論文 - 詳細
| RRC ID | 39254 |
|---|---|
| 著者 | Ono T, Matsuoka I, Ohkubo S, Kimura J, Nakanishi H. |
| タイトル | Effects of YT-146 [2-(1-octynyl) adenosine], an adenosine A2A receptor agonist, on cAMP production and noradrenaline release in PC12 cells. |
| ジャーナル | Jpn J Pharmacol |
| Abstract |
Effects of YT-146 [2-(1-octynyl) adenosine], an adenosine A2 receptor agonist, on cAMP production and noradrenaline (NA) release were investigated in PC12 cells. YT-146 caused a concentration-dependent cAMP accumulation (EC50: 1.2+/-0.9 nM). In [3H]NA-prelabeled cells, YT-146 increased the basal NA release and enhanced ATP-evoked NA release in a concentration-dependent manner (EC50: 0.23+/-0.15 nM). YT-146 augmented the maximal response to ATP without affecting the EC50 value of ATP. These effects of YT-146 were inhibited by several adenosine receptor antagonists with a characteristic of adenosine A2A receptor subtype. The effects of YT-146 were mimicked by forskolin, dibutylyl cAMP and Sp-cAMPS, and inhibited by H-89, a cAMP-dependent protein kinase inhibitor. YT-146 had little effect on ATP-induced increase in intracellular Ca2+ concentration. YT-146 enhanced the NA release induced by several different stimuli including Ca2+ ionophore A23187. The present results suggest that YT-146 is a potent agonist on adenosine A2A receptors in PC12 cells and causes a cAMP-dependent enhancement of NA release by affecting the exocytosis process at a point downstream of the intracellular Ca2+ increase. |
| 巻・号 | 78(3) |
| ページ | 269-77 |
| 公開日 | 1998-11-1 |
| DOI | 10.1254/jjp.78.269 |
| PMID | 9869260 |
| MeSH | Adenosine / analogs & derivatives* Adenosine / pharmacology Adenosine Triphosphate / pharmacology Alkynes / pharmacology* Animals Bucladesine / pharmacology Calcimycin / pharmacology Calcium / metabolism Carbachol / pharmacology Cholinergic Agonists / pharmacology Colforsin / pharmacology Cyclic AMP / analogs & derivatives Cyclic AMP / biosynthesis* Cyclic AMP / pharmacology Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors Enzyme Inhibitors / pharmacology Ionophores / pharmacology Isoquinolines / pharmacology Membrane Potentials / drug effects Norepinephrine / metabolism* PC12 Cells Potassium Chloride / pharmacology Purinergic P1 Receptor Agonists* Rats Receptor, Adenosine A2A Sulfonamides* Thionucleotides / pharmacology Tritium Vasodilator Agents / pharmacology* |
| 引用数 | 6 |
| WOS 分野 | PHARMACOLOGY & PHARMACY |
| リソース情報 | |
| ヒト・動物細胞 | PC-12(RCB0009) |