ArticleDrug development research1994
Structure Activity Relationships for Derivatives of Adenosine-5'-Triphosphate as Agonists at P(2) Purinoceptors: Heterogeneity Within P(2X) and P(2Y) Subtypes.
Article in Drug development research, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 99 citations in OpenAlex.
- New paradigms in purinergic receptor ligand discovery.Neuropharmacology · 2023Review
- Structure-activity relationships of pyrimidine nucleotides containing a 5'-α,β-methylene diphosphonate at the P2YBioorganic & medicinal chemistry letters · 2021Article
- Medicinal chemistry of P2 and adenosine receptors: Common scaffolds adapted for multiple targets.Biochemical pharmacology · 2021Review
- A Photo-clickable ATP-Mimetic Reveals Nucleotide Interactors in the Membrane Proteome.Cell chemical biology · 2020Article
- Demystifying P2YJournal of chemical information and modeling · 2017Article
- Purinergic signalling in the gastrointestinal tract and related organs in health and disease.Purinergic signalling · 2014Review
- Purinergic signalling in the urinary tract in health and disease.Purinergic signalling · 2014Review
- Biochemical characterization of soluble nucleotide pyrophosphatase/phosphodiesterase activity in rat serum.Molecular and cellular biochemistry · 2010Article
- Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.Journal of medicinal chemistry · 2010Article
- Identification of hydrolytically stable and selective P2Y(1) receptor agonists.European journal of medicinal chemistry · 2009Article
- Development of selective agonists and antagonists of P2Y receptors.Purinergic signalling · 2009Article
- Signaling of the Human P2Y(1) Receptor Measured by a Yeast Growth Assay with Comparisons to Assays of Phospholipase C and Calcium Mobilization in 1321N1 Human Astrocytoma Cells.Purinergic signalling · 2005Article
- A pre-clinical study showing how dopaminergic drugs administered during pre-exposure can impair or facilitate latent inhibition.Psychopharmacology · 2005Article
- Purine and pyrimidine (P2) receptors as drug targets.Journal of medicinal chemistry · 2002Review
- Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.Journal of medicinal chemistry · 2002Article
- Pharmacological characterization of ATP- and LPS-induced IL-1beta release in human monocytes.British journal of pharmacology · 1999Article
- Characterization of "mini-nucleotides" as P2X receptor agonists in rat cardiomyocyte cultures. An integrated synthetic, biochemical, and theoretical study.Journal of medicinal chemistry · 1999Article
- Synthesis and Structure-Activity Relationships of Pyridoxal-6-arylazo-5'-phosphate and Phosphonate Derivatives as P2 Receptor Antagonists.Drug development research · 1998Article
- Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors.Journal of medicinal chemistry · 1998Article
- A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor.Molecular pharmacology · 1997Article
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
Abstract
The structure-activity relationships for a variety of adenine nucleotide analogues at P(2x)- and P(2Y)-purinoceptors were investigated. Compounds formed by structural modifications of the ATP molecule including substitutions of the purine ring (C2, C8, N1, and N(6)-substituents, and a uridine base instead of adenine), the ribose moiety (2' and 3'-positions), and the triphosphate group (lower phosphates, bridging oxygen substitution, and cyclization) were prepared. Pharmacological activity at P(2Y)-purinoceptors was assayed in the guinea pig taenia coli, endothelial cells of the rabbit aorta, smooth muscle of the rabbit mesenteric artery, and turkey erythrocyte membranes. Activity at P(2X)-purinoceptors was assayed in the rabbit saphenous artery and the guinea-pig vas deferens and urinary bladder. Some of the analogues displayed selectivity, or even specificity, for either the P(2X)- or the P(2Y)-purinoceptors. Certain analogues displayed selectivity or specificity within the P(2X)- or P(2Y)-purinoceptor superfamilies, giving hints about possible subclasses. For example, 8-(6-aminohexylamino)ATP and 2',3'-isopropylidene-AMP were selective for endothelial Pzypurinoceptors over P(2Y)-purinoceptors in the guinea pig taenia coli, rabbit aorta, and turkey erythrocytes. These compounds were both inactive at P(2X)-purinoceptors. The potent agonist N(6)-methyl ATP and the somewhat less potent agonist 2'-deoxy-ATP were selective for P(2Y)-purinoceptors in the guinea pig taenia coli, but were inactive at P(2X)-purinoceptors and the vascular P(2Y)-purinoceptors. 3'-Benzylamino-3'-deoxyATP was very potent at the P(2X)-purinoceptors in the guinea pig vas deferens and bladder, but not in the rabbit saphenous artery and was inactive at P(2Y) receptors. These data suggest that specific compounds can be developed that can be utilized to activate putative subtypes of the P(2X)- and P(2Y)-purinoceptor classes.
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