Ishiwata Kiichi, Mizuno Masaki, Kimura Yuichi, Kawamura Kazunori, Oda Keiichi, Sasaki Toru, Nakamura Yoshio, Muraoka Isao, Ishii Kenji
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, 1-1 Naka-cho, Itabashi-ku, Tokyo 173-0022, Japan.
Nucl Med Biol. 2004 Oct;31(7):949-56. doi: 10.1016/j.nucmedbio.2004.06.003.
We examined the potential of [7-methyl-11C]-(E)-8-(3,4,5-trimethoxystyryl)-1,3,7-trimethylxanthine ([11C]TMSX) for the assessment of adenosine A2A receptors in muscle. In rodents, specific binding of [11C]TMSX was observed in muscle and heart by blockade with A2A-selective CSC and non-selective theophylline, but not with A1-selective DPCPX. Swimming exercise fluctuated radioligand-receptor binding in these tissues. In a PET study of two subjects, theophylline-infusion slightly deceased the distribution volume of [11C]TMSX in the heart (20% reduction) and muscle (10% reduction), which suggested the specific binding.
我们研究了[7-甲基-¹¹C]-(E)-8-(3,4,5-三甲氧基苯乙烯基)-1,3,7-三甲基黄嘌呤([¹¹C]TMSX)用于评估肌肉中腺苷A2A受体的潜力。在啮齿动物中，通过A2A选择性拮抗剂CSC和非选择性茶碱阻断，观察到[¹¹C]TMSX在肌肉和心脏中有特异性结合，但A1选择性拮抗剂DPCPX则无此作用。游泳运动使这些组织中的放射性配体-受体结合发生波动。在一项针对两名受试者的PET研究中，静脉输注茶碱使[¹¹C]TMSX在心脏中的分布容积略有降低(降低20%)，在肌肉中的分布容积也略有降低(降低10%)，这表明存在特异性结合。
