Chang W H, Wu H S, Tseng Y T
Taipei City Psychiatric Center, Taiwan, Republic of China.
Biol Psychiatry. 1987 Nov;22(11):1369-74. doi: 10.1016/0006-3223(87)90071-0.
The effects of acute administration of reduced haloperidol (RHAL) on homovanillic acid (HVA) in the caudate and prefrontal cortex were examined in rats. Haloperidol (HAL) was used as a reference compound. Concentrations of HVA and HAL were measured by HPLC/ECD. The maximal HVA response time was 3 hr after the injection, in both caudate and prefrontal cortex, for both RHAL and HAL. The potency of RHAL in the elevations of HVA in the caudate and prefrontal cortex was only about one-third to one-fifth that of HAL. The concentrations of HAL in the prefrontal cortex and caudate after RHAL administration were just about one-third to one-fifth those after HAL administration. These results suggest that less antidopaminergic activity of RHAL in this neuroleptic test might be explained by the lesser conversion of RHAL to HAL.
在大鼠中研究了急性给予还原氟哌啶醇（RHAL）对尾状核和前额叶皮质中高香草酸（HVA）的影响。氟哌啶醇（HAL）用作参考化合物。通过高效液相色谱/电化学检测法（HPLC/ECD）测量HVA和HAL的浓度。对于RHAL和HAL，尾状核和前额叶皮质中HVA的最大反应时间均为注射后3小时。RHAL在尾状核和前额叶皮质中升高HVA的效力仅约为HAL的三分之一至五分之一。给予RHAL后前额叶皮质和尾状核中HAL的浓度约为给予HAL后的三分之一至五分之一。这些结果表明，在该抗精神病药物测试中，RHAL较低的抗多巴胺能活性可能是由于RHAL向HAL的转化率较低所致。
