小分子免疫调节剂 L—2—(3—羟基—4—羟甲基苯基)—甘氨酸前体物 DL—2—(3—羟基—4—羟甲基苯基)—N—乙酰基甘氨酸的合成

本文通过对小分子免疲调节剂L—2—(3—羟基—4—羟甲基苯基)—甘氨酸(英文名:Forphenicinol)前体物DL—2—(3—羟基—4—羟甲基苯基)—N—乙酰基甘氨酸的合成方法研究,探索了终产物Forphenicinol 的合成路线及实验方法、并通过对各步产物之红外光谱分析,确证各步产物之主要特征吸收峰,为今后的合成工作打下良好之基础、     

DL—1—(2,6—二甲基苯氧基)—2——氨基丙烷氨基酸衍生物的研究

<正> DL—1—(2,6—二甲基苯氧基)—乙—氨基丙烷盐酸盐,商品名为慢心律(Mcxiletine)是七十年代进行临床研究的一个抗心律失常药物。目前国内外广泛用于临床,其特点是可以长期口服治疗和预防室性心律失常。根据国内外近十年的临床观察,若用量超过600—800mg/日,则有明显副作用如神经兴奋、噁心、复视、抽搐、振颤等。为了寻找更理想的抗心律失常药物,国内外已做过一些慢心律的类似物供药理筛选研究。本文是从前体药物的角度以慢心律自由碱DL—1—(2,6—甲基苯氧基)—2—氨基丙     

新型O—连接糖基化—O—GlcNAc

一种新型糖基化,单糖Ｎ－乙酰葡萄糖胺通过Ｏ－连接与蛋白质共价相连,随着研究的不断深入,这种新型糖基化受到愈来愈多的重视,本主要论述它的发现,存在部位及可能的功能。     

越南——黄连国家公园

说起越南,国人头脑里首先出现的是下龙湾、芽庄、岘港这些海边的旅游胜地,而相比之下西方人则更钟情于越南北部大山里的一个小县——沙坝（Sa Pa）。这个被誉为亚洲的＂欧洲小镇＂＂越南丽江＂的地方不仅有美丽的法式风格建筑和独特的越南少数民族的风情,更著名的名片则是秀色可餐的黄连国家公园。     

水中精灵——热带鱼

一说起热带鱼,很多人脑海中就浮现出色彩斑斓的小鱼欢快游动的情景,但是这情景很可能是朦胧的,因为我们大多数人对于热带鱼都没有很清晰的概念,也可以说,热带鱼本身就没有一个明确的定义。     

非典—SARS—冠状病毒

2002年11月,一种神秘不明的疾病出现在我国广东省继而肆虐全球,世界上有27个国家和地区相继报道出现这种疫情。由于这种疾病的症状不同于典型肺炎,故初期称之为“非典型肺炎”(简称“非典”)并沿用至今。其学名应称为“严重急性呼吸综合征”(Severe Acute Respiratory Syndrome,     

电刺激大鼠尾核头部镇痛的中枢效应——〔~3H〕-2脱氧葡萄糖放射自显影研究

本文利用[~3H]-2脱氧葡萄糖定量放射自显影方法,研究了电刺激大鼠尾核头部镇痛时中枢神经系统有关结构的葡萄糖代谢率变化。结果表明,痛刺激后,皮层躯体感觉Ⅰ,Ⅱ区、扣带回皮质、丘脑束旁核、丘脑中央中核、丘脑腹后核、尾核、外侧缰核、外侧隔核、中缝背核及中脑导水管周围灰质等结等的葡萄糖代谢率均明显升高(P<0.05)。电刺激大鼠尾核头部后,中缝大核及延髓旁巨细胞网状外侧核的葡萄糖代谢率显著升高,中脑导水管周围灰质和中缝背核的葡萄糖代谢率亦有升高趋势。电刺激大鼠尾核头部可部份降低痛刺激引起的有关结构葡萄糖代谢率升高(如皮层躯体感觉Ⅰ、Ⅱ区、扣带回皮质、丘脑束旁核、丘脑中央中核、丘脑腹后核、外侧隔核及外侧缰核等)。上述结果提示,电刺激大鼠尾核头部镇痛时抑制了与痛感觉有关的结构,同时激活了与镇痛有关的结构。中缝大核、中缝背核、中脑导水管周围灰质及延髓旁巨细胞网状外侧核等结构是实现尾核镇痛的重要环节。     

Serotonin and substance P afferents to parafascicular and central medial nuclei.

