Boyer J L, Mohanram A, Camaioni E, Jacobson K A, Harden T K
Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill 27599-7365, USA.
Br J Pharmacol. 1998 May;124(1):1-3. doi: 10.1038/sj.bjp.0701837.
The antagonist activity of N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate (N6MABP) has been examined at the phospholipase C-coupled P2Y1 receptor of turkey erythrocyte membranes. N6MABP antagonized 2MeSATP-stimulated inositol phosphate hydrolysis with a potency approximately 20 fold greater than the previously studied parent molecule, adenosine 3',5'-bisphosphate. The P2Y1 receptor antagonism observed with N6MABP was competitive as revealed by Schild analysis (pK(B) = 6.99 +/- 0.13). Whereas N6MABP was an antagonist at the human P2Y1 receptor, no antagonist effect of N6MABP was observed at the human P2Y2, human P2Y4 or rat P2Y6 receptors.
已在火鸡红细胞膜的磷脂酶C偶联P2Y1受体上检测了N6-甲基2'-脱氧腺苷3',5'-二磷酸（N6MABP）的拮抗活性。N6MABP拮抗2MeSATP刺激的肌醇磷酸水解，其效力比先前研究的母体分子腺苷3',5'-二磷酸大约高20倍。如Schild分析所示（pK(B)=6.99±0.13），N6MABP对P2Y1受体的拮抗作用具有竞争性。虽然N6MABP是人类P2Y1受体的拮抗剂，但在人类P2Y2、人类P2Y4或大鼠P2Y6受体上未观察到N6MABP的拮抗作用。
