ArticleEuropean journal of pharmacology2002
2-Chloro-N(6)-cyclopentyladenosine, adenosine A(1) receptor agonist, antagonizes the adenosine A(3) receptor.
Article in European journal of pharmacology, 2002. 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, 22 citations in OpenAlex.
- Review
- Therapeutic potential of adenosine receptor modulators in cancer treatment.RSC advances · 2025Review
- Adenosine receptors as promising targets for the management of ocular diseases.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021Review
- Ocular Purine Receptors as Drug Targets in the Eye.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2016Review
- A1 Adenosine Receptor-Mediated Inhibition of Parasympathetic Neuromuscular Transmission in Human and Murine Urinary Bladder.The Journal of pharmacology and experimental therapeutics · 2016Article
- Recent developments in adenosine receptor ligands and their potential as novel drugs.Biochimica et biophysica acta · 2011Review
- The cross-species A3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure.Current eye research · 2005Article
- Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.Bioorganic & medicinal chemistry letters · 2004Article
- Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety.Biochemical pharmacology · 2004Article
- Partial agonists for A(3) adenosine receptors.Current topics in medicinal chemistry · 2004Review
- N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.Biochemical pharmacology · 2003Article
- Engineering of ADrug development research · 2003Article
- Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry · 2002Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The potent adenosine A(1) receptor agonists, N(6)-cyclopentyladenosine (CPA) and 2-chloro-N(6)-cyclopentyladenosine (CCPA), were studied in Chinese hamster ovary (CHO) cells expressing the human adenosine A(3) receptor. CPA, but not CCPA, induced phosphoinositide turnover. CPA inhibited forskolin-stimulated cyclic AMP production (EC(50) value of 242+/-47 nM). CCPA competitively antagonized the effects of agonist Cl-IB-MECA (2-chloro-N(6)-(3-iodobenzyl)-5'-N-methylcarbamoyladenosine) with K(B) value of 5.0 nM. CPA competition curves versus the A(3) antagonist radioligand [3H]PSB-11 (8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2.1-i]purin-5-one) were right-shifted four-fold by 100 microM GTP, which had no effect on binding of CCPA or the antagonist MRS 1220 (N-[9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-yl]benzene-acetamide). Thus, CCPA is a moderately potent antagonist (K(i)=38 nM) of the human A(3) adenosine receptor.
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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.