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用于检测眼部黑色素瘤的潜在放射性药物。第三部分。一项关于¹⁴C和¹¹C标记的酪氨酸及二羟基苯丙氨酸的研究。

Potential radiopharmaceuticals for the detection of ocular melanoma. Part III. A study with 14C and 11C labelled tyrosine and dihydroxyphenylalanine.

作者信息

van Langevelde A, van der Molen H D, Journée-de Korver J G, Paans A M, Pauwels E K, Vaalburg W

机构信息

Department of Pharmacology, University, Sylvius Laboratories, Leiden, The Netherlands.

出版信息

Eur J Nucl Med. 1988;14(7-8):382-7. doi: 10.1007/BF00254389.

Abstract

In order to investigate the possibility of using [1-11C] labelled 3,4-dihydroxyphenylalanine (DOPA) and tyrosine as radiopharmaceuticals for the detection of eye melanoma, the biodistributions of the same 1- and 3-14C-labelled compounds were investigated in Syrian golden hamsters with Greene melanoma. The results of these investigations were compared with positron emission tomography (PET) images of 11C labelled DOPA and tyrosine. The synthesis of these 11C labelled compounds procures of DL mixture, from which D and L forms can be separated. One h after intravenous injection, both 14C labelled DL-, L- and D-DOPA showed a high uptake in tumour tissue, that of DL- and D-DOPA being the highest. These high uptakes, together with relatively low uptake in bone, skin and eye resulted in high tumour/non tumour ratio (for DL-DOPA 5.9, 4.5 and 6.6 respectively). Extraction of the tumour tissue with trichloroacetic acid showed that L-DOPA was mainly incorporated into melanin, whereas D-DOPA was not. Also, the uptake 1 h after intravenous injection of 1-14C-L- and DL-tyrosine into the tumour were high, but L- and DL- were less different; tumour/non tumour ratios were favorable. PET images of the tumour obtained 40-80 min after injection of the [1-11C] labelled DOPA and tyrosine confirmed that melanoma detection was promising and that D-DOPA produced a better melanoma image than L-DOPA.

摘要

为了研究使用[1-¹¹C]标记的3,4-二羟基苯丙氨酸(DOPA)和酪氨酸作为放射性药物检测眼黑色素瘤的可能性,研究了相同的¹⁴C标记的1-和3-DOPA及酪氨酸在患有格林黑色素瘤的叙利亚金仓鼠体内的生物分布。将这些研究结果与¹¹C标记的DOPA和酪氨酸的正电子发射断层扫描(PET)图像进行了比较。这些¹¹C标记化合物的合成得到了DL混合物,其中D型和L型可以分离。静脉注射后1小时,¹⁴C标记的DL-、L-和D-DOPA在肿瘤组织中均有高摄取,DL-和D-DOPA的摄取最高。这些高摄取,再加上在骨骼、皮肤和眼睛中的相对低摄取,导致了高肿瘤/非肿瘤比值(DL-DOPA分别为5.9、4.5和6.6)。用三氯乙酸提取肿瘤组织表明,L-DOPA主要掺入黑色素中,而D-DOPA则不然。此外,静脉注射¹⁴C-L-和DL-酪氨酸后1小时肿瘤对其摄取也很高,但L-和DL-的差异较小;肿瘤/非肿瘤比值良好。注射[1-¹¹C]标记的DOPA和酪氨酸后40 - 80分钟获得的肿瘤PET图像证实,检测黑色素瘤是有前景的,且D-DOPA产生的黑色素瘤图像比L-DOPA更好。

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