• 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

1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.

作者信息

Williams P D, Clineschmidt B V, Erb J M, Freidinger R M, Guidotti M T, Lis E V, Pawluczyk J M, Pettibone D J, Reiss D R, Veber D F

机构信息

Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA.

出版信息

J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002.

DOI:10.1021/jm00023a002
PMID:7473590
Abstract
摘要

相似文献

1
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.1-(1-[4-[(N-乙酰基-4-哌啶基)氧基]-2-甲氧基苯甲酰基]哌啶-4-基)-4H-3,1-苯并恶嗪-2(1H)-酮(L-371,257):一种新型的、口服生物可利用的非肽类催产素拮抗剂。
J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002.
2
Progress in the development of oxytocin antagonists for use in preterm labor.
Adv Exp Med Biol. 1995;395:601-12.
3
Orally active, nonpeptide oxytocin antagonists.口服活性非肽类催产素拮抗剂。
J Med Chem. 1992 Oct 16;35(21):3919-27. doi: 10.1021/jm00099a020.
4
Progress in the development of oxytocin antagonists for use in preterm labor.
Adv Exp Med Biol. 1998;449:473-9. doi: 10.1007/978-1-4615-4871-3_61.
5
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.非肽类催产素拮抗剂:L-371,257的强效、口服生物可利用类似物,含有1-R-(吡啶基)乙醚末端。
Bioorg Med Chem Lett. 1998 Nov 3;8(21):3081-6. doi: 10.1016/S0960-894X(98)00568-X.
6
Effects of the non-peptide inhibitor OPC-21268 on oxytocin and vasopressin stimulation of rat and human myometrium.非肽类抑制剂OPC-21268对大鼠和人子宫肌层中催产素和加压素刺激的影响。
Eur J Pharmacol. 1995 Jul 25;281(1):63-8. doi: 10.1016/0014-2999(95)00225-a.
7
Spontaneous contractions of myometrium from humans, non-human primate and rodents are sensitive to selective oxytocin receptor antagonism in vitro.来自人类、非人灵长类动物和啮齿动物的子宫肌层自发收缩在体外对选择性催产素受体拮抗剂敏感。
BJOG. 2001 Sep;108(9):960-6. doi: 10.1111/j.1471-0528.2001.00226.x.
8
1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.1-((7,7-二甲基-2(S)-(2(S)-氨基-4-(甲基磺酰基)丁酰胺基)双环[2.2.1]庚烷-1(S)-基)甲基)磺酰基)-4-(2-甲基苯基)哌嗪(L-368,899):一种口服生物可利用的非肽类催产素拮抗剂,对治疗早产具有潜在效用。
J Med Chem. 1994 Mar 4;37(5):565-71. doi: 10.1021/jm00031a004.
9
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.口服活性催产素拮抗剂的研发:对1-(1-[4-[1-(2-甲基-1-氧化吡啶-3-基甲基)哌啶-4-基氧基]-2-甲氧基苯甲酰基]哌啶-4-基)-1,4-二氢苯并[d][1,3]恶嗪-2-酮(L-372,662)及相关吡啶的研究
J Med Chem. 1998 Jun 4;41(12):2146-63. doi: 10.1021/jm9800797.
10
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6. doi: 10.1016/s0960-894x(99)00181-x.

引用本文的文献

1
Neurohypophysial and paracrine vasopressinergic signaling regulates aquaporin trafficking to hydrate marine teleost oocytes.神经垂体和旁分泌血管加压素能信号调节水通道蛋白向海洋硬骨鱼卵母细胞的转运,以保持其水分。
Front Endocrinol (Lausanne). 2023 Aug 11;14:1222724. doi: 10.3389/fendo.2023.1222724. eCollection 2023.
2
Arginine vasopressin potentiates inspiratory bursting in hypoglossal motoneurons of neonatal mice.精氨酸加压素增强新生小鼠舌下运动神经元的吸气爆发。
Respir Physiol Neurobiol. 2023 Aug;314:104087. doi: 10.1016/j.resp.2023.104087. Epub 2023 Jun 2.
3
The Current Status of Drug Discovery for the Oxytocin Receptor.
阿片促黑皮质素原受体药物研发的现状
Methods Mol Biol. 2022;2384:153-174. doi: 10.1007/978-1-0716-1759-5_10.
4
Nanoparticle encapsulated oxytocin increases resistance to induced seizures and restores social behavior in Scn1a-derived epilepsy.纳米颗粒包裹的催产素可提高癫痫诱导的耐药性,并恢复 Scn1a 源性癫痫的社会行为。
Neurobiol Dis. 2021 Jan;147:105147. doi: 10.1016/j.nbd.2020.105147. Epub 2020 Oct 25.
5
Relevance of number and physiological status of conspecifics in preventing stress-induced decreases in newly proliferated cells and neuroblasts.同种个体数量和生理状态对预防应激引起的新增殖细胞和神经母细胞减少的相关性。
Psychopharmacology (Berl). 2019 Nov;236(11):3329-3339. doi: 10.1007/s00213-019-05290-4. Epub 2019 Jun 14.
6
Oxytocin blocks enhanced motivation for alcohol in alcohol dependence and blocks alcohol effects on GABAergic transmission in the central amygdala.催产素可阻断酒精依赖者对酒精的增强动机,并阻断酒精对中枢杏仁核 GABA 能传递的影响。
PLoS Biol. 2019 Apr 16;17(4):e2006421. doi: 10.1371/journal.pbio.2006421. eCollection 2019 Apr.
7
Skeletal Muscle-Specific Activation of G Signaling Maintains Glucose Homeostasis.骨骼肌特异性激活 G 信号可维持血糖稳态。
Diabetes. 2019 Jun;68(6):1341-1352. doi: 10.2337/db18-0796. Epub 2019 Apr 1.
8
Differential contributions of vasopressin V1A and oxytocin receptors in the amygdala to pain-related behaviors in rats.大鼠杏仁核中血管加压素V1A受体和催产素受体对疼痛相关行为的不同作用
Mol Pain. 2016 Nov 11;12. doi: 10.1177/1744806916676491. Print 2016.
9
In silico molecular comparisons of C. elegans and mammalian pharmacology identify distinct targets that regulate feeding.线虫和哺乳动物药理学的计算机分子比较鉴定出调节摄食的不同靶点。
PLoS Biol. 2013 Nov;11(11):e1001712. doi: 10.1371/journal.pbio.1001712. Epub 2013 Nov 19.
10
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.合成和评价 C-11、F-18 和 I-125 小分子放射性配体用于检测催产素受体。
Bioorg Med Chem. 2012 Apr 15;20(8):2721-38. doi: 10.1016/j.bmc.2012.02.019. Epub 2012 Feb 25.