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201.
采用Barthel指数对120例脑卒中住院患者在发病后5 ̄6周进行日常生活活动(ADL)能力的证实。因脑卒中遗留的功能不全,ADL的受损率达66.7%,肢体的Brunnstrom功能分级与ADL积分高度相关,相关性下肢高于上肢;多元逐步回归分析显示,躯体(偏瘫)和心理(认知障碍和抑郁因素)影响ADL的能力。认为ADL能力的提高,不仅依赖于肢体功能障碍的改善,提高认知功能,改善情感状况,对于脑卒中患 相似文献
202.
Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site 总被引:2,自引:0,他引:2
M S Allen Y C Tan M L Trudell K Narayanan L R Schindler M J Martin C Schultz T J Hagen K F Koehler P W Codding 《Journal of medicinal chemistry》1990,33(9):2343-2357
The structural requirements for ligand binding to the benzodiazepine receptor (BzR) inverse agonist site were probed through the synthesis and in vitro evaluation of 3-substituted beta-carbolines 6, 7, 11, 12, gamma-carboline 13, and diindoles 18-21, 23-25, 27, 28, and 34. On the basis of the apparent binding affinities of these and other analogues, a hydrogen bond acceptor site (A2) on the receptor is proposed to interact with the N(9) hydrogen atom of the beta-carbolines or the N(7) hydrogen nuclei of the diindoles. Likewise, a proposed hydrogen bond donating site (H1) interacts with the N(2) nitrogen atom of the beta-carbolines or the N(5) nitrogen atom of the diindoles. It appears that interaction with both sites is a prerequisite for high affinity since analogues which have either one or both of these positions blocked exhibit substantial reduction in affinity. Moreover, H1 appears to be capable of engaging in a three-centered hydrogen bond with appropriately functionalized ligands, which explains the increase in potency observed in the following series of 3-substituted beta-carbolines: the n-butyl (12, IC50 = 245 nM), n-propoxy (9, IC50 = 11 nM), and propyl ketone (11, IC50 = 2.8 nM) congeners. In addition to H1 and A2, there appears to be a relatively narrow hydrophobic pocket in the binding cleft that can accommodate substituents at the 3-position of the beta-carbolines which have chain lengths less than or equal to C5. There is a 1 order of magnitude decrease in affinity between n-propoxy analogue 9 (IC50 = 11 nM, chain length = 4) and n-butoxy derivative 7 (IC50 = 98 nM, chain length = 5). Furthermore, alpha- and gamma-branching [e.g. ethoxycarbonyl (2), IC50 = 5 nM and tert-butoxycarbonyl (31) IC50 = 10 nM] but not beta- and delta-branching [e.g. isopropoxy (6), IC50 = 500 nM and (neopentyloxy) carbonyl (48), IC50 = 750 nM] at position 3 are tolerated. Occupation of this hydrophobic pocket is clearly important for high affinity as evidenced by the relatively low affinity of 30, a beta-carboline which possesses a hydrogen atom at the 3-position. This same hydrophobic pocket is partially filled by the D and E rings of the diindoles, which accounts for the high affinity of several members of this series. An excluded volume analysis using selected 3-substituted beta-carbolines and ring-E substituted pyridodiindoles is consistent with the presence of this hydrophobic pocket (see Figure 1).(ABSTRACT TRUNCATED AT 400 WORDS) 相似文献
203.
采用加热、硫酸铵分段盐析和DEAE-SephadexA-50柱层析,从大鼠睾丸中分离纯化了LDH-C4。比活性提高784倍,活性回收率为12.3%,纯化的LDH-C4经聚丙烯酰胺凝胶电泳(PAGE)鉴定均为一条酶带,位于LDH3和LDH4之间。 相似文献
204.
目的:探讨准分子激光原位角膜磨镶术(LASIK)对近视眼患者双眼影像不等(BA)的影响。方法:采用中国人民解放军海军总医院眼科刘蔼年设计的《双眼影像不等检查图》,对64例行MSIK术的近视眼患者按双眼屈光度差的程度分为四组,术前、术后6个月分别行BA检查,并观察双眼视力与BA恢复的关系。结果:双眼屈光度差≤2.50D的患者术前、术后双眼影像不等的一、二、三类检查图的差异无显著性。屈光度差大于2.50D的患者,术前、术后双眼一、三类检查图的差异有显著性,术后双眼裸眼视力与第三类检查图的恢复密切相关。结论:LASIK术可以使双眼屈光度差值大的患者的BA减小到可以承受的范围,并有助于三级功能的恢复,同时术后视力越好,三级功能恢复越佳。眼科学报2003;19:107-109 相似文献
205.
