Lejeune F, Millan M J
Institut de Recherches Servier, Centre de Recherches de Croissy, Croissy-sur-Seine, France.
Eur J Pharmacol. 1995 Mar 14;275(3):R7-9. doi: 10.1016/0014-2999(95)00106-u.
The firing rate of dopaminergic neurones in the ventral tegmental area of anaesthetised rats was dose-dependently (0.31-5.0 micrograms/kg i.v.) inhibited by the dopamine D3 receptor agonist, (+)-7-OH-DPAT (7-hydroxy-2-(di-n-propylamino)tetralin). The selective dopamine D3 receptor antagonist, (+)-S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), dose-dependently (16-125 micrograms/kg i.v.) inhibited the action of (+)-7-OH-DPAT (5 micrograms/kg i.v.); its inactive distomer, (-)-S 17777 (125 micrograms/kg i.v.), was ineffective. Alone, (+)-S 14297 (125 micrograms/kg i.v.) did not modify the firing rate. Haloperidol (16 micrograms/kg i.v.) fully reversed the action of (+)-7-OH-DPAT and, alone, significantly increased firing rate. These data suggest that inhibitory (dendritic) dopamine D3 (auto)receptors control the electrical activity of ventral tegmental area-localised dopaminergic neurones.
多巴胺D3受体激动剂（+）-7-羟基-二丙基氨基四氢萘（（+）-7-OH-DPAT）对麻醉大鼠腹侧被盖区多巴胺能神经元的放电频率有剂量依赖性（静脉注射0.31 - 5.0微克/千克）抑制作用。选择性多巴胺D3受体拮抗剂（+）-S 14297（（+）-[7-（N，N-二丙基氨基）-5,6,7,8-四氢萘并（2,3b）二氢呋喃，2,3-]）对（+）-7-OH-DPAT（静脉注射5微克/千克）的作用有剂量依赖性（静脉注射16 - 125微克/千克）抑制；其无活性的差向异构体（-）-S 17777（静脉注射125微克/千克）无效。单独使用时，（+）-S 14297（静脉注射125微克/千克）不改变放电频率。氟哌啶醇（静脉注射16微克/千克）完全逆转了（+）-7-OH-DPAT的作用，且单独使用时显著提高放电频率。这些数据表明，抑制性（树突状）多巴胺D3（自身）受体控制腹侧被盖区多巴胺能神经元的电活动。
