1995
DOI: 10.1358/dof.1995.020.07.531583
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A3-adenosine receptors: Design of selective ligands and therapeutic prospects

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Cited by 122 publications
(154 citation statements)
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“…Relaxant responses to CGS 21680 were only observed at concentrations greater than 10 mM and as the a nity of CGS 21680 at A 2A receptors is 15 nM (Jacobson et al, 1995), these relaxant responses are unlikely to be mediated via A 2A receptors. This was con®rmed by use of 50 mM 8-SPT, which failed to block the responses to CGS 21680.…”
Section: Controlmentioning
confidence: 93%
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“…Relaxant responses to CGS 21680 were only observed at concentrations greater than 10 mM and as the a nity of CGS 21680 at A 2A receptors is 15 nM (Jacobson et al, 1995), these relaxant responses are unlikely to be mediated via A 2A receptors. This was con®rmed by use of 50 mM 8-SPT, which failed to block the responses to CGS 21680.…”
Section: Controlmentioning
confidence: 93%
“…Recently a third receptor termed the A 3 receptor has been cloned (Zhou et al, 1992) which is activated by adenosine and some analogues such as N 6 -(3-iodo-benzyl)-adenosine-5'-Nmethyluronamide (IB-MECA, K i =1.1 nM, Jacobson et al, 1995). Unlike A 1 and A 2 receptors, the rat A 3 receptor is resistant to blockade by all but a few methylxanthines, one of which is 1,3-dipropyl -8-(4-acrylate)phenylxanthine (BWA1433, K i =15 mM, Jacobson et al, 1995).…”
Section: Introductionmentioning
confidence: 99%
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“…N 6 -(3-iodobenzyl)-adenosine-5'-N-methylcarboxamide (IB-MECA) has been reported as a selective A 3 -receptor agonist (Jacobson et al, 1993;Gallo-RodrõÂ guez et al, 1994). A 3 -receptors are resistant to blockade with methylxanthines, although it has been reported that compounds such as 1,3-dipropyl-8-(4-acrylate)phenylxanthine (BWA1433) block them (Jacobson et al, 1995).…”
Section: Introductionmentioning
confidence: 99%
“…Pharmacological studies, using antagonists to the different adenosine receptors, revealed that A3AR plays a key role in the adenosineinduced inhibition of tumour cell proliferation, simultaneously stimulating bone marrow cell growth (Fishman et al, 2000a, b;BarYehuda et al, 2001). Indeed, synthetic agonists to A3AR, such as CF101 and Cl-IB-MECA (Jacobson et al, 1995), were found to act similar to adenosine, while having the advantage of being stable, nondegradable, and bioavailable molecules (Fishman et al, 2000a, b).…”
mentioning
confidence: 99%