Pindolol increases extracellular 5-HT while inhibiting serotonergic neuronal activity.

Pindolol increases extracellular 5-HT while inhibiting serotonergic neuronal activity.
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吲哚洛尔增加细胞外 5-HT,同时抑制血清素能神经元活动。

DOI:
10.1016/s0014-2999(99)00430-6
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发表时间:
1999
影响因子:
5
通讯作者:
Jacobs,BL
Jacobs,BL
中科院分区:
医学2区
文献类型:
--
作者:
Fornal,CA;Martín,FJ;Mendlin,A;Metzler,CW;Bjorvatn,B;Jacobs,BL

文献摘要

被引文献

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在自由活动的猫上,观察了β-肾上腺素受体阻滞剂/5-羟色胺(5-HT)1A/1B拮抗剂吲哚洛尔(pindolol)对中缝背核(dorsal raphe nucleus,DRN)多巴胺能神经元单位放电和尾状核细胞外5-HT含量的影响。施用(±)-吲哚洛尔(1和10 mg/kg,s.c.)神经元活性降低,5-HT水平升高,呈剂量和时间依赖性。随后给予WAY-100635 {N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-(2-吡啶基)环己烷甲酰胺}(0.2 mg/kg,s.c.),选择性5-HT 1A受体拮抗剂,可阻断吲哚洛尔诱导的神经元抑制并增强5-HT输出。这些结果表明,吲哚洛尔可能在神经末梢水平起作用,以增加5-HT。
The effects of pindolol, a beta-adrenoceptor blocker/putative 5-hydroxytryptamine (5-HT)1A/1Bantagonist, on both the single-unit activity of serotonergic neurons in the dorsal raphe nucleus (DRN) and extracellular 5-HT levels in the caudate nucleus, were examined in freely moving cats. Administration of (±)-pindolol (1 and 10 mg/kg, s.c.) decreased neuronal activity and increased 5-HT levels in a dose- and time-dependent manner. The subsequent administration of WAY-100635 {N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide} (0.2 mg/kg, s.c.), a selective 5-HT1Areceptor antagonist, blocked pindolol-induced neuronal suppression and potentiated 5-HT output. These results indicate that pindolol may be acting at the level of the nerve terminal to increase 5-HT.