GABAB receptor inhibition causes locomotor stimulation in mice
GABAB receptor inhibition causes locomotor stimulation in mice
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DOI：
10.1016/s0014-2999(01)01494-7
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发表时间：
2001-12-14
影响因子：
5
通讯作者：
Gessa, GL
中科院分区：
文献类型：
--
作者：
Colombo, G;Melis, S;Gessa, GL
本研究研究了GABA（B）受体拮抗剂SCH 50911 [（2S）（+）-5，5-二甲基-2-吗啉乙酸]、CGP 46381 [（3-氨基丙基）（环己基甲基）次膦酸]和CGP 52432（3-[[（3，4-二氯苯基）甲基]氨基]丙基]二乙氧基甲基）次膦酸）给药对小鼠自发活动的影响。所有药物均以10和30 mg/kg（i. p.）的剂量急性给药。所有药物的30 mg/kg剂量均导致自发活动的显著刺激。氟哌啶醇（0.1 mg/kg，i. p.）完全阻断SCH 50911引起的自发刺激，表明GABA（B）受体阻断诱导的活动过度是由多巴胺释放增强介导的。这些结果表明存在GABA（B）受体介导的多巴胺神经元的紧张性抑制。(C)2001爱思唯尔科技有限公司。保留所有权利。
The present study investigated the effect of the administration of the GABA(B) receptor antagonists, SCH 50911 [(2S)(+)-5,5-dimethyl-2-morpholineacetic acid], CGP 46381 [(3-aminopropyl)(cyclohexylmethyl)phosphinic acid] and CGP 52432 (3-[[(3,4-dichlorophenyl)methyl]amino]propyl]diethoxymethyl)phosphinic acid), on spontaneous locomotor activity in mice. All drugs were acutely administered at the doses of 10 and 30 mg/kg (i.p.). The dose of 30 mg/kg of all drugs resulted in a significant stimulation of locomotor activity. The locomotor stimulation elicited by SCH 50911 was completely blocked by haloperidol (0.1 mg/kg, i.p.), suggesting that hyperactivity induced by blockade of the GABA(B) receptor is mediated by enhanced dopamine release. These results suggest the existence of a GABA(B) receptor-mediated tonic inhibition of dopamine neurons. (C) 2001 Elsevier Science B.V. All rights reserved.