• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

新型中枢性肌肉松弛剂6-氨基-2-氟甲基-3-(邻甲苯基)-4(3H)-喹唑啉酮(阿夫唑仑)的药理学研究。(II)对脊髓反射电位和强直的影响。

Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity.

作者信息

Ochiai T, Ishida R

出版信息

Jpn J Pharmacol. 1982 Jun;32(3):427-38. doi: 10.1254/jjp.32.427.

DOI:10.1254/jjp.32.427
PMID:7109348
Abstract

Effects of afloqualone on mono- (MSR) and poly-synaptic reflex (PSR) potentials and alpha- and gamma-rigidities were studied in experimental animals. Afloqualone dose dependently inhibited both MSR and PSR potentials in spinalized cats though afloqualone had no inhibitory effect on the patellar reflex in cats as reported in the previous paper. Afloqualone, like tolperisone, more selectively inhibited the PSR potential than MSR potential, whereas baclofen inhibited them in reverse order. However, the selectivity towards the PSR potential was higher with afloqualone than with tolperisone. In rats and cats, afloqualone dose dependently relaxed both alpha- and gamma-rigidity when administered p.o. as well as i.v. Its 50% inhibitory dose for alpha-rigidity was 1.5-2 times larger than that for gamma-rigidity. Tolperisone also relaxed both rigidities in i.v. administration, but had little effect when given p.o. Only mephenesin relaxed the post-ischaemic spinal rigidity in cats. These results suggest that afloqualone, like other well known centrally acting muscle relaxants except for baclofen, more strongly inhibits the polysynaptic pathway than the mono-synaptic pathway of the spinal cord as well as more strongly the gamma-system than the alpha-system.

摘要

在实验动物中研究了阿夫喹酮对单突触反射(MSR)和多突触反射(PSR)电位以及α和γ僵直的影响。阿夫喹酮剂量依赖性地抑制脊髓麻醉猫的MSR和PSR电位,尽管如前文报道,阿夫喹酮对猫的髌反射没有抑制作用。与托哌酮一样,阿夫喹酮对PSR电位的抑制作用比MSR电位更具选择性,而巴氯芬则以相反的顺序抑制它们。然而,阿夫喹酮对PSR电位的选择性高于托哌酮。在大鼠和猫中,口服和静脉注射阿夫喹酮均剂量依赖性地减轻α和γ僵直。其对α僵直的50%抑制剂量比对γ僵直的大1.5 - 2倍。托哌酮静脉注射时也能减轻两种僵直,但口服时作用很小。只有美芬新能减轻猫缺血后脊髓僵直。这些结果表明,与除巴氯芬外的其他知名中枢性肌肉松弛剂一样,阿夫喹酮对脊髓多突触通路的抑制作用比对单突触通路更强,对γ系统的抑制作用比对α系统更强。

相似文献

1
Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity.新型中枢性肌肉松弛剂6-氨基-2-氟甲基-3-(邻甲苯基)-4(3H)-喹唑啉酮(阿夫唑仑)的药理学研究。(II)对脊髓反射电位和强直的影响。
Jpn J Pharmacol. 1982 Jun;32(3):427-38. doi: 10.1254/jjp.32.427.
2
Pharmacological studies of the new centrally acting muscle relaxant 4'-ethyl-2-methyl-3-pyrrolidinopropiophenone hydrochloride.新型中枢性肌肉松弛剂盐酸4'-乙基-2-甲基-3-吡咯烷丙酰苯的药理学研究
Arzneimittelforschung. 1987 Mar;37(3):331-6.
3
[General pharmacology of 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. I. Effects on the central nervous system (author's transl)].新型中枢性肌肉松弛剂6-氨基-2-氟甲基-3-(邻甲苯基)-4(3H)-喹唑啉酮(阿夫唑仑)的一般药理学。I. 对中枢神经系统的作用(作者译)
Nihon Yakurigaku Zasshi. 1981 Oct;78(4):347-57.
4
Pharmacological studies of 1-(2,3-dimethyl-4-methoxyphenyl)-2-methyl-3-(1-pyrrolidinyl)-1- propanone hydrochloride (AD-2239), a centrally acting muscle relaxant.1-(2,3-二甲基-4-甲氧基苯基)-2-甲基-3-(1-吡咯烷基)-1-丙酮盐酸盐(AD-2239)的药理学研究,一种中枢性肌肉松弛剂。
Arch Int Pharmacodyn Ther. 1985 May;275(1):105-22.
5
[General pharmacology of 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. II. Effects on the peripheral system (author's transl)].新型中枢性肌肉松弛剂6-氨基-2-氟甲基-3-(邻甲苯基)-4(3H)-喹唑啉酮(阿夫唑仑)的一般药理学。II. 对外周系统的影响(作者译)
Nihon Yakurigaku Zasshi. 1981 Oct;78(4):359-80.
6
Effects of some centrally acting muscle relaxants on spinal root potentials: a comparative study.某些中枢性肌肉松弛剂对脊髓根电位的影响:一项比较研究。
Neuropharmacology. 1989 Feb;28(2):161-73. doi: 10.1016/0028-3908(89)90053-1.
7
The effects of centrally acting muscle relaxants on the intrathecal noradrenaline-induced facilitation of the flexor reflex mediated by group II afferent fibers in rats.中枢性肌肉松弛剂对大鼠鞘内注射去甲肾上腺素诱导的由Ⅱ类传入纤维介导的屈肌反射易化作用的影响。
Jpn J Pharmacol. 1993 Nov;63(3):369-76. doi: 10.1254/jjp.63.369.
8
Pharmacological properties of NK433, a new centrally acting muscle relaxant.新型中枢性肌肉松弛剂NK433的药理特性
Eur J Pharmacol. 1995 Jan 24;273(1-2):47-56. doi: 10.1016/0014-2999(94)00666-u.
9
Effects of tizanidine, a centrally acting muscle relaxant, on motor systems.中枢性肌肉松弛剂替扎尼定对运动系统的影响。
Gen Pharmacol. 1986;17(2):137-42. doi: 10.1016/0306-3623(86)90130-8.
10
[Effects of 4'ethyl-2-methyl-3-piperidinopropiophenone on experimental rigidity and spinal cord activities (author's transl)].4'-乙基-2-甲基-3-哌啶丙酰苯对实验性强直及脊髓活动的影响(作者译)
Nihon Yakurigaku Zasshi. 1981 May;77(5):511-20.

