PET-characterization of [carbonyl-C-11]WAY-100635 binding to 5-HT1A receptors in the primate brain
PET-characterization of [carbonyl-C-11]WAY-100635 binding to 5-HT1A receptors in the primate brain
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DOI：
10.1007/s002130050391
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发表时间：
1997-09-01
影响因子：
3.4
通讯作者：
Halldin, C
中科院分区：
文献类型：
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作者：
Farde, L;Ginovart, N;Halldin, C
[carbonyl-C-11]WAY-100635 是一种新型放射性配体，可与正电子发射断层扫描 (PET) 结合使用，为富含 5-HT1A 受体的人脑区域提供高对比度描绘。在本 PET 研究中，[羰基-C-11]WAY-100635 的结合在食蟹猴大脑中进行了表征。用两种参考化合物 WAY-100635 和 8-OH-DPAT 以及药物丁螺环酮和吲哚洛尔进行预处理，可显着抑制[羰基-C-11]WAY-100635 在新皮质和中缝核中的结合。初步的 Scatchard 分析得出的 5-HT1A 受体密度值与体外报道的值相同。该研究表明，[carbonyl-C-11]WAY-100635 与灵长类动物大脑中的 5-HT1A 受体特异性结合，并具有确定精神病患者中 5-HT1A 受体占用率和密度的潜力。
[carbonyl-C-11]WAY-100635 is a new radioligand which can be used with positron emission tomography (PET) to provide high contrast delineation of human brain regions that are rich in 5-HT1A receptors. In the present PET study, the binding of [carbonyl-C-11]WAY-100635 was characterized in the cynomolgus monkey brain. Pretreatment with each of the two reference compounds, WAY-100635 and 8-OH-DPAT, as well as the drugs buspirone and pindolol, induced a marked inhibition of [carbonyl-C-11]WAY-100635 binding in the neocortex and the raphe nuclei, A preliminary Scatchard analysis yielded 5-HT1A receptor density values of the same order as those that have been reported in vitro. The study shows that [carbonyl-C-11]WAY-100635 binds specifically to 5-HT1A receptors in the primate brain and has potential for determination of 5-HT1A receptor occupancy and density in psychiatric patients.