Zarevics P, Weidley E, Setler P
Psychopharmacology (Berl). 1977 Aug 16;53(3):283-8. doi: 10.1007/BF00492365.
The involvement of central alpha-noradrenergic receptors in intracranial self-stimulation (ICSS) was studied. Dose-response curves were established for the blockade of ICSS by the antipsychotic drugs chlorpromazine, thioridazine, clozapine, and pimozide and the alpha-antagonist phenoxybenzamine. Antagonism of the facilitation, produced by the central alpha-agonist clonidine, of flexor withdrawal reflexes in the reserpinized spinal rat was used to assess the central alpha-blocking potency of the same drugs, and dose-response curves were established. No correlation was found between central alpha-blockade, as reflected by the ED50 for blockade of clonidine-facilated spinal reflexes, and the ED50 for blockade of ICSS. Pimozide blocked ICSS at doses virtually devoid of central alpha-blocking activity, while phenoxybenzamine was a potent alpha-antagonist and a weak blocker of ICSS. The lack of correlation between central alpha-blockade and decreased ICSS suggests that alpha-receptors are not critically involved in self-stimulation behavior.
研究了中枢α-去甲肾上腺素能受体在颅内自我刺激（ICSS）中的作用。建立了抗精神病药物氯丙嗪、硫利达嗪、氯氮平和匹莫齐特以及α-拮抗剂酚苄明对ICSS阻断作用的剂量-反应曲线。利用中枢α-激动剂可乐定对利血平化脊髓大鼠屈肌退缩反射的促进作用的拮抗作用，来评估相同药物的中枢α-阻断效力，并建立剂量-反应曲线。可乐定促进的脊髓反射阻断的半数有效剂量（ED50）所反映的中枢α-阻断作用与ICSS阻断的ED50之间未发现相关性。匹莫齐特在几乎没有中枢α-阻断活性的剂量下就能阻断ICSS，而酚苄明是一种强效α-拮抗剂，对ICSS的阻断作用较弱。中枢α-阻断与ICSS降低之间缺乏相关性，这表明α-受体并非自我刺激行为的关键参与者。
