Gonzalez A M, Sibley D R
Molecular Neuropharmacology Section, National Institute of Neurological Disorders & Stroke, National Institutes of Health, Bethesda, MD 20892.
Eur J Pharmacol. 1995 Jan 5;272(1):R1-3. doi: 10.1016/0014-2999(94)00738-s.
The binding of 3H-7-hydroxy-2-(N,N-di-n-propylamino)tetralin ([3H]7-OH-DPAT) to dopamine D2 and D3 receptors expressed in Chinese hamster ovary (CHO) cells was investigated and compared with [3H]methylspiperone. [3H]7-OH-DPAT labeled the D3 receptor in the CHO cells in a guanine nucleotide-insensitive fashion and exhibited a Kd of about 0.5 nM. In the presence of MgCl2. [3H]7-OH-DPAT was also found to label the D2 receptor in CHO cells with high affinity (3.6 nM). The binding of [3H]7-OH-DPAT to the D2 receptor was sensitive to guanine nucleotides suggesting occupancy of a high affinity G protein-coupled state of the receptor. These results suggest that caution should be exercised when using [3H]7-OH-DPAT to label the dopamine D3 receptor in brain tissues.
研究了3H-7-羟基-2-(N,N-二正丙基氨基)四氢萘([3H]7-OH-DPAT)与中国仓鼠卵巢(CHO)细胞中表达的多巴胺D2和D3受体的结合,并与[3H]甲基螺哌隆进行了比较。[3H]7-OH-DPAT以鸟嘌呤核苷酸不敏感的方式标记CHO细胞中的D3受体,其解离常数(Kd)约为0.5 nM。在MgCl2存在的情况下,还发现[3H]7-OH-DPAT以高亲和力(3.6 nM)标记CHO细胞中的D2受体。[3H]7-OH-DPAT与D2受体的结合对鸟嘌呤核苷酸敏感,表明该受体处于高亲和力G蛋白偶联状态。这些结果表明,在使用[3H]7-OH-DPAT标记脑组织中的多巴胺D3受体时应谨慎。