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选择性5-HT2A受体拮抗剂123I-5-I-R91150在正常犬体内的生物分布及置换研究。

Biodistribution and displacement studies of the selective 5-HT2A receptor antagonist 123I-5-I-R91150 in the normal dog.

作者信息

Peremans K, Audenaert K, Jacobs F, Dumont F, De Vos F, Van De Wiele C, Vandecapelle M, Van Bree H, Verschooten F, Slegers G, Mertens J, Dierckx R

机构信息

Department of Medical Imaging, Faculty of Veterinary Medicine, Ghent University, Ghent, Belgium.

出版信息

Nucl Med Commun. 2002 Oct;23(10):1019-27. doi: 10.1097/00006231-200210000-00013.

Abstract

There is increasing interest in mapping receptors in vivo by using functional imaging modalities such as single photon emission tomography (SPET) and positron emission tomography (PET). Since SPET is a more accessible functional imaging modality than PET and, overall, it is more economical, radioligands suitable for this technique are in greater demand. Recently, 123I-5-I-R91150, a radioligand with high selectivity and affinity for 5-HT(2A) receptors in the brain, was introduced for SPET. This study reports on the whole-body distribution and brain uptake of the selective 123I-5-I-R91150 ligand in four normal dogs. The frontal to cerebellar ratio of uptake in time was determined in three dogs. Time-activity curve of venous blood was determined in one dog. Maximal global brain uptake was found at 10-60 min post-injection. Higher brain uptake was noted in the frontal cortical areas compared to the cerebellum. The frontal-cerebellar ratio reached the highest values at 90-180 min. Reversibility and pharmacological selectivity of ligand binding was demonstrated through displacement and blocking studies with the 5-HT(2A) receptor antagonist ketanserin. This study demonstrates that the specific 5-HT(2A) iodinated ligand can be used for imaging and semi-quantification of the 5-HT(2A) receptors in the canine brain in vivo by using SPET.

摘要

利用单光子发射断层扫描(SPET)和正电子发射断层扫描(PET)等功能成像方式在体内绘制受体图谱的研究兴趣日益浓厚。由于SPET是一种比PET更容易获得的功能成像方式,而且总体上更经济,因此对适用于该技术的放射性配体的需求更大。最近,一种对大脑中5-HT(2A)受体具有高选择性和亲和力的放射性配体123I-5-I-R91150被引入用于SPET。本研究报告了选择性123I-5-I-R91150配体在四只正常犬体内的全身分布和脑摄取情况。测定了三只犬摄取的额叶与小脑比值随时间的变化。测定了一只犬静脉血的时间-活性曲线。在注射后10-60分钟发现最大全脑摄取量。与小脑相比,额叶皮质区域的脑摄取量更高。额叶-小脑比值在90-180分钟时达到最高值。通过用5-HT(2A)受体拮抗剂酮色林进行置换和阻断研究,证明了配体结合的可逆性和药理选择性。本研究表明,特异性5-HT(2A)碘化配体可通过SPET用于犬脑内5-HT(2A)受体的体内成像和半定量分析。

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