Yokoo H, Goldstein M, Meller E
New York University Medical Center, Neurochemistry Research Laboratories 10016.
Eur J Pharmacol. 1988 Oct 18;155(3):323-7. doi: 10.1016/0014-2999(88)90523-7.
Electrically stimulated release of [3H]dopamine [( 3H]DA) in slices of rat striatum was dose dependently inhibited by apomorphine (67% maximal inhibition) with an EC50 of 17 nM. DA receptor inactivation with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ; 0.5 and 2 mg/kg) dose dependently shifted the ED50 for apomorphine to the right and reduced the maximal inhibition obtained. Analysis of the results yielded a hyperbolic plot of receptor occupancy vs. response, indicating that a large receptor reserve (50-60%) for apomorphine exists at the DA autoreceptor in rat striatum mediating inhibition of transmitter release.
在大鼠纹状体切片中，阿扑吗啡以剂量依赖性方式抑制电刺激诱发的[3H]多巴胺（[3H]DA）释放（最大抑制率为67%），半数有效浓度（EC50）为17 nM。用N-乙氧羰基-2-乙氧基-1,2-二氢喹啉（EEDQ；0.5和2 mg/kg）使多巴胺受体失活，可使阿扑吗啡的半数有效剂量（ED50）剂量依赖性地右移，并降低所获得的最大抑制率。对结果的分析得出了受体占有率与反应的双曲线图，表明在大鼠纹状体多巴胺自身受体处存在大量（50 - 60%）阿扑吗啡受体储备，介导对递质释放的抑制。
