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1
The synthesis and pharmacology of some 1,4,5,6-tetrahydropyrimidines.某些1,4,5,6 - 四氢嘧啶的合成与药理学
Br J Pharmacol. 1969 Oct;37(2):425-35. doi: 10.1111/j.1476-5381.1969.tb10579.x.
2
[Blocking of the neuromuscular conduction by decamethylene-bis-pyridinium].[十亚甲基双吡啶对神经肌肉传导的阻滞作用]
Farmakol Toksikol. 1970 Sep-Oct;33(5):536-8.
3
Further studies on the neuromuscular effects of beta-diethylaminoethyl-diphenyl propylacetate hydrochloride (SKF-525-A).
Arch Int Pharmacodyn Ther. 1969 Jan;177(1):185-95.
4
Pharmacology of some acetylcholine homologues.某些乙酰胆碱同系物的药理学
Br J Pharmacol. 1970 May;39(1):40-8. doi: 10.1111/j.1476-5381.1970.tb09554.x.
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A comparison between the blocking actions of 2-(4-phenylpiperidino) cyclohexanol (AH 5183) and its N-methyl quaternary analogue (AH 5954).2-(4-苯基哌啶基)环己醇(AH 5183)及其N-甲基季铵类似物(AH 5954)阻断作用的比较。
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[Neuro-muscular and ganglionic effects of quaternary bis-ammonium compounds derived from phosphoric acid].[磷酸衍生的季铵双铵化合物的神经肌肉和神经节效应]
Arch Int Pharmacodyn Ther. 1969 Apr;178(2):269-84.
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Some pharmacodynamic effects of the nematocides: methyridine, tetramisole and pyrantel.杀线虫剂:甲噻嘧啶、四咪唑和噻嘧啶的一些药效学作用。
J Pharm Pharmacol. 1970 Jan;22(1):26-36. doi: 10.1111/j.2042-7158.1970.tb08380.x.
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Studies on the neuromuscular effects of beta-diethylaminoethyl-diphenyl propylacetate hydrochloride (SKF-525-A).盐酸β-二乙氨基乙基二苯基丙基乙酸酯(SKF-525-A)的神经肌肉效应研究。
Arch Int Pharmacodyn Ther. 1968 May;173(1):133-43.
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Sites of action of SKF 525-A in nerve and muscle.SKF 525 - A在神经和肌肉中的作用位点。
J Pharmacol Exp Ther. 1970 Mar;172(1):33-43.
10
[Mechanism of action of diethylaminoethyl ether of diphenylpropylacetic acid (SKF-525A) on the neuromuscular synapse].[二苯基丙乙酸二乙氨基乙醚(SKF - 525A)对神经肌肉突触的作用机制]
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An updated review of fatty acid residue-tethered heterocyclic compounds: synthetic strategies and biological significance.脂肪酸残基连接的杂环化合物的最新综述:合成策略与生物学意义
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Investigation of the Possible Pharmacologically Active Forms of the Nicotinic Acetylcholine Receptor Agonist Anabaseine.关于烟碱型乙酰胆碱受体激动剂安非他命可能的药理学活性形式的研究。
Mar Drugs. 2019 Oct 29;17(11):614. doi: 10.3390/md17110614.
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Synthesis of -substituted aryl amidines by strong base activation of amines.通过胺的强碱活化合成α-取代芳基脒
Tetrahedron Lett. 2015 Jul 1;56(27):4109-4111. doi: 10.1016/j.tetlet.2015.05.029.

本文引用的文献

1
The isolated chick biventer cervicis nerve-muscle preparation.离体鸡颈二腹肌神经-肌肉标本。
Br J Pharmacol Chemother. 1960 Sep;15(3):410-1. doi: 10.1111/j.1476-5381.1960.tb01264.x.
2
A new biological method for the assay of depolarizing substances using the isolated semispinalis muscle of the chick.一种使用鸡的离体半棘肌测定去极化物质的新生物学方法。
Br J Pharmacol Chemother. 1960 Sep;15(3):412-6. doi: 10.1111/j.1476-5381.1960.tb01265.x.
3
The ganglion-stimulating effects of some amino-acid esters.某些氨基酸酯的神经节刺激作用。
Br J Pharmacol. 1968 Oct;34(2):358-69. doi: 10.1111/j.1476-5381.1968.tb07057.x.
4
The cholinergic properties of some amino-acid esters and amides.某些氨基酸酯和酰胺的胆碱能特性。
Br J Pharmacol. 1968 Oct;34(2):345-57. doi: 10.1111/j.1476-5381.1968.tb07056.x.

某些1,4,5,6 - 四氢嘧啶的合成与药理学

The synthesis and pharmacology of some 1,4,5,6-tetrahydropyrimidines.

作者信息

Brimblecombe R W, Hunt R R, Rickard R L, Taylor J V

出版信息

Br J Pharmacol. 1969 Oct;37(2):425-35. doi: 10.1111/j.1476-5381.1969.tb10579.x.

DOI:10.1111/j.1476-5381.1969.tb10579.x
PMID:5348429
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1703675/
Abstract
  1. Several 1- and 2-substituted, and 1,2-disubstituted, 1,4,5,6-tetrahydropyrimidines have been prepared and their toxicological and pharmacological properties have been investigated.2. In general the compounds were neuromuscular blocking agents with the monosubstituted members of the series showing a depolarizing type of activity and the disubstituted compounds a non-depolarizing type.3. The toxicity to mice of some of the monosubstituted compounds was increased by pretreatment of the animals with SKF 525A, but the toxicity of the disubstituted compounds was unaffected.4. The results obtained with these compounds are not at variance with a suggestion made previously that nicotinic action at the neuromuscular junction can result from an interaction between drug and receptor at two points separated by about 4 A.
摘要
  1. 已经制备了几种1-和2-取代以及1,2-二取代的1,4,5,6-四氢嘧啶,并对它们的毒理学和药理学性质进行了研究。

  2. 一般来说,这些化合物是神经肌肉阻滞剂,该系列的单取代成员表现出去极化型活性,而二取代化合物表现出非去极化型活性。

  3. 用SKF 525A预处理动物会增加一些单取代化合物对小鼠的毒性,但二取代化合物的毒性不受影响。

  4. 用这些化合物获得的结果与先前提出的一种观点一致,即在神经肌肉接头处的烟碱样作用可能源于药物与受体在相距约4埃的两个位点之间的相互作用。