Article
- Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.Journal of medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Adenosine A(1) receptor (A(1)AR) agonists have antinociceptive effects in multiple preclinical models of acute and chronic pain. Although numerous A(1)AR agonists have been developed, clinical applications of these agents have been hampered by their cardiovascular side effects. Herein we report a series of novel A(1)AR agonists, some of which are structurally related to adenosine 5'-monophosphate (5'-AMP), a naturally occurring nucleotide that itself activates A(1)AR. These novel compounds potently activate A(1)AR in several orthogonal in vitro assays and are subtype selective for A(1)AR over A(2A)AR, A(2B)AR, and A(3)AR. Among them, UNC32A (3a) is orally active and has dose-dependent antinociceptive effects in wild-type mice. The antinociceptive effects of 3a were completely abolished in A(1)AR knockout mice, revealing a strict dependence on A(1)AR for activity. The apparent lack of cardiovascular side effects when administered orally and high affinity (K(i) of 36 nM for the human A(1)AR) make this compound potentially suitable as a therapeutic.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.