3H-SCH 23390在体内与多巴胺D1受体的特异性结合。

Specific binding of 3H-SCH 23390 to dopamine D1 receptors in vivo.

作者信息

Andersen P H, Grønvald F C

出版信息

Life Sci. 1986 Apr 21;38(16):1507-14. doi: 10.1016/0024-3205(86)90564-3.

Abstract

The binding of 3H-SCH 23390 was studied in vivo in the mouse brain. The binding was saturable, reversible and stereospecific. The level of nonspecific binding was 5-15% of total binding. Pharmacological characterization revealed binding of 3H-SCH 23390 to D1 receptors. Thus, dopaminergic antagonists known to possess D1 affinity, e.g., SCH 23390 itself, cis-flupentixol and (+)-butaclamol, were potent inhibitors of the 3H-SCH 23390 binding. On the other hand, high doses of D2 selective compounds were required to inhibit the 3H-SCH 23390 binding. These results indicate that 3H-SCH 23390 is a ligand of choice for in vivo studies of D1 receptors.

摘要

在小鼠脑内对³H-SCH 23390的结合进行了体内研究。该结合具有饱和性、可逆性和立体特异性。非特异性结合水平为总结合的5 - 15%。药理学特性表明³H-SCH 23390与D1受体结合。因此，已知具有D1亲和力的多巴胺能拮抗剂，如SCH 23390本身、顺式氟哌噻吨和(+)-丁酰苯，是³H-SCH 23390结合的强效抑制剂。另一方面，需要高剂量的D2选择性化合物才能抑制³H-SCH 23390的结合。这些结果表明³H-SCH 23390是用于D1受体体内研究的理想配体。