Potent analgesia is elicited by electrical stimulation of the periaqueductal gray (PAG), dorsal raphe nucleus (DRN) and intralaminar thalamus. Horseradish peroxidase conjugated wheat germ agglutinin (HRP-WGA) was stereotaxically pressure injected into the parafascicular (PF) or central medial (CM) nucleus to identify brainstem afferents to the intralaminar thalamus. WGA-immunoreactive (-ir) neurons were identified in the DRN, PAG and lateral dorsal tegmentum (LDTg) after PF and CM injections. Many retrogradely labeled cells in the DRN and ventral PAG were also serotonin-ir, and a portion of WGA-ir cells in the LDTg were substance P-ir. These results substantiate previous studies implicating the intralaminar thalamus and periaqueductal region, as well as serotonin and substance P, in antinociception.     

福尔马林致痛提高大鼠中枢μ阿片受体密度及电针的加强作用

用放射自显影方法观察到;（１）大鼠脚掌注射福尔马林后,某些与镇痛有关的脑区如尾核头部、伏隔核、杏仁核、中央灰质、脚间核、中缝大核、脊髓背角等结构中μ阿片受体密度明显增加（Ｐ＜０．０５,Ｐ＜０．０１）;（２）给予电针抑制痛反应的大鼠,在其大部分上述结构及扣带回、隔区、视前内侧区、内膝体、上丘、中缝背核及中央上核受体密度明显增加;与福尔马林注射组相比,脚间核、中央灰质尾端腹外侧区、腰膨大背角的受体密度进一步增加。从而在受体水平支持伤害性刺激可以激活体内内阿片肽能活动,而电针可以加强这一活动的设想。     

Arginine8-vasopressin affects catecholamine metabolism in specific brain nuclei

Following the i.c.v. administration of arginine⁸-vasopressin (30 ng in 1 μl saline) to rats that had been injected i.p with α-MPT 30 min prior to the administration of the peptide catecholamine metabolism was altered in a restricted number of brain nuclei. Noradrenaline disappearance was accelerated as compared to saline treated controls in the dorsal septal nucleus, the anterior hypothalamic nucleus, the medial forebrain bundle, the parafascicular nucleus, the dorsal raphe nucleus, the locus coeruleus, the nucleus tractus solitarii and the Al-region. In the supraoptic nucleus and the nucleus ruber a decreased noradrenaline disappearnce was observed after the administration of the peptide. Dopamine disappearance was accelerated in the caudate nucleus, the median eminence, the dorsal raphe nucleus and the A8-region. These results support the view that vasopressin is participating in the regulation of a variety of physiological processes by modulating neurotransmission in specific brain nuclei.     

Cortical and septal responses to dorsal raphe nucleus stimulation in the rat: long-term clomipramine actions.

In cerebral cortex and lateral septal nuclei different serotonergic receptor subtypes coexist, thus a different action on neuronal firing may be expected depending on the receptor activated. Dorsal raphe nucleus stimulation produced an increased rate of firing in cortical layer V, and in lateral septal nuclei. However, firing rate in cortical layer VI remained unchanged after stimulating the dorsal raphe nucleus. Clomipramine is a tricyclic which exerts its main actions on serotonergic receptors, and long-term treatment with this antidepressant produced a selective increased firing rate in lateral septal neurons, but not in cortical neurons. From an electrophysiological point of view, it is concluded that the excitatory actions on firing rate elicited by dorsal raphe nucleus stimulation or clomipramine treatment are mediated by 5-HT2 receptor subtype activation which is likely to be acting as a 5-HT1A modulator in such places where both receptor subtypes coexist.     

