[11C]TMSX 通过正电子发射断层扫描评估骨骼肌中腺苷 A2A 受体的潜力。

Potential of [11C]TMSX for the evaluation of adenosine A2A receptors in the skeletal muscle by positron emission tomography.

作者信息

Ishiwata Kiichi, Mizuno Masaki, Kimura Yuichi, Kawamura Kazunori, Oda Keiichi, Sasaki Toru, Nakamura Yoshio, Muraoka Isao, Ishii Kenji

机构信息

Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, 1-1 Naka-cho, Itabashi-ku, Tokyo 173-0022, Japan.

出版信息

Nucl Med Biol. 2004 Oct;31(7):949-56. doi: 10.1016/j.nucmedbio.2004.06.003.

DOI:10.1016/j.nucmedbio.2004.06.003

PMID:15464397

Abstract

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.

摘要

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。