使用非肽配体对促肾上腺皮质激素释放激素1型受体进行放射自显影可视化：[(76)Br]MJL-1-109-2的合成。
Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2.
作者信息
Jagoda Elaine, Contoreggi Carlo, Lee Mei-Jing, Kao Chih-Hao K, Szajek Lawrence P, Listwak Sam, Gold Philip, Chrousos George, Greiner Elisabeth, Kim B Moon, Jacobson Arthur E, Rice Kenner C, Eckelman William
机构信息
PET Department, Warren G. Magnuson Clinical Center, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892, USA.
出版信息
J Med Chem. 2003 Aug 14;46(17):3559-62. doi: 10.1021/jm034077k.
A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood-brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.
合成了一种用于促肾上腺皮质激素释放激素受体1（CRHR1）的高亲和力非肽放射性配体，并通过体外放射自显影显示其在大鼠脑中的分布与CRHR1一致。这是首个兼具高亲和力和适当亲脂性的非肽放射性示踪剂，能够穿透血脑屏障，因此有潜力用于正电子发射断层扫描（PET）成像研究。对CRH1受体变化或其占有率进行体内可视化，将有助于进一步了解应激相关疾病的病理生理学。
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