腹外侧视前区微量注射组胺对大鼠睡眠-觉醒周期的影响

目的 研究组胺作用于腹外侧视前区对大鼠睡眠-觉醒周期的影响。方法 通过脑立体定位、腹外侧视前区微量注射组胺,脑电图仪记录及分析睡眠、觉醒时相。结果 微量注射50μmol/L组胺无明显影响,而100μmol/L组胺显著减少大鼠睡眠,增加觉醒。结论 组胺在腹外侧视前区对大鼠睡眠-觉醒周期发挥重要的调节作用,具有明显的促觉醒作用。     

美洲大蠊提取物CⅡ-3抗炎作用及机制研究

目的:研究美洲大蠊提取物CⅡ-3抗急性炎症的作用,并探讨其可能的作用机制。方法:采用二甲苯致大鼠耳肿胀和角叉菜胶致小鼠足跖肿胀法急性炎症模型考察美洲大蠊提取物CⅡ-3抗急性炎症的作用。结果:50、100mg/kg的CⅡ-3对大鼠耳肿胀有明显抑制作用;100、200mg/kg的CⅡ-3对小鼠足跖肿胀有非常明显的抑制作用,且能显著降低小鼠炎足浸泡液中炎症介质PGE2、组胺和MDA的含量,并能提高炎症组织中SOD的活性。结论:美洲大蠊提取物CⅡ-3对急性炎症具有较好的抑制作用,其抗炎作用可能与减少炎症介质的含量和清除自由基有关。     

组织胺在兔十二指肠纵肌收缩中的作用及递质间的相互关系

以家兔离体十二指肠纵肌方向的张力为指标，观察了乙酰胆碱（Ａｃｈ）、去甲肾上腺素（ＮＥ）、组织胺（Ｈｉｓｔａｍｉｎｅ）对十二指肠的作用，探讨了组织胺对Ａｃｈ，ＮＥ的调制作用．实验表明，在正常情况下兔离体十二指肠收缩活动比较规律，并出现梭形波，纵肌的张力变化呈现周期性．Ａｃｈ对十二指肠的作用依其剂量的不同而不同．ＮＥ通过β抑制性受体对十二指肠产生抑制作用，而β兴奋性受体和α兴奋性受体介导兴奋．组织胺对十二指肠的作用与肠的机能状态有关，Ｈ１型受体介导兴奋．阈下剂量的组织胺可激活ＮＥ的α受体使ＮＥ表现为兴奋作用，对Ａｃｈ具有调制作用     

Nitric oxide mediates histamine induced down-regulation of H<Subscript>2</Subscript> receptor mRNA and internalization of the receptor protein (R1)

During agonist-dependent long-term stimulation of cells, histamine receptor subtypes are frequently down-regulated. However, the mechanisms underlying the modulation of receptor expression during long-term histamine stimulation have yet to be resolved. Based on our recently reported results showing an H₁-mediated down-regulation of histamine H₂ receptor mRNA in endothelial cells, our aim was to characterize the mechanism controlling rapid and long-term histamine-mediated modulation of H₂ receptor expression in more detail. We were able to show that the histamine-induced down-regulation of H₂ receptor mRNA and cell surface expression lasting for 24 h was accompanied by augmentation of the receptor protein level in the cytoplasmatic fraction of endothelial cells for this time period. Furthermore, changes in receptor protein levels in whole-cell lysate were negligible, indicating that the rapid and prolonged modulation of cell surface H₂ receptor levels by histamine was regulated solely via internalization. The role of nitric oxide (NO) as a key mediator in histamine-stimulated cell responses was underlined by subsequent studies showing the attenuation of histamine-induced H₂ receptor mRNA down-regulation and protein trafficking following NO synthase isozyme inhibition.Received 11 March 2003; received after revision 11 June 2003; accepted 17 June 2003     

受体缺乏改变小鼠脑内组胺含量及昼夜节律

在乙谜麻醉下,分别于明时(8:00 a.m.)及暗时(8:00 p.m.)断头处死野生型及组胺H1R基因敲除型小鼠,迅速取出脑组织并分离出皮层、纹状体、海马、下丘脑、丘脑、中脑及脑干等脑区.这些脑组织被制成匀浆并用HPLC荧光检测法测量其组胺含量.结果显示暗时处死时,H1R基因敲除型小鼠海马、丘脑、中脑及脑干中的组胺含量明显低于野生型小鼠.明时处死时,野生型小鼠各脑区组胺含量均较暗时处死显著降低,但这一变化在H1R基因敲除型小鼠中并未观察到.这些表明作为组胺的功能靶,H1R不仅介导组胺的功能,而且调节大脑中组胺含量与释放的昼夜节律.     

