Olgiati V, Quirion R, Bowen W D, Pert C B
Life Sci. 1982;31(16-17):1675-8. doi: 10.1016/0024-3205(82)90183-7.
Recent evidence suggests that the Type 1 opiate receptor (in rat striatal patches) is a mobile receptor which is able to adopt a mu, delta, or kappa opiate receptor ligand selectivity pattern under appropriate conditions. In this paper, we have investigated such a possibility for Type 2 opiate receptors which are visualized diffusely over rat striatum. Ligand selectivity analysis suggested that the Type 2 opiate binding site is equivalent to a delta opiate receptor. The auto-radiographic distribution of Type 2 opiate binding sites is diffuse over most areas of rat brain. Thus, Type 2 opiate binding sites are different from Type 1 opiate receptors which are very discretely distributed in rat brain. Our results suggest that Type 2 opiate receptors, unlike Type 1 opiate receptors, are receptors locked in a delta-like ligand selectivity conformation.
最近的证据表明，1型阿片受体（在大鼠纹状体斑块中）是一种移动受体，在适当条件下能够呈现μ、δ或κ阿片受体配体选择性模式。在本文中，我们研究了在大鼠纹状体中广泛可见的2型阿片受体存在这种可能性。配体选择性分析表明，2型阿片结合位点等同于δ阿片受体。2型阿片结合位点的放射自显影分布在大鼠脑的大部分区域是弥散的。因此，2型阿片结合位点与在大鼠脑中分布非常离散的1型阿片受体不同。我们的结果表明，与1型阿片受体不同，2型阿片受体是锁定在δ样配体选择性构象中的受体。