如何提高医学素材数码摄影的画面效果 总被引:1,自引:1,他引:0
介绍了数码影像技术在图像画面拍摄中的应用,使医学素材具有真实性和艺术性相结合的画面效果,从而提高了教学质量. 相似文献
206.
无症状心肌缺血心率变异分析的临床意义 总被引:3,自引:0,他引:3
对148例无症状心肌缺血(SMI)患者及30例对照组进行24h动态心电图心肌缺血程度及心率变异时域的分析,并随访1.5年,结果示SMI Ⅰ、Ⅲ,Ⅱ型心肌缺血程度(ST段下移幅度、SMI发作次数,总缺血时间)及室性早搏发生率依次增加,而差值心率,心率变异指数(HRVI)和RR间期标准差(SDNN)依次递减。心肌缺血程度与最低心率及室性早搏发生率呈正相关,而与HRVI和SDNN呈负相关。说明随着心肌缺 相似文献
207.
208.
目的:观察重组人α-肿瘤坏死因子(rhuTNF-α)对烧伤后增生性瘢痕组织胶原含量及组织形态学的影响。方法:12只BALB/c裸鼠,于背部体表移植人体烧伤后增生性瘢痕组织(2cm×2cm)成活后,随机分为试验组及对照组。试验组在增生性瘢痕组织内注射生理盐水溶解的rhuTNF-α0.1ml(500ng/ml),每周3次,对照组同法注射生理盐水,3周后测定瘢痕组织中胶原、羟脯氨酸及酸性粘多糖含量,同时观察组织形态学变化。结果:局部注射rhuTNF-α后,增生性瘢痕组织中胶原、羟脯氨酸及酸性粘多糖含量显著降低。增生性瘢痕组织变平、缩小,胶原结节明显减少或消失。成纤维细胞粗面内质网显著减少,无扩张。结论:rhuTNF-α能显著减少增生性瘢痕组织中胶原沉积,在增生性瘢痕治疗中可能有潜在应用价值。 相似文献
209.
介绍了一种新型的防腐杀菌剂--二羟甲基二甲海因的合成方法,采用5,-5二甲海因与甲醛在常压、碱性、冰浴下,反应2小时,产率88.6%。 相似文献
210.
Summary Using acetylcholinesterase histochemical and choline acetyltransferase immunocytochemical localization methods, this study has provided conclusive evidence for the existence of cholinergic neurons in the external cuneate nucleus of gerbils. By light microscopy, both acetylcholinesterase and choline acetyltransferase labelling was confined to the rostral portion of the external cuneate nucleus. Ultrastructurally, acetylcholinesterase reaction products were found in the nuclear envelope, cisternae of rough endoplasmic reticulum and Golgi saccules of some somata and large dendrites as well as in the membranes of small dendrites, myelinated axons and axon terminals. These neuronal elements were also stained for choline acetyltransferase; immunoreactivity was associated with nuclear pores, nuclear envelope, perikaryal membrane and all the membranous structures within the cytoplasm. Of the total choline acetyltransferase-labelled neuronal profiles analysed, 79% were myelinated axons, 15% dendrites, 4% somata and 2% axon terminals. The immunostained axon terminals consisted of two types containing either round (Rd type; 62.5%) or pleomorphic (Pd type; 37.5%) vesicles. Both were associated directly with choline acetyltransferase-positive dendrites. In contrast to the paucity of choline acetyltransferase-labelled axon terminals, numerous choline acetyltransferase-positive myelinated axons were present. It may thus be hypothesized that most, if not all, of the external cuneate nucleus cholinergic neurons are projection cells; such cells may give rise to axonal collaterals which synapse onto their own dendrites for possible feedback control. Choline acetyltransferase-positive dendrites were contacted by numerous unlabelled presynaptic boutons, 60% of which contained round or spherical synaptic vesicles (Rd boutons) and 40% flattened vesicles (Fd boutons), suggesting that these neurons are under strong inhibitory control. The preferential concentration of cholinergic components in the rostral external cuneate nucleus may be significant in the light of the highly organized somatotopy in the external cuneate nucleus and its extensive efferent projections to medullary autonomic-related nuclei. Our results suggest that the cholinergic neurons may be involved in somatoautonomic integration. 相似文献