中枢和外周“毒蕈碱敏感型”乙酰胆碱受体的立体特异性比较：用丙环定和三环己哌酯对映体形式的观察结果
A comparison of stereospecificity at central and peripheral 'muscarine-sensitive' acetylcholine receptors: observations with the enantiomeric forms of procyclidine and tricyclamol.
作者信息
Barlow R B, Dawbarn D, Pycock C J
出版信息
Br J Pharmacol. 1981 Feb;72(2):277-80. doi: 10.1111/j.1476-5381.1981.tb09125.x.
Abstract
1 Procyclidine resembles hyoscine in enhancing the effects of amphetamine on ipsiversive turning by mice with a unilateral central dopamine lesion. 2 The stereospecific index for procyclidine is not greater than 10, in contrast to 173 for acetylcholine receptors in ileum from the same mice. 3 This suggests that although the central effects of procyclidine in this test involve acetylcholine receptors similar to those at peripheral sites, they cannot be identical with them unless there are differences at some secondary site, for example, if the weaker enantiomer were a stronger inhibitor of dopamine uptake or if there were a stereoselective uptake process for procyclidine itself.
摘要
- 丙环定在增强苯丙胺对单侧中枢多巴胺损伤小鼠向患侧翻转作用方面类似于东莨菪碱。2. 丙环定的立体特异性指数不大于10，而同一小鼠回肠中乙酰胆碱受体的立体特异性指数为173。3. 这表明，尽管丙环定在该试验中的中枢效应涉及与外周部位相似的乙酰胆碱受体，但除非在某些二级位点存在差异，例如，如果较弱的对映体是更强的多巴胺摄取抑制剂，或者丙环定本身存在立体选择性摄取过程，否则它们不可能完全相同。
相似文献
1
A comparison of stereospecificity at central and peripheral 'muscarine-sensitive' acetylcholine receptors: observations with the enantiomeric forms of procyclidine and tricyclamol.中枢和外周“毒蕈碱敏感型”乙酰胆碱受体的立体特异性比较：用丙环定和三环己哌酯对映体形式的观察结果
Br J Pharmacol. 1981 Feb;72(2):277-80. doi: 10.1111/j.1476-5381.1981.tb09125.x.
2
Differences in the stereospecificity of closely related compounds; a reinvestigation of the enantiomers of procyclidine, benzhexol and their metho- and etho-salts.
J Pharm Pharmacol. 1971 Feb;23(2):90-7. doi: 10.1111/j.2042-7158.1971.tb08618.x.
3
Decrease in muscarinic acetylcholine receptors in the small intestine of mice subjected to repeated cold stress.反复遭受冷应激的小鼠小肠中毒蕈碱型乙酰胆碱受体减少。
Life Sci. 1978 Jun 26;22(24):2197-203. doi: 10.1016/0024-3205(78)90571-4.
4
Muscarinic receptor sub-type in the rat anococcygeus muscle.大鼠肛门尾骨肌中的毒蕈碱受体亚型。
J Pharm Pharmacol. 1983 Jul;35(7):469-70. doi: 10.1111/j.2042-7158.1983.tb04327.x.
5
Apparent activity of 5-methylfurmethide at muscarinic receptors.5-甲基糠甲醚在毒蕈碱受体上的表观活性。
Arch Int Pharmacodyn Ther. 1980 Nov;248(1):69-75.
6
Interaction of phencyclidine and its new adamantyl derivatives with muscarinic receptors.苯环利定及其新型金刚烷基衍生物与毒蕈碱受体的相互作用。
Life Sci. 1980 Jan 14;26(2):89-95. doi: 10.1016/0024-3205(80)90051-x.
7
The interaction of bis-pyridinium oximes with mouse brain muscarinic receptor.
Biochem Pharmacol. 1980 Feb 15;29(4):483-8. doi: 10.1016/0006-2952(80)90366-4.
8
Muscarinic activity and receptor binding of the enantiomers of aceclidine and its methiodide.
Mol Pharmacol. 1982 May;21(3):594-9.
9
10
Structural and stereochemical requirements for muscarinic receptor binding.
Mol Pharmacol. 1979 Mar;15(2):227-34.
本文引用的文献
1
The pharmacological properties of the optical isomers of benzhexol, procyclidine, tricyclamol and related compounds.苯海索、丙环定、三环己丙醇及相关化合物光学异构体的药理学特性。
Br J Pharmacol Chemother. 1955 Sep;10(3):383-6. doi: 10.1111/j.1476-5381.1955.tb00888.x.
2
Temperature changes produced by the injection of catecholamines and 5-hydroxytryptamine into the cerebral ventricles of the conscious mouse.向清醒小鼠脑室注射儿茶酚胺和5-羟色胺所产生的体温变化。
J Physiol. 1967 Oct;192(3):805-13. doi: 10.1113/jphysiol.1967.sp008332.
3
The relation between biological activity and the degree of resolution of optical isomers.生物活性与光学异构体拆分程度之间的关系。
J Pharm Pharmacol. 1972 Oct;24(10):753-61. doi: 10.1111/j.2042-7158.1972.tb08879.x.
4
Differences in the stereospecificity of closely related compounds; a reinvestigation of the enantiomers of procyclidine, benzhexol and their metho- and etho-salts.
J Pharm Pharmacol. 1971 Feb;23(2):90-7. doi: 10.1111/j.2042-7158.1971.tb08618.x.
5
Turning behavior of mice with unilateral 6-hydroxydopamine lesions in the striatum: effects of apomorphine, L-DOPA, amanthadine, amphetamine and other psychomotor stimulants.单侧纹状体6-羟基多巴胺损伤小鼠的转向行为：阿扑吗啡、左旋多巴、金刚烷胺、苯丙胺及其他精神运动兴奋剂的作用
Neuropharmacology. 1973 May;12(5):451-62. doi: 10.1016/0028-3908(73)90061-0.
6
Inhibition of circling behavior by neuroleptic drugs in mice with unilateral 6-hydroxydopamine lesions of the striatum.用神经安定药物抑制纹状体单侧6-羟基多巴胺损伤小鼠的转圈行为。
Psychopharmacologia. 1975 Dec 31;45(2):211-9. doi: 10.1007/BF00429063.
7
The effect of manipulation of cholinergic mechanisms on turning behaviour in mice with unilateral destruction of the nigro-neostriatal dopaminergic system.胆碱能机制调控对黑质 - 新纹状体多巴胺能系统单侧破坏小鼠旋转行为的影响。
Neuropharmacology. 1978 Mar;17(3):175-83. doi: 10.1016/0028-3908(78)90097-7.
Zotero 插件