氟哌利多结合电针使大鼠脑内前脑啡肽原mRNA的表达进一步增加(英文)

目的:观察氟哌利多与电针(EA)合用后前脑啡肽原(PPE)mRNA的表达.方法:氟哌利多与电针合用后取大鼠脑切片,以非放射性的原位杂交组织化学技术观察PPE mRNA.结果:电针10 h之后,PPE mRNA的表达增强了;而EA与氟哌利多合用后,PPE mRNA的表达在许多与痛觉调制有关的核团被进一步增强.如尾壳核,伏核,隔核,斜角带核,杏仁核,下丘脑,中脑导水管周围灰质,脚间核,黑质,脊髓背角.结论:氟哌利多促进电针对PPE mRNA表达的作用,与其加强针刺镇痛的机制有关.     

硬膜外镇痛药两种配方的临床观察

阿片类受体激动剂与局麻药，联合应用于术后患者自控硬膜外镇痛（PCEA）可产生协同作用，减少各自用药量，从而降低两类药物所产生的不良反应。如果再复合氟哌利多，将起到加强镇静、镇痛、止吐等作用。本研究观察芬太尼复合罗哌卡因、氟哌利多用于耻区手术后PCEA的临床镇痛效果和不良反应，并与芬太尼复合布比卡因作比较。报告如下：     

羟甲芬太尼对映异构体的镇痛活性及对阿片受体的选择性

羟甲芬太尼对映异构体的镇痛活性及对阿片受体的选择性金文桥，王智贤，陈洁，陈新建，池志强（中国科学院上海药物研究所，上海２０００３１，中国）关键词羟甲芬太尼；立体异构体；痛测定；μ阿片受体；δ阿片受体；放射配位体测定；结构活性关系目的：研究羟甲芬太尼...     

乳腺癌术后两种镇痛方法的临床比较

目的:比较乳腺癌术后两种镇痛方法的效果与不良反应。方法:将拟行择期乳癌根治术的60例病人随机分成罗哌卡因硬膜外镇痛组(PCEA组,n=30)和芬太尼静脉镇痛组(PCIA组,n=30)两组。PCEA组采用0.1%罗哌卡因(含芬太尼2μg.mL-1),PCIA组采用0.001%芬太尼加0.005%氟哌利多,比较观察术后镇痛镇静效果及不良反应。结果:术后镇痛效果两组比较无显著性差异(P>0.05),术后不良反应PCIA明显多于PCEA(P<0.05)。结论:用于乳癌术后镇痛0.1%罗哌卡因硬膜外镇痛优于芬太尼静脉镇痛。     

两种联合用药方案在成人局麻扁桃体切除手术中的效果比较

目的：观察地佐辛加氟哌利多合剂（简称地氟合剂）与芬太尼加氟哌利多合剂（简称芬氟合剂）在成人局麻扁桃体切除手术中效果观察。方法将80例成人局麻扁桃体切除手术患者随机分为两组;地氟合剂组术前30 min肌注地佐辛10 mg＋氟哌利多2 mg;芬氟合剂组术前30 min肌注芬太尼0.1 mg＋氟哌利多2 mg,分别对两组的镇痛、镇吐、术后镇痛效果及不良反应进行观察比较。结果地氟合剂组与芬氟合剂组术中镇痛、镇吐效果相仿,但是术后镇痛效果好、不良反应明显低。结论地佐辛加氟哌利多合剂比芬太尼加氟哌利多合剂在成人局麻扁桃体切除手术中应用安全、有效。     

硬膜外持续输注布比卡因、氟芬合剂用于剖宫产术后镇痛

目的 观察剖宫产术后硬膜外持续注入布比卡因、氟哌利多、芬太尼的镇痛效果。方法 选156例足月临产在硬膜外麻醉下的剖宫产患者,术毕随机分两组,镇痛组(A组,n=106),对照组(B组,n=50)。结果 A组VAS明显低于B组(P<0.01)。A组睡眠好,初乳早于B组(P<0.05)。结论 持续硬膜外输注布比卡因、氟哌利多、芬太尼镇痛效果持久、恒定,产妇术后休息好、早泌乳。     

