大脑皮层~3H-三环哌酯结合位点的药理学特征 |
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引用本文: | 汪海 崔文玉. 大脑皮层~3H-三环哌酯结合位点的药理学特征[J]. 中国药理学通报, 1998, 14(3): 224-226 |
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作者姓名: | 汪海 崔文玉 |
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作者单位: | 军事医学科学院毒物药物研究所 |
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摘 要: | 目的研究大脑皮层3H-三环哌酯(3H-TCPN)结合位点的药理学特征。方法在大鼠大脑皮层匀浆标本上,测定3H-TCPN的特异性结合位点以及药物对它的影响。结果3H-TCPN与大鼠大脑皮层膜标本具有特异性结合,其饱和性结合的参数与3H-QNB的饱和性结合参数相似,其中,Kd值为0.40nmol·L-1,Bmax值为1258pmol·g-1。3H-TCPN特异性结合位点中,被阿托品取代的M受体部分占70%,不被阿托品取代的称X位点部分占30%;X结合位点既不为N受体激动剂烟碱和非竞争拮抗剂美加明所占据,也不为GABA受体拮抗剂苦味毒素,甘氨酸受体拮抗剂士的宁和胆碱酯酶抑制剂毒扁豆碱所占据。结论大鼠大脑皮层3H-TCPN特异性结合位点中,70%为M受体,其它位点的药理学性质有待进一步研究
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关 键 词: | 盐酸三环哌酯;受体,胆碱能;烟碱 |
Pharmacological profiles of 3H tricyclopinate hydrochloride binding sites in cerebral cortex |
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Abstract: | AIM To study the pharmacological profiles of 3H tricyclopinate hydrochloride (3H TCPN) binding sites in cerebral cortex. METHODS The specific binding of 3H TCPN and displacement of the drugs on the specific binding were determined in rat cerebral homogenates.RESULTS The specific binding of 3H TCPN in rat cerebral homogenates was saturable, the apparent dissociation constant value was 04 nmol·L-1. 70% of the 3H TCPN(10 nmol·L-1) specific binding could be displaced by atropine(1 μmol·L-1); the other 30% fractions could not be displaced by nicotinic receptor agonist nicotine, nicotinic receptor antagonist mecamylamine, GABA receptor antagonist picrotoxin, glycine receptor antagonist strychnine or cholinesterase inhibitor physostigmine at high concentration of 10 μmol·L-1. CONCLUSION The 70% of the 3H TCPN specific binding sites revealed muscarinic receptor profiles, but the pharmacological characteristics of the other 30% 3H TCPN specific binding sites remained to be further investigated. |
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Keywords: | tricyclopinate hydrochloride receptors cholinergic nicotine |
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