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- W1986836161 abstract "We recently reported that 2-substitution of N6-benzyladenosine-5′-uronamides greatly enhances selectivity of agonists for rat A3 adenosine receptors (J. Med. Chem. 1994, 37, 3614–3621). Specifically, 2-Chloro-N6-(3-iodobenzyl)adenosine-5′-N-methyluronamide (2-CI-IB-MECA), which displayed a Ki value of 0.33 nM, is the most selective for A3 receptors yet reported with selectivity versus A1 and A2a receptors of 2500- and 1400-fold, respectively. In order to obtain pharmacological tools for the study of A3 adenosine receptors, two routes for radiolabeling of 2-CI-IB-MECA through incorporation of tritium at the 5′-methylamido group were compared. One route formed a 2′,3′-protected nucleoside 5′-carboxylic acid (9), which was condensed with methylamine and deprotected. The more efficient synthesis started from D-ribose and provided 2-CI-IB-MECA (12) in six steps with an overall yield of 5.6%. Tritium was introduced in the penultimate step by heating N6-(3-iodobenzyl)-2-chloro-2′,3′-di-O-acetyl-5′-(methoxycarbonyl)adenosine (17) with [3H]methylamine in methanol at 60°C for 2 h. The specific activity of [3H]2-CI-IB-MECA was 29 Ci/mmol with a radiochemical purity of 99%." @default.
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- W1986836161 date "1996-06-01" @default.
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- W1986836161 title "Radiolabeling and efficient synthesis of tritiated 2-chloro-N6-(3-iodobenzyl)adenosine-5′-N-methyluron-amide, a potent, selective A3 adenosine receptor agonist" @default.
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- W1986836161 doi "https://doi.org/10.1002/(sici)1099-1344(199606)38:6<547::aid-jlcr870>3.0.co;2-y" @default.
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