氯胺酮联合小剂量芬太尼术后镇痛用于预防术后睡眠失调的可行性

目的探讨氯胺酮联合小剂量芬太尼术后镇痛用于预防术后睡眠失调的影响和机制。方法选择ASAⅠ~Ⅱ级,年龄(48.8±12.2)岁、全麻下行腹部手术60例病人随机分成二组:Ⅰ组:单纯芬太尼镇痛组,芬太尼0.4μg.kg-1.h-1氟哌利多5mg;Ⅱ组:氯胺酮复合芬太尼镇痛组,氯胺酮2.5μg.kg-1.h-1 芬太尼0.2μg.kg-1.h-1 氟哌利多5mg。各组镇痛药物均以医用生理盐水稀释至100mL,以每小时2mL速率持续输注。观察各组患者48h的静息镇痛评分(VAS方法),恶心呕吐、皮肤瘙痒的发生率,镇静程度,睡眠质量。结果Ⅱ组的镇痛效果显著优于Ⅰ组,恶心呕吐、皮肤瘙痒发生率少于Ⅰ组,患者睡眠质量好于Ⅰ组。结论氯胺酮联合小剂量芬太尼术后镇痛效果明显,不良反应少,能够显著改善患者术后睡眠质量,可以用于预防手术患者的术后睡眠失调。     

应用芬太尼和曲马多患者自控静脉镇痛效果比较

目的比较曲马多、芬太尼与氟哌利多、地塞米松不同配伍术后患者自控镇痛（PCA）的临床效果。方法60例（ASAⅠ～Ⅱ级）手术患者随机分为2组,Q组（n=30）镇痛药液为曲马多＋氟哌利多＋地塞米松;F组（n=30）镇痛药液为芬太尼＋氟哌利多＋地塞米松。选用上海怡新泵行PCA（YX-3）镇痛技术,采用双盲法对比观察。结果两组患者静息时、活动时的镇痛效应、镇静评分差异均无显著性,恶心呕吐、皮肤瘙痒、呼吸抑制、尿潴留,头痛、幻觉、嗜睡等不良反应差异亦无显著性。结论术后行PCA镇痛时,曲马多＋氟哌利多＋地塞米松配伍镇痛效果与芬太尼＋氟哌利多＋地塞米松配伍同样有效,但芬太尼组不良反应略少于曲马多组。     

不同硬膜外镇痛方法的镇痛效果及护理

目的 总结不同硬膜外镇痛方法的镇痛效果及护理经验.方法 随机选择下腹部、下肢手术患者60例,随机分为两组,每组30例,A组(芬太尼组):0.2%罗哌卡因+0.0002%芬太尼+0.005%氟哌利多;B组(吗啡组):0.2%罗哌卡因+0.01%吗啡+0.005%氟哌利多.术后以LCP模式(负荷剂量5 ml,持续输注量2 mL/h,单次自控给药量1 ml,锁定时间为20 min)进行镇痛.结果 A、B两组的镇痛效果均满意,B组的尿潴留、恶心呕吐、皮肤瘙痒、嗜睡等不良反应的发生率明显高于A组(P<0.05).结论 A组镇痛效果满意且不良反应少,便于术后护理.     

罗哌卡因联合吗啡或芬太尼镇痛对手术后肠蠕动的影响

目的 探讨罗哌卡因联合不同镇痛药物对手术后肠蠕动恢复情况的影响.方法 对105例普外科择期手术患者,ASA Ⅰ～Ⅱ级,根据不同的镇痛方案分成三组,吗啡组:0.125％罗哌卡因+0.005％吗啡+0.005％氟哌利多,芬太尼组:0.125％罗哌卡因+0.0005％芬太尼+0.005％氟哌利多,对照组不实施患者术后自控镇痛;镇痛治疗后4、8、12、24、36 h进行随访,观察疼痛程度、镇静状态、平均动脉压(MAP)、心率(HR)、呼吸频率(RR)、脉搏氧饱和度( SpO2),并记录肠蠕动恢复时间.结果 吗啡组与芬太尼组均取得较好的镇痛效果,VAS评分显著低于对照组(P＜0.01);芬太尼组肠蠕动恢复时间为(52.65±10.63)h,较吗啡组、对照组[分别为(73.11±14.23)、(74.54±16.61)h]均明显缩短(均P＜0.05).结论 罗哌卡因联合吗啡、芬太尼行患者术后自控镇痛均能获得良好的效果;罗哌卡因与芬太尼联用可缩短肠蠕动的恢复时间.     

