Imaging benzodiazepine receptors in man with [11C]suriclone by positron emission tomography.
Imaging benzodiazepine receptors in man with [11C]suriclone by positron emission tomography.
复制标题
通过正电子发射断层扫描使用[11C]舒立克隆对人体苯二氮卓受体进行成像。
DOI：
10.1016/0014-2999(86)90422-x
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发表时间：
1986
影响因子：
5
通讯作者：
Snyder,SH
中科院分区：
文献类型：
--
作者：
Frost,JJ;WagnerJr,HN;Dannals,RF;Ravert,HT;Wilson,AA;Links,JM;Rosenbaum,AE;Trifiletti,RR;Snyder,SH
人体内多巴胺（Wagner et al., 1983）和阿片（Frost et al., 1985）受体的正电子发射断层扫描（PET）成功成像，在很大程度上取决于[11C] n -甲基spiperone和[11C]卡芬太尼这两种配体对多巴胺和阿片受体的极高亲和力（KD-0.1 nM）。受体的PET成像要求大脑中几乎所有的放射配体都与受体结合，这是亲和力较低的配体所不能满足的条件。苯二氮卓(BZD)-氨基丁酸（GABA）受体复合物具有潜在的临床重要性，因为GABA与癫痫、焦虑和神经退行性疾病有关。氟硝西泮（FNZ）是一种有效的BZD激动剂，作为一种配体，在体内结合研究中相对不成功。在0℃时，FNZ对受体位点的亲和力为-1.0 nM KD，而在37℃时，FNZ与其他BZDs的亲和力降低了10倍。BZD拮抗剂Ro15-1788在0℃时比FNZ更有效，但在0℃时的亲和力也比37℃时高10倍；[HC] Ro15-1788确实提供了人类和狒狒BZD/GABA受体的PET图像（Hantraye et al., 1984; Persson et al., 1985）。
Successful imaging by positron emission tomography (PET) of dopamine (Wagner et al., 1983) and opiate (Frost et al., 1985) receptors in man has depended in large part on the extremely high affinity (KD-0.1 nM) of the ligands,[11C] N-methylspiperone and [11C] carfentanil, for dopamine and opiate receptors respectively. PET imaging of receptors requires that almost all the radioligand in the brain be bound to receptors, a condition which is not fulfilled with ligands of lesser affinity. The benzodiazepine (BZD)-yaminobutyric acid (GABA) receptor complex has potential clinical importance, because GABA has been implicated in epilepsy, anxiety, and neurodegenerative disease.Flunitrazepam (FNZ), a potent BZD agonist, has been relatively unsuccessful as a ligand for in vivo binding studies. While at 0 C FNZ displays-1.0 nM KD for receptor sites, the affinity of FNZ and other BZDs decreases 10-fold at 37 C. The BZD antagonist Ro15-1788 is more potent in vitro at 0 C than FNZ, but also has ten times higher affinity at 0 as at 37 C;[HC] Ro15-1788 does provide PET images of BZD/GABA receptors in man and baboon (Hantraye et al., 1984; Persson et al., 1985).