Radiolabeling of a high potency cannabinoid subtype-1 receptor ligand, N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl)-indole-1-sulfonyl)benzamide (PipISB), with carbon-11 or fluorine-18
Radiolabeling of a high potency cannabinoid subtype-1 receptor ligand, N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl)-indole-1-sulfonyl)benzamide (PipISB), with carbon-11 or fluorine-18
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DOI：
10.1002/jlcr.1491
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发表时间：
2008-03-15
影响因子：
1.8
通讯作者：
Pike, Victor W.
中科院分区：
文献类型：
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作者：
Donohue, Sean R.;Halldin, Christer;Pike, Victor W.
PipISB [N-(4-氟-苄基)-4-(3-(哌啶-1-基)-吲哚-1-磺酰基)苯甲酰胺, 9] 被鉴定为选择性高效 CB1 受体配体。在这里，我们描述了用正电子发射体标记 9 ，为利用正电子发射断层扫描 (PET) 对大脑 CB1 受体进行成像提供候选放射性配体。 9的放射性标记通过两种方法实现，方法A使用碳11，方法B使用氟18。在方法A中，[C-11]9由[C-11]一氧化碳一步制备，而[C-11]一氧化碳本身由回旋加速器产生的[C-11]二氧化碳制备。在方法B中，以[18F]4-氟-苄基溴作为标记剂，通过两阶段、四步合成，由回旋加速器产生的[F-18]氟离子制备[F-18]9。方法A的放射合成时间为44分钟； [C-11]一氧化碳的衰变校正放射化学产率 (RCY) 范围为 3.1 至 11.6%，比放射性范围为 21 至 67 GBq/mu mol。方法B的放射合成时间为115分钟； [F-18]氟离子的 RCY 范围为 1.5 至 5.6%，比放射性范围为 200 至 348 GBq/mu mol。通过这些方法，可以以足够的活性和质量制备[C-11]9和[F-18]9，用于未来作为PET放射性配体的评估。
PipISB [N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl)-indole-1-sulfonyl)benzamide, 9] was identified as a selective high potency CB, receptor ligand. Here we describe the labeling of 9 with positron-emitters to provide candidate radioligands for imaging brain CB1 receptors with positron emission tomography (PET). The radiolabeling of 9 was achieved by two methods, method A with carbon-11 and method B with fluorine-18. In method A, [C-11]9 was prepared in one step from [C-11]carbon monoxide, itself prepared from cyclotron-produced [C-11]carbon dioxide. In method B, [F-18]9 was prepared from cyclotron-produced [F-18]fluoride ion in a two-stage, four-step synthesis with [18F]4-fluoro-benzyl bromide as a labeling agent. The radiosynthesis time for method A was 44 min; decay-corrected radiochemical yields (RCYs) from [C-11]carbon monoxide ranged from 3.1 to 11.6% and specific radioactivities ranged from 21 to 67 GBq/mu mol. The radiosynthesis time for method B was 115 min; RCYs from [F-18]fluoride ion ranged from 1.5 to 5.6% and specific radioactivities ranged from 200 to 348 GBq/mu mol. With these methods, [C-11]9 and [F-18]9 may be prepared in adequate activity and quality for future evaluation as PET radioligands.