阿片受体在自发性高血压大鼠和正常大鼠中的不同分布(英文)

目的:比较16周自发性高血压大鼠(SHR)和对照组Wistar-Kyoto(WKY)大鼠中枢神经系统中与血压调节有关的核团内阿片受体密度的变化.方法:用放射自显影方法,运用氚标依托啡作配基检测阿片受体的分布. 结果:在海马(P<0.01)、中央灰质、孤束核、胸髓(P<0.05)几处,SHR阿片受体密度较WKY大鼠低;而在杏仁核(P<0.01)、僵核(P<0.05)和下丘脑核群包括弓状核(P<0.01),SHR却有较高的阿片受体密度. 结论:不同分布的阿片受体与自发性高血压大鼠的血压有关.     

中国淡水鱼油的研究：Ⅲ淡水鱼油对高脂血症疗效的临床观察

高脂血症的患者血中ＥＰＡ和ＤＨＡ含量ＥＰＡ／ＡＡ和ＤＨＡ／ＥＰＡ值均低于健康对照组，以淡水鱼油乳化剂对４４例高血脂病人作了小剂量ｎ－３不饱和脂肪酸的补充（ＥＰＡ＋ＤＨＡ约１．５９ｇ／ｄ）３～４ｗ后，患者血浆中ＥＰＡ和ＤＨＡ分别增加了２４２％（Ｐ〈０．０１）和１０１８％（Ｐ〈０．０１），ＥＰＡ／ＡＡ和ＤＨＡ／ＥＰＡ值亦显著提高，血浆ＴＣ，ＴＧ，ＬＤＬ及Ｌｐ（ａ）分别降低１９．６％（Ｐ〈０．０１），２     

大鼠电惊厥后脑内生长抑素受体的变化

目的观察大鼠电惊厥后脑内生长抑素受体的变化。方法应用受体结合放射自显影术、计算机显微图象处理技术观测。结果正常大鼠大脑皮层、杏仁核、新纹状体、伏膈核、海马CA区、齿状回、嗅球、弓状核、下丘脑室周区、下丘脑腹内侧核、视前区内侧区、中央灰质、黑质等脑区内有125I-Tyr11-SS28特异性结合;电惊厥后，大鼠颞叶听皮质、梨状皮质、内嗅皮质、杏仁内侧核、海马CA区、齿状回、下丘脑腹内侧核等脑区125I-Tyr11-SS28的特异性结合比正常大鼠显著增加（P＜0.05）。结论电惊厥的发作可能与不同脑区内生长抑素受体的上调有关。     

2,3,6,7-二苯并蒽对大鼠生殖内分泌影响的研究

目的：探讨2，3，6，7－二苯并蒽对切除卵巢大鼠生殖内分泌和子宫雌激素受体的影响。方法：应用放射免疫法（RIA）和放射配体受体法。结果：2，3，6，7－二苯并蒽在皮下注射5d后，低及高剂量均可导致切除卵巢的大鼠子宫湿重明显增加（P＜0．01），低及高剂量组大鼠子宫雌激素受体数量与对照组比，差异无显著性（P＞0．05），但高剂量组大鼠子宫雌激素受体亲和力明显高于对照组（P＜0．05）。低及高剂量组血清中卵泡刺激素（FSH）含量与对照组比，差异无显著性（P＞0．05），低及,高剂量组血清中黄体生成素（LH）含量明显降低（P＜0．01，P＜0．05），高剂量组血清中催乳素（PRL）含量明显增加（P＜0．05）。结论：2，3，6，7－二苯并蒽雌激素活性的作用机制可能是干扰下丘脑－垂体－卵巢轴对生殖内分泌的调控。     

