Inositol Phospholipid Hydrolysis in Rat Cerebral Cortical Slices: I. Receptor Characterisation
Inositol Phospholipid Hydrolysis in Rat Cerebral Cortical Slices: I. Receptor Characterisation
复制标题
大鼠大脑皮质切片中的肌醇磷脂水解：I. 受体表征
DOI：
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发表时间：
1984
影响因子：
4.7
通讯作者：
S. Nahorski
中科院分区：
文献类型：
--
作者：
Elaine H. Brown;D. Kendall;S. Nahorski
摘要：使用直接测定法（包括[3 H]肌醇预标记）对大鼠皮质切片中受体介导的肌醇磷脂分解进行了表征。当切片与[3 H]肌醇预孵育时，发现锂大大增强了受体激动剂（如卡巴胆碱、去甲肾上腺素和5-羟色胺）增加肌醇磷酸盐中放射性含量的能力。使用多种激动剂和拮抗剂，可以表明胆碱能毒蕈碱受体、α1肾上腺素受体和组胺H1受体似乎与皮质中的肌醇磷脂分解有关。受体激动剂产生的大的反应允许完全和部分激动剂之间的明确区分以及每个受体的竞争性拮抗剂的定量分析。而卡巴胆碱和乙酰胆碱（在胆碱酯酶抑制剂的存在下）是完全激动剂，oxotremorine和槟榔碱只是部分激动剂。极低浓度的阿托品使卡巴胆碱剂量反应曲线向右移动，并使拮抗剂的抑制常数易于计算。烟碱拮抗剂美加明无效。去甲肾上腺素和肾上腺素是α1-肾上腺素受体的完全激动剂，但苯肾上腺素和甲氧胺可能是部分激动剂。哌唑嗪，但不是育亨宾，有力和竞争性拮抗去甲肾上腺素肌醇磷脂反应。甲吡胺而不是西咪替丁竞争性拮抗组胺反应。这些数据为锂对神经递质肌醇磷脂分解的增强作用提供了强有力的证实，并强调了在许多皮层受体的功能反应可以表征的容易性。
Abstract: Characterisation of receptor‐mediated breakdown of inositol phospholipids in rat cortical slices has been performed using a direct assay which involves prelabelling with [3H]inositol. When slices were preincubated with [3H]inositol, lithium was found to greatly amplify the capacity of receptor agonists such as carbachol, noradrenaline, and 5‐hydroxytryptamine to increase the amount of radioactivity appearing in the inositol phosphates. Using a large variety of agonists and antagonists it could be shown that cholinergic muscarinic, α1,‐adrenoceptor, and histamine H1, receptors appear to be linked to inositol phospholipid breakdown in cortex. The large responses produced by receptor agonists allowed a clear discrimination between full and partial agonists as well as quantitative analysis of competitive antagonists for each receptor. Whereas carbachol and acetylcholine (in the presence of a cholinesterase inhibitor) were full agonists, oxotremorine and arecoline were only partial agonists. Very low concentrations of atropine shifted the carbachol dose‐response curve to the right and allowed inhibition constants for the antagonist to be easily calculated. The nicotinic antagonist, mecamylamine, was ineffective. Noradrenaline and adrenaline were full agonists at α1‐adrenoceptors, but phenylephrine and probably methoxamine were partial agonists. Prazosin, but not yohimbine, potently and competitively antagonised the noradrenaline inositol phospholipid response. Mepyramine but not cimetidine competitively antagonised the histamine response. These data provide strong confirmation for the potentiating effect of lithium on neurotransmitter inositol phospholipid breakdown and emphasise the ease with which functional responses at a number of cortical receptors can be characterised.
组胺通过直接的 H-1 受体介导机制刺激脑磷脂周转。
影响因子：
6.1
作者：
Subramanian,N;Whitmore,WL;Seidler,FJ;Slotkin,TA
通讯作者：
Slotkin,TA
α去甲肾上腺素能受体参与体内脑多磷酸肌醇代谢的介导。
DOI：
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发表时间：
1982
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Soukup,J;Schanberg,S
通讯作者：
Schanberg,S