某些毒蕈碱拮抗剂对豚鼠嗅皮层切片影响的定量研究。
A quantitative study of the effects of some muscarinic antagonists on the guinea-pig olfactory cortex slice.
作者信息
Williams S H, Constanti A
机构信息
M.R.C. Neuropharmacology Research Group, Dept. of Pharmacology, School of Pharmacy, London.
出版信息
Br J Pharmacol. 1988 Apr;93(4):855-62. doi: 10.1111/j.1476-5381.1988.tb11472.x.
Abstract
- Muscarinic depression of the electrically-evoked surface-negative field potential (N-wave) was measured in guinea-pig olfactory cortex slices maintained in vitro. 2. The effects of three muscarinic receptor antagonists, pirenzepine, atropine and gallamine on this muscarinic response were analysed in detail. 3. Pirenzepine was a potent competitive antagonist of carbachol (CCh)-evoked responses. Schild plot analysis yielded a pA2 value of 7.9 (Schild slope constrained to unity). A similar analysis for atropine versus CCh responses gave a pA2 of 8.9. 4. Combination experiments using pirenzepine and atropine produced dose-ratio shifts close to those expected for two antagonists competing for a similar receptor site. 5. Gallamine was only a weak antagonist of responses to CCh. 6. Oxotremorine behaved as a competitive antagonist at this muscarinic receptor (pA2 = 6.1). 7. It is concluded that the presynaptic muscarinic receptor mediating depression of the N-wave in the olfactory cortex slice is of the M1-subtype.
摘要
- 在体外培养的豚鼠嗅皮质切片中，测量了毒蕈碱对电诱发的表面负向场电位（N波）的抑制作用。2. 详细分析了三种毒蕈碱受体拮抗剂哌仑西平、阿托品和加拉明对这种毒蕈碱反应的影响。3. 哌仑西平是卡巴胆碱（CCh）诱发反应的强效竞争性拮抗剂。施尔德分析得出pA2值为7.9（施尔德斜率限定为1）。对阿托品与CCh反应进行的类似分析得出pA2为8.9。4. 使用哌仑西平和阿托品的联合实验产生的剂量比变化接近两种拮抗剂竞争相似受体位点时预期的变化。5. 加拉明只是对CCh反应的弱拮抗剂。6. 氧化震颤素在这个毒蕈碱受体上表现为竞争性拮抗剂（pA2 = 6.1）。7. 得出的结论是，介导嗅皮质切片中N波抑制的突触前毒蕈碱受体为M1亚型。
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本文引用的文献
1
A modification of receptor theory.受体理论的一种修正。
Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.
2
Antagonist discrimination between ganglionic and ileal muscarinic receptors.神经节与回肠毒蕈碱受体之间的拮抗剂鉴别
Br J Pharmacol. 1980;71(2):362-4. doi: 10.1111/j.1476-5381.1980.tb10948.x.
3
Pirenzepine distinguishes between different subclasses of muscarinic receptors.哌仑西平可区分毒蕈碱受体的不同亚类。
Nature. 1980 Jan 3;283(5742):90-2. doi: 10.1038/283090a0.
4
Gallamine triethiodide (flaxedil): tetraethylammonium- and pancuronium-like effects in myelinated nerve fibers.三碘季铵酚（弗来西德）：在有髓神经纤维中产生类似四乙铵和泮库溴铵的效应。
Science. 1981 Jun 5;212(4499):1170-2. doi: 10.1126/science.7233212.
5
Muscarinic receptor subtypes: M1 and M2 biochemical and functional characterization.毒蕈碱受体亚型：M1和M2的生化及功能特性
Life Sci. 1982 Dec 27;31(26):2991-8. doi: 10.1016/0024-3205(82)90066-2.
6
7
A unique regulatory profile and regional distribution of [3H]pirenzepine binding in the rat provide evidence for distinct M1 and M2 muscarinic receptor subtypes.大鼠体内[3H]哌仑西平结合的独特调节特征和区域分布为不同的M1和M2毒蕈碱受体亚型提供了证据。
Life Sci. 1983 Jun 27;32(26):3001-11. doi: 10.1016/0024-3205(83)90652-5.
8
Muscarinic receptors in rat sympathetic ganglia.大鼠交感神经节中的毒蕈碱受体。
Br J Pharmacol. 1980 Dec;70(4):577-92. doi: 10.1111/j.1476-5381.1980.tb09777.x.
9
Heterogeneity of presynaptic muscarinic receptors regulating neurotransmitter release in the rat brain.调节大鼠脑内神经递质释放的突触前毒蕈碱受体的异质性
J Pharmacol Exp Ther. 1984 Jan;228(1):209-14.
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