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氯胺酮异构体对神经元和神经元外儿茶酚胺摄取机制的不同影响。

Differential effects of ketamine isomers on neuronal and extraneuronal catecholamine uptake mechanisms.

作者信息

Lundy P M, Lockwood P A, Thompson G, Frew R

出版信息

Anesthesiology. 1986 Mar;64(3):359-63. doi: 10.1097/00000542-198603000-00010.

DOI:10.1097/00000542-198603000-00010
PMID:3954131
Abstract

Contractile responses of isolated rabbit aortic strips to epinephrine and norepinephrine were potentiated in a dose-related manner by (+) ketamine but not by (-) ketamine (1.1 X 10(-5) M - 3.7 X 10(-4) M). Potentiation was blocked completely by pretreatment with the extraneuronal uptake inhibitor cortisol (83-138 microM) but was unaffected by the neuronal uptake inhibitor cocaine (29 microM). Responses of the rat anococcygeus muscle to these catecholamines were potentiated by both isomers, with (+) ketamine being more potent than its optical antipode. These effects were blocked completely in tissues from 6-hydroxydopamine sympathectomized animals. Results suggest that inhibition of extraneuronal uptake of catecholamines by racemic ketamine is due solely to an action of the (+) isomer, whereas both isomers appear capable of inhibiting neuronal uptake.

摘要

(+)氯胺酮能以剂量相关的方式增强离体兔主动脉条对肾上腺素和去甲肾上腺素的收缩反应,而(-)氯胺酮则不能(1.1×10⁻⁵ M - 3.7×10⁻⁴ M)。用非神经元摄取抑制剂皮质醇(83 - 138微摩尔)预处理可完全阻断这种增强作用,但神经元摄取抑制剂可卡因(29微摩尔)对其无影响。大鼠肛尾肌对这些儿茶酚胺的反应在两种异构体作用下均增强,(+)氯胺酮比其旋光对映体更有效。这些效应在6 - 羟基多巴胺交感神经切除动物的组织中被完全阻断。结果表明,外消旋氯胺酮对儿茶酚胺非神经元摄取的抑制作用仅归因于(+)异构体的作用,而两种异构体似乎都能够抑制神经元摄取。

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Differential effects of ketamine isomers on neuronal and extraneuronal catecholamine uptake mechanisms.氯胺酮异构体对神经元和神经元外儿茶酚胺摄取机制的不同影响。
Anesthesiology. 1986 Mar;64(3):359-63. doi: 10.1097/00000542-198603000-00010.
2
Ketamine: evidence of tissue specific inhibition of neuronal and extraneuronal catecholamine uptake processes.氯胺酮:对神经元和神经元外儿茶酚胺摄取过程组织特异性抑制的证据。
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Ketamine potentiates catecholamine responses of vascular smooth muscle by inhibition of extraneuronal uptake.氯胺酮通过抑制非神经元摄取来增强血管平滑肌的儿茶酚胺反应。
Can J Physiol Pharmacol. 1981 Jun;59(6):520-7. doi: 10.1139/y81-078.
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