荧光阿片受体探针的合成与药理学特性研究。

Synthesis and pharmacological characterization of fluorescent opioid receptor probes.

机构信息

Department of Chemistry and Biochemistry, Southern Illinois University, Carbondale, Illinois, 62901, USA.

出版信息

Pharm Res. 1985 Nov;2(6):266-71. doi: 10.1023/A:1016385416294.

Abstract

A series of five fluorescent opioid receptor probes was synthesized by coupling naloxone, oxymorphone or naltrexone with fluorescein or tetramethylrhodamine B. The series was characterized for capacity to displace (3)H-dihydromorphine from rat brain opioid receptors. All compounds showed receptor binding, and 1-(N)-fluoresceinyl naltrexone thiosemicarbazone displayed the highest mu-receptor affinity with a Ki value of 3 nM. l-(N)-fluoresceinyl naloxone thiosemicarbazone was a morphine antagonist in vivo, approximately 6 % as potent as naloxone and naloxonazine in the mouse hot-plate test.

摘要

通过将纳洛酮、羟吗啡酮或纳曲酮与荧光素或四甲基罗丹明 B 偶联，合成了一系列五个荧光阿片受体探针。该系列的特征是能够从大鼠脑阿片受体中置换 (3)H-二氢吗啡。所有化合物均显示出受体结合，并且 1-(N)-荧光素纳曲酮硫代半卡巴腙显示出最高的 mu 受体亲和力，Ki 值为 3 nM。l-(N)-荧光素纳洛酮硫代半卡巴腙在体内是一种吗啡拮抗剂，在小鼠热板试验中约为纳洛酮和纳洛酮嗪的 6%。