Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5829122 | European Journal of Pharmacology | 2013 | 5 Pages |
Abstract
A novel adenosine A3 receptor antagonist (SSR161421) was characterized by both receptor binding assays and pharmacological tests. Binding studies on cloned human adenosine receptors showed that SSR161421 has high affinity for adenosine hA3 receptors (Ki=0.37Â nM) with at least 1000-fold selectivity compared to hA1, hA2A and hA2B receptors. The receptor antagonist nature of SSR161421 was determined in a functional study on Chinese hamster ovarian cells (CHO) cells expressing human adenosine A3 receptors. SSR161421 competitively antagonized the effect of 2-chloro-N6-(3-iodobenzyl)-adenosine-5â²-N-methylcarboxamide (Cl-IB-MECA) on cAMP production with a pA2 value in a luciferase reporter gene construct. In mice, intravenously administered SSR161421 inhibited the N6-(4-aminobenzyl)-adenosine-5â²-N-methyl-uronamide dihydrochloride (AB-MECA) induced increase in plasma histamine levels (ED50=2.0Â mg/kg) and the Cl-IB-MECA evoked plasma extravasation (ID50=2.9Â mg/kg) and oedema formation (ID50=4.6Â mg/kg) in mouse ear.
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Authors
Endre G. Mikus, Kinga Boér, Géza Timári, Katalin Urbán-Szabó, Zoltán Kapui, Judit Szeredi, Katalin Gerber, Tibor Szabó, Sándor Bátori, Michel Finet, Péter Arányi, Anne-Marie Galzin,