期刊论文详细信息
FEBS Letters
8‐(3‐Chlorostyryl)caffeine (CSC) is a selective A2‐adenosine antagonist in vitro and in vivo
Jacobson, Kenneth A.1  Nikodijević, Olga1  Daly, John W.1  Maillard, Michel1  Gallo-Rodriguez, Carola1  Padgett, William L.1 
[1] Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
关键词: Adenosine receptor;    Xanthine;    Locomotor activity;    Dopamine;    Adenylate cyclase;   
DOI  :  10.1016/0014-5793(93)81466-D
学科分类:生物化学/生物物理
来源: John Wiley & Sons Ltd.
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【 摘 要 】

An adenosine antagonist, 8-(3-chlorostyryl)caffeine (CSC), was shown previously to be 520-fold selective for A2a-adenosine receptors in radioligand binding assays in the rat brain. In reversing agonist effects on adenylate cyclase, CSC was 22-fold selective for A2a receptors in rat pheochromocytoma cells (K b 60 nM) vs. A1 receptors in rat adipocytes (K b 1.3 μM). Administered i.p. in NIH mice at a dose of 1 mg/kg, CSC shifted the curve for locomotor depression elicited by the A2a-selective agonist APEC to the right (ED50 value for APEC shifted from 20 μg/kg i.p. to 190 μg/kg). CSC had no effect on locomotor depression elicited by an ED50 dose of the A1-selective agonist CHA. CSC alone at a dose of 5 mg/kg stimulated locomotor activity by 22% over control values. Coadministration of CSC and the A1-selective antagonist CPX, both at non-stimulatory doses, increased activity by 37% (P < 0.001) over CSC alone, suggesting a behavioral synergism of A1- and A2-antagonist effects in the CNS.

【 授权许可】

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