Brain regional mu-opioid receptor function in rat lines selected for differences in alcohol preference

It has been suggested that opioid peptides play a role in the reinforcing effects of alcohol. The present study was designed to examine the function of the mu-opioid receptor system in rat lines selectively bred for alcohol preference (AA [Alko, Alcohol] rat line) and alcohol avoidance (ANA [Alko, Non-Alcohol] rat line). The functional coupling of mu-opioid receptors to G proteins was determined autoradiographically using Tyr-D-Ala-Gly-N(Me)Phe-Gly-ol-enkephalin-stimulated [35S]GTPgammaS binding in brain cryostat sections. The binding was significantly increased in the striatal patches and substantia nigra reticulata of the AA rats in comparison with that of the ANA rats. Within the AA rat line, there was a significant positive correlation between 3 mg/kg morphine-induced locomotor activity and activation of G-proteins in the substantia nigra compacta and nucleus accumbens core. These results of the selective breeding experiment suggest that brain region-specific differences in mu-opioid receptor function may correlate with innate differences in alcohol preference.     

4—16周龄高血压大鼠脑与脊髓苯环利定受体的变化(英文)

目的:研究高血压大鼠(SHR)脑和胸髓中苯环利定受体密度变化与高血压发生的关系.方法:4,8,12,16周大鼠中枢中[~3H]Phe标记的苯环利定受体密度用放射自显影法检测.结果:高血压稳定期(12,16周),SHR海马和胸髓背角中苯环利定受体明显少于非高血压大鼠(WKY);而血压升高前,4周的SHR则相反;8周血压开始上升时,SHR海马苯环利定受体增加,而在背角无差别.结论:苯环利定受体可能参与了SHR的发病过程.     

Effects of chronic toluene exposure on central monoamine and peptide receptors and their interactions in the adult male rat

The effects of chronic toluene exposure (CTE) (80 ppm, 6 h/day, 5 days/week, 3 months) were studied on neuropeptide and 5-hydroxytryptamine receptors, on protein phosphorylation levels and on catecholamine levels in various brain regions in the 15-month-old male rat. Behavioral parameters and serum levels of hypophyseal hormones and corticosterone were also analyzed. CTE selectively reduced [3H]neurotensin [( 3H]NT) binding in the basal layers of the orbital cortex. Instead, CTE increased the binding of [3H]etorphine in the nucleus accumbens and of [125I]vasoactive intestinal polypeptide [( 125I]VIP) in the area postrema and hypoglossal nucleus. Acute treatment with the irreversible monoamine receptor antagonist N-ethoxycarboxyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) increased the binding of [3H]NT in the orbital cortex in toluene exposed rats as compared with the reduced [3H]NT binding obtained in air exposed rats treated with EEDQ. Furthermore, the EEDQ induced increase in [125I]VIP binding in the area postrema and the hypoglossal nucleus was replaced by a reduced binding of [125I]VIP in EEDQ-treated CTE rats. CTE produced an overall increase in calcium-induced back phosphorylation and an overall decrease in cyclic adenosine monophosphate-induced back phosphorylation in the frontoparietal cortex. Noradrenaline stores tended to be reduced within various hypothalamic subnuclei and the serum prolactin levels were increased following CTE. However, no marked effects of CTE were seen on the behavioral parameters. In conclusion, the regional selectivity of CTE in disturbing [3H]NT and [125I]VIP binding may be due to the demonstrated vulnerability of monoamine-neuropeptide interactions to toluene.     

