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组胺H_3受体激动剂和拮抗剂的研究进展 被引量:2

The Research of Histamine H_3 Receptor Agonists and Antagonists
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摘要 组胺受体激动剂和拮抗剂的研究已经有半世纪,上世纪八十年代来才取得了重大进展.目前已研究组胺H_1、H_2和H_3受体激动剂和拮抗剂.其激动剂在目前虽然没有临床应用,但它促进了拮抗剂的研究进展.H_3受体拮抗剂在20世纪80年代初才开始研究.寻找选择性高、效价强的H_3受体激动剂和拮抗剂,不仅对于H_3受体功能、分布及作用机制的研究十分重要,同时对于开发具有潜在临床应用前景的该类药物也有重要意义. Histamine receptor agonists and antagonists have been studied half a century before the last century to 80 years has made significant progress. Currently histamine H1, H2 and H2 receptor agonists and antagonists has been studied. Although there is no clinical application of its agonist, antagonist, it promoted the research. H3 receptor antagonist began to study in the early 80s of the 20th century. Looking for high selectivity and potency of strong H3 receptor agonists and antagonists, not only for the H3 receptor function, distribution and mechanism of action is important, also have potential clinical application for the development prospects of such drugs is also important.
作者 王景和 曲伟
机构地区 德州学院医学系
出处 《德州学院学报》 2010年第6期106-110,共5页 Journal of Dezhou University
关键词 组胺H_3受体 组胺H_3受体激动剂 组胺H_3受体拮抗剂 histamine H3 receptor histamine Ha receptor agonists histamine H3 receptor antagonists
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参考文献27

  • 1Schwartz J C,Arrang J M,Garbarg M,et al.A third histamine receptor subtype:charact-erization,localization andfunctions of the H3-receptor[J].Agents Actions.1990,30(1):13.
  • 2Vander Werf JF.Timmerman H.The histamine H3-receptor:a general presynaptic histaminergic regulatory system[J].Trends Pharmacol Sci,1989,10(4),154.
  • 3Hey JA,A slanian R,Bolser DC,et al.Studies on the pharmacology of the novel H3-recep-tor agonist.Sch 50971[J].A rzneim ittel-Forschung,1998,48(9):881.
  • 4Sasse A,Stark H,Reidemeister S,et al.Novel partial agonists fo r the h istam ine H3 -receptor with high in vitro and in vivo activity[J].J Med Chem,1999,42(20):4269.
  • 5Kazuta Y,H irano K,N itsume K.Cyclopropane-based conformational restriction of histamine,(Is,2s)-2-(2-aminoethyl)-(1 H-imidazo 1-4-yl) cyclopropane,a highly restricted agonist for the histamine H3 receptor,having acyclopropane structure[J].J Med Chem,2003,46(10):1980.
  • 6West RE Jr,Zweig A.Granzow RT et al.Bioexpone tial kinetics of(R)-a-[3 H] methylhista mine binding to the rat brain histamine receptor[J].Neurochem,1990,55:1612-1616.
  • 7ZARAGOZA F,STEPHENSEN H,PESCHKE B,et al.2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists[J].J Med Chem,2005,48 (1):306-311.
  • 8Jansen FP,Rademaker B,Bast A,et al.The first radiolabled histamine H3-rec-eptor antagonist[125I] iodophenpropit:saturable and reversible binding torat cortex membrane[J].Eur J Pharmacol,1992; 217:203 -205.
  • 9Sasse A,Sadek B,Ligneau X.New histamine H3 receptor ligands of proxifan series imoproxifan and other selective antagonists with high oral in v ivo potency[J].J Med Chem,2000,43(17):3335.
  • 10M iko T,Ligneau X,Pertz HH,et al.Novel nonim idazole histamine H3-receptor antagonists:1-(42(phenol-xymethyl) benzyl) p iperidines and related compounds[J].J Med Chem,2003,46(8):1523.

二级参考文献17

  • 1胡春梅,董榕,刘保森,张晓红,季吉.大鼠孤束核内H_3受体对哮喘发作时脑组织中Fos蛋白表达的影响[J].东南大学学报(医学版),2005,24(6):371-374. 被引量:4
  • 2董榕,张敏,刘保森.中枢组胺H_3受体对哮喘豚鼠呼吸运动的影响[J].中国应用生理学杂志,2006,22(1):117-121. 被引量:3
  • 3肖剑,董榕,刘佳,刘伲娜.下丘脑室旁核经迷走神经复合体对哮喘大鼠的神经调控研究[J].神经解剖学杂志,2007,23(3):299-304. 被引量:4
  • 4ELWOOD W, LOTVALL JO, BARNES PJ,et al. Characterization of allergen-induced bronchial hyper-responsiveness and airway inflammation in actively sensitized brown-Norway rats[.I]. J Allergy Clin Immunol , 1991,88 (6) :951 - 960.
  • 5BROWN RE, STEVENS DR, HAAS HL. The physiology of brain histamine [ J ]. Prog Neurophysiol, 2001,63 ( 6 ) : 637 - 672.
  • 6XIE QM,CHEN JQ,SHEN WH,et al. Correlative changes of interferan-γ and interleukin-4 between cortical layer and pulmonary airway of the sensitized rats [ J ]. Acta Pharmacol Sin,2002,23 (3) :248 - 252.
  • 7LIU J,DONG R,XIAO J,et al. Mechanism of hypothalamic paraventricular nucleus in regulating asthmatic attack [ J]. Neural Regener Res ,2007,1 ( 7 ) :593 - 596.
  • 8KC P, KARIBI-IKIRIKO A, RUST CF,et al. Phenotypic traits of the hypothalamic PVN cells innervating airway-related vagal preganglionic neurons [ J ]. J Respir Physiol Neurobiol, 2006,154 (3) :319 -330.
  • 9ICHINOSE M, STRETTON CD, SCHWARTZ JC,et al. Histamine H3-receptors inhibit cholinergic neurotransmission in guinea-pig airways [ J ]. Br J Pharmacol, 1989,97 ( 1 ) : 13 - 15.
  • 10ARRANG JM, GARBARG M, LANCELOT JC. Highly potent and selective ligands for histamine H3-receptors [ J ]. Nature, 1987,327(6117) :117 - 123.

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