β -肾上腺素能受体放射性示踪剂[11C]卡拉唑尔的制备及体内结合

Marc S. Berridge, Emily H. Cassidy, Andrew H. Terris, Jean-Marc Vesselle
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引用次数: 28

摘要

卡拉唑尔是一种高亲和力的β -肾上腺素能受体拮抗剂,对受体亚型相对非特异性。用碳-11标记该化合物的两个对映体,包括合成所需的标记前体,报道。产率和比活度足以用于正电子断层扫描。生物分布和特异性受体结合研究表明,作为正电子断层扫描的放射性药物,该标记物质值得进一步研究。
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Preparation and in vivo binding of [11C]carazolol, a radiotracer for the beta-adrenergic receptor

Carazolol is a high affinity beta-adrenergic receptor antagonist which is relatively non-specific for the receptor subtypes. The labeling of the two enantiomers of this compound with carbon-11, including the synthesis of the required labeling precursors, is reported. The yield and specific activity are sufficient for use in positron tomography. Biodistribution and specific receptor binding studies show the labeled material to be of interest for further investigation as a radiopharmaceutical for positron tomography.

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