Detailed distribution of Neurokinin 3 receptors in the rat, guinea pig and gerbil brain: a comparative autoradiographic study

The neurokinin 3 (NK3) receptor is predominantly expressed in the central nervous system (CNS). Species differences in neurokinin 3 (NK3) receptor pharmacology have led to the preferential use of guinea pigs and gerbils in the characterization of non-peptide NK3 antagonists. Little is known about the central localization of NK3 receptors in the CNS of these species. To study this, [(3)H]senktide and [(3)H]SR 142801 were used in autoradiography experiments to visualize the NK3 receptors in the guinea pig and gerbil brain and compared to with the distribution of [(3)H]senktide binding sites in the rat brain. In the three species, the NK3 receptor was similarly distributed within the cerebral cortex, the zona incerta, the medial habenula, the amygdaloid complex, the superior colliculus and the interpeduncular nucleus. Outside of these structures, our study has revealed that each species displayed a specific distribution pattern of central NK3 receptors. The rat was the only species where NK3 receptors could be visualized in the striatum, the supraoptic nucleus and the paraventricular nucleus of the hypothalamus. The guinea pig differed mainly from the two other species by the absence of detectable binding sites in the substantia nigra pars compacta and the ventral tegmental area. A specific localization of NK3 receptors in the anterodorsal and anteroventral thalamic nuclei characterized the gerbil. This last species is also unique by in the higher level of NK3 receptors in the dorsal and median raphe nuclei. All these differences suggest that the NK3 receptor mediates different functions in different species.     

PACAP对老年大鼠脑缺血再灌注神经元损伤及M受体的影响

目的　观察垂体腺苷环化酶激活肽 (PACAP)对老年大鼠全脑缺血再灌注模型神经元损伤和M受体 (mAChR)的影响。方法　利用四血管结扎法 (4 VO)建立老年大鼠全脑缺血再灌注复合伤模型 ,侧脑室注射PACAP38(5 0nmol·kg-1 ) ,用HE染色和TUNEL标记法计数皮层和海马CA1区正常神经元和凋亡神经元数目 ,采用放射性配体结合实验和饱和结合实验检测皮层和海马mAChR的3 H QNB特异结合量和结合参数。结果　脑缺血再灌注d 3后 ,皮层和海马CA1区正常神经元数显著减少、凋亡神经元数显著增加 (P<0 0 1 ) ,海马 (P <0 0 1 )和皮层 (P <0 0 5 ) 3 H QNB的特异结合量减低 ,最大结合容量 (Bmax)显著下降 (P <0 0 1 ) ,但亲和力 (Kd)不变。PACAP组皮层和海马CA1区缺血损伤神经元和凋亡神经元数目均比模型组明显降低 (P <0 0 5 ) ,3 H QNB的特异结合量和Bmax提高 (P <0 0 5 ) ,Kd 值不变。结论　脑缺血再灌注所致神经元损伤、凋亡和缺失可能是导致mAChR活性降低、密度下降的主要原因。PACAP具有抗脑缺血所致神经元损伤、保护中枢胆碱能系统的作用 ,在缺血性脑血管病防治中有潜在应用价值     

苦豆子对大鼠学习和记忆的损伤作用

目的探讨苦豆子对大鼠学习和记忆的影响。方法将48只SD大鼠随机分为正常组及苦豆子低、中、高剂量组。除正常组外,其余大鼠以80,120和160g·kg~(-1)·d~(-1)的苦豆子粉连续灌胃给药30d。给药完成后,利用Morris水迷宫、穿梭避暗测试仪和跳台记录仪测定大鼠的学习和记忆能力,化学比色法测定大鼠脑组织中的AchE活性。结果与正常组相比,120和160g·kg~(-1)·d~(-1)的苦豆子可使水迷宫实验中大鼠的潜伏期显著延长,穿越平台的次数明显减少(P<0.05或P<0.01);避暗实验中大鼠的错误次数明显增多,潜伏期显著缩短(P<0.05或P<0.01);穿梭实验给药组大鼠的主动回避反应次数显著减少,主动回避潜伏期明显延长(P<0.05或P<0.01);跳台实验给药组大鼠的下台潜伏期明显缩短,错误次数显著增加(P<0.01)。此外,苦豆子给药组大鼠脑组织中AchE活性也明显升高(P<0.05或P<0.01)。结论 120和160g·kg~(-1)·d~(-1)的苦豆子对大鼠学习和记忆具有损伤作用。