长效H2受体拮抗剂-拉呋替丁的合成

以2-溴-4-(哌啶基甲基)吡啶为原料,与2-丁烯-1,4-二醇醚化,经氯化、G abrie l反应、肼解,然后再与2-呋喃甲硫基-S-氧代乙酸对硝基苯酚酯进行胺解反应,制得第二代长效H2受体拮抗剂拉呋替丁,总收率为29.89%[以2-溴-4-(哌啶基甲基)吡啶计]。     

Excitatory effect of histamine on neuronal activity of rat cerebellar fastigial nucleus Jn vitro

The cerebellar fastigial nucleus （FN） holds an important role in motor control and body balance. Previous studies have revealed that the nucleus is innervated by direct hypothalamocerebellar hletaminergic fibers. However, the functional role of histaminergic projection in cerebellar FN has never been established. In this study, we investigated the effect of histamine on neuronal firing of cerebellar FN by using slice preparations. Sixty-five FN cells were recorded from 47 cerebellar slices, and a vast majority of the cells responded to histamine stimulation with an excitatory response （58/65, 89.2%）. Perfusing slices with low-Ca^2＋/high-Mg^2＋ medium did not block the histamine-induced excitation （n=10）, supporting a direct postsynaptic action of histamine on the cells. Furthermore, the excitatory effect of histamine on FN neurons was not blocked by selective histamine H1 receptor antagonist triprolidine （n=15） or chlorpheniramine （n=10）, but was effectively suppressed by ranitidine （n=15）, a highly selective histamine H2 receptor antagonist. On the other hand, highly selective histamine H2 receptor agonist dimaprit （n=20） instead of histamine HI receptor agonist 2-pyridylethylamine （n=16） mimicked the excitatory effect of histamine on FN neurons. The dimaprit-induced FN neuronal excitation was effectively antagonized by selective histamine H2 receptor antagonist ranitidine （n=13） but not influenced by selective histamine H1 receptor antagonist triprolidine （n=15）. These results demonstrate that histamine excites cerebellar FN cells via the histamine H2 receptor mechanism and suggest that the hypothalamocerebellar histaminergic fibers may modulate cerebellar FN-mediated sensorimotor integration through their excitatory innervations on FN neurons.     

Effects of gastric secretagogues on tissue glycerol in the isolated amphibian gastric mucosa

Summary Histamine and theophylline, two gastric secretagogues, significantly increased tissue glycerol content by 121 and 66%, respectively, in the isolated toad gastric mucosa. This is new evidence in favor of the hypothesis that gastric segretagogues may act via lipid mobilization.This investigation was supported by Consejo de Desarrollo Científico y humanístico de la Universidad del Zulia, Maracaibo, Venezuela.     

Excitatory effect of histamine on neuronal activity of rat cerebellar fastigial nucleus in vitro

The cerebellar fastigial nucleus (FN) holds an important role in motor control and body balance. Previous studies have revealed that the nucleus is innervated by direct hypothalamocerebellar histaminergic fibers. However, the functional role of histaminergic projection in cerebellar FN has never been established. In this study, we investigated the effect of histamine on neuronal firing of cerebellar FN by using slice preparations. Sixty-five FN cells were recorded from 47 cerebellar slices, and a vast majority of the cells responded to histamine stimulation with an excitatory response (58/65, 89.2%). Perfusing slices with low-Ca2 /high-Mg2 medium did not block the histamine-induced excitation (n=10), supporting a direct postsynaptic action of histamine on the cells. Furthermore, the excitatory effect of histamine on FN neurons was not blocked by selective histamine H1 receptor antagonist triprolidine (n=15) or chlorpheniramine (n=10), but was effectively suppressed by ranitidine (n=15), a highly selective histamine H2 receptor antagonist. On the other hand, highly selective histamine H2 receptor agonist dimaprit (n=20) instead of histamine H1 receptor agonist 2-pyridylethylamine (n=16) mimicked the ex- citatory effect of histamine on FN neurons. The dimaprit-induced FN neuronal excitation was effectively antagonized by selective histamine H2 receptor antagonist ranitidine (n=13) but not influenced by se- lective histamine H1 receptor antagonist triprolidine (n=15). These results demonstrate that histamine excites cerebellar FN cells via the histamine H2 receptor mechanism and suggest that the hypotha- lamocerebellar histaminergic fibers may modulate cerebellar FN-mediated sensorimotor integration through their excitatory innervations on FN neurons.     

不同解冻方式对金枪鱼新鲜度的影响研究

金枪鱼营养物质丰富,但极易腐败,其新鲜度对金枪鱼的品质安全、运输储藏和加工都有重要意义,而解冻方式对其新鲜度有很大的影响。以不同解冻方式下金枪鱼的pH、K值、组胺含量的变化和电子鼻测定的鲜度值为指标,找出比较合适的解冻方式。在整个解冻过程中,pH呈现出减小的趋势,而组胺含量和K值则会随着解冻时间的延长而有所增加。结果显示,外部解冻中的温度梯度解冻和内部解冻中的超声波解冻能够较好地保持金枪鱼的新鲜度。