电刺激家兔大脑皮层感觉区对丘脑束旁核痛敏单位放电活动的影响

本工作目的在于探讨大脑皮层与丘脑束旁核痛觉信息活动之间的关系。用玻璃微电极记录了60只清醒麻痹状态下家兔束旁核痛敏单位的诱发放电活动。按其对外周伤害性刺激的反应型式而分成两类,分别称为痛兴奋单位和痛抑制单位。观察到在电刺激大脑皮层感觉区时,多数痛兴奋单位呈抑制性改变,并且有时施予皮层的每一单个刺激均能立即遏止一阵痛放电,少数呈易化性改变;痛抑制单位则对伤害性刺激呈现抑制反应解除,而施予皮层的每一单个刺激均可使之先有一阵短暂的放电,然后出现抑制的现象。本组实验观察过程,完整的总例数共32个单位,包括25个痛兴奋单位(18个呈抑制改变,7个呈易化改变)和7个痛抑制单位(全部呈易化改变)。实验结果表明,大脑皮层感觉区传出系统对机体的痛觉信息传递活动具有下行调制作用。由于皮层刺激对束旁核放电的影响是逐渐发展起耒的,因此考虑在上述过程中可能有体液因素的参与。     

Effect of electric stimulation of the somatosensory cortex and caudate nucleus on extinctive inhibition of a conditioned alimentary reflex to sound]

In experiments performed on 9 dogs with alimentary method, extinctive inhibition was deepened and its elaboration was aceelerated by electrical stimulation of somatosensory and motor cortical areas and ventral segment of the caudate nucleus head. The extinction of the conditioned reflex was slowed down by stimulation of the anterolateral gyrus and the central segment of the caudate nucleus head. General motor excitation of animals during stimulation of the dorsal zone of caudate nucleus head impaired the elaboration of extinctive inhibition.     

Reward circuitry activation by noxious thermal stimuli.

Using functional magnetic resonance imaging (fMRI), we observed that noxious thermal stimuli (46 degrees C) produce significant signal change in putative reward circuitry as well as in classic pain circuitry. Increases in signal were observed in the sublenticular extended amygdala of the basal forebrain (SLEA) and the ventral tegmentum/periaqueductal gray (VT/PAG), while foci of increased signal and decreased signal were observed in the ventral striatum and nucleus accumbens (NAc). Early and late phases were observed for signals in most brain regions, with early activation in reward related regions such as the SLEA, VT/PAG, and ventral striatum. In contrast, structures associated with somatosensory perception, including SI somatosensory cortex, thalamus, and insula, showed delayed activation. These data support the notion that there may be a shared neural system for evaluation of aversive and rewarding stimuli.     

大鼠扣带回前部对外侧缰核单位放电的抑制作用

电刺激扣带回前部,对75％的外侧缰核痛兴奋神经元(pain-excitative neuron of lateral habenular nucleus,LHPE)和75％的痛抑制神经元(pain-inhibitive neuron of lateral habenular nucleus,LHPI)的自发放电均产生抑制作用,并取消躯体和内脏伤害性刺激对外侧缰核(lateral habenular nucleus,LHN)单位放电的影响。扣带回内微量注射吗啡可以抑制LHPE的自发放电,并取消伤害性刺激对LHPE的增频效应。注射纳洛酮则使LHPE的自发放电增多,加强伤害性刺激对LHPE的增频作用,并可拮抗电针对LHPE伤害性刺激反应的抑制作用。     

胃肠道伤害性刺激诱导中缝背核触液神经元Fos表达

本文以ＣＢ－ＨＲＰ逆行追踪和原癌基因ｃ－ｆｏｓ表达技术相结合,观察胃肠道伤害性刺激后中缝背核触液神经元Ｆｏｓ的表达。在中缝背核发现三种标记神经元,包括ＣＢ－ＨＲＰ逆行标记神经元（３０８）、Ｆｏｓ阳性神经元（４２）和ＣＢ－ＨＲＰ／Ｆｏｓ双重标记神经元（５）。本研究提示中缝背核含有一些具有双重功能的神经元,它们既在脑－脑脊液神经体液回路中传递信息,又在胃肠道伤害性刺激的中枢传递和功能调控中起一定的作用