引用本文的文献

1
Nucleophilic Fluorination of a Secondary Alkyl Bromide with KF(18-Crown-6) and Bulky Diols: Microsolvation Causes Chemoselectivity Inversion in the Free Energy Profile.用KF(18-冠-6)和大体积二醇对仲烷基溴进行亲核氟化:微溶剂化导致自由能分布中的化学选择性反转。
Chempluschem. 2025 Aug;90(8):e202500257. doi: 10.1002/cplu.202500257. Epub 2025 Jul 1.
2
Synthesis, characterization, antimicrobial, cytotoxic and carbonic anhydrase inhibition activities of multifunctional pyrazolo-1,2-benzothiazine acetamides.多功能吡唑并[1,2 - b]苯并噻嗪乙酰胺的合成、表征、抗菌、细胞毒性及碳酸酐酶抑制活性
Beilstein J Org Chem. 2025 Feb 12;21:348-357. doi: 10.3762/bjoc.21.25. eCollection 2025.
3
Discovering the inhibition of YAP/TEAD Hippo signaling pathway via new pyrazolone derivatives: synthesis, molecular docking and biological investigations.
发现新型吡唑啉酮衍生物对 YAP/TEAD Hippo 信号通路的抑制作用:合成、分子对接和生物学研究。
Sci Rep. 2024 Nov 21;14(1):28859. doi: 10.1038/s41598-024-79992-x.
4
Green Synthetic and Pharmacological Developments in the Hybrid Quinazolinone Moiety: An Updated Review.杂合喹唑啉酮部分的绿色合成与药理学进展:最新综述
Curr Top Med Chem. 2025;25(5):493-532. doi: 10.2174/0115680266313354240807051401.
5
Monofluoromethylation of -Heterocyclic Compounds.-杂环化合物的单氟甲基化。
Int J Mol Sci. 2023 Dec 18;24(24):17593. doi: 10.3390/ijms242417593.
6
Coma and seizure caused by an afloqualone overdose.阿弗喹酮过量导致昏迷和癫痫发作。
Pediatr Int. 2019 Feb;61(2):212-213. doi: 10.1111/ped.13777.
7
Quinazolin-4(3)-ones and 5,6-Dihydropyrimidin-4(3)-ones from β-Aminoamides and Orthoesters.β-氨基酰胺和原甲酸酯合成的喹唑啉-4(3H)-酮和5,6-二氢嘧啶-4(3H)-酮。
Molecules. 2018 Nov 9;23(11):2925. doi: 10.3390/molecules23112925.
8
Accidental afloqualone intoxication in two dogs.两只狗意外摄入阿夫罗喹酮中毒。
J Vet Med Sci. 2018 Feb 2;80(1):152-155. doi: 10.1292/jvms.17-0305. Epub 2017 Nov 14.
9
Oral muscle relaxant may induce immediate allergic reactions.口腔肌肉松弛剂可能会引起即刻过敏反应。
Yonsei Med J. 2012 Jul 1;53(4):863-5. doi: 10.3349/ymj.2012.53.4.863.
10
N'-(3-Methoxy-benzyl-idene)-4-nitro-benzohydrazide monohydrate.N'-(3-甲氧基-亚苄基)-4-硝基苯甲酰肼一水合物
Acta Crystallogr Sect E Struct Rep Online. 2010 Mar 31;66(Pt 4):o977-8. doi: 10.1107/S1600536810010986.