高浓度吗啡对体外培养的小鼠淋巴细胞增殖的抑制效应

高浓度吗啡对体外培养的小鼠淋巴细胞增殖的抑制效应北京医科大学药理学教研室陆正武，林志彬利用不同刺激原诱导的淋巴细胞增殖反应，研究吗啡的体外作用机制。结果表明：（１）高浓度吗啡（≥０．１ｍｍｏｌ·Ｌ－１）以剂量依赖方式，抑制ＣｏｎＡ／ＬＰＳ所致淋巴细胞...     

High postovariectomy LH levels are not due to decreased opioid inhibition of GnRH

It has been proposed that endogenous opioid peptide (EOP) inhibition of hypothalamic GnRH secretion mediates and is dependent upon gonadal steroid feedback of LH secretion, although considerable conflicting data have been reported. Accordingly, a well-characterized replacement regimen was used to approximate physiological stimulation by estradiol (E2) and progesterone (P4) in adult rats 10 days after ovariectomy (OVX), followed by in vitro incubation of the isolated median eminence to evaluate the role of E2 and P4 in modifying GnRH release in response to the opiate receptor antagonist, naloxone (NAL). Basal (control) GnRH release from median eminences of OVX, OVX + E2, and OVX + E2 + P4 rats was similar, and NAL treatment elicited a comparable increase in GnRH release under all three gonadal steroid conditions. Thus, EOP suppression of median eminence GnRH secretion does not appear to mediate or be dependent upon negative feedback regulation of LH secretion by physiological concentrations of gonadal steroids.     

痛力克对癌症疼痛镇痛效果的临床观察

应用印度ＬＵＰＩＮ公司提供的痛力克（酮酷酸氨丁三醇 ）对中重度癌症疼痛３０例进行镇痛效果的临床观察，有效率９３％，平均显效时间９ｍｉｎ，均数缓解时间５．１ｈ，并用哌替啶做了同期交叉自身镇痛对比研究，结果表明：两药的镇痛效果相似（Ｐ＞０．０５），但痛力克的不良反应发生率明显低于哌替啶。     

Evaluation of the effects of opioid agonists and antagonists under a delayed matching-to-sample procedure in pigeons

The effects of several opioid agonists and antagonists were examined in pigeons performing under a delayed matching-to-sample procedure. The mu agonists morphine and l-methadone, the kappa agonists U 50,488 and ethylketocyclazocine, and the opioid antagonist naloxone had no effect on the accuracy of responding. These drugs were, however, behaviorally active as evidenced by the dose-dependent decreases in rates of responding associated with their administration. In contrast, the sigma agonists (+) N-allylnormetazocine and phencyclidine decreased the accuracy of responding in a dose-dependent fashion. The relative magnitude of these drug-induced decreases in accuracy were similar across the no delay (0-s), short (2-s), and long (8-s) delay intervals. For these drugs, accuracy-decreasing effects were obtained only at doses that reduced rates of responding. The results of the present investigation parallel those reported in pigeons responding under drug discrimination tasks, in which the discriminative stimulus properties produced by the mu and kappa agonists are similar to each other but distinguishable from those produced by the sigma agonists.Recipient of Research Scientist Development Award DA 00033 from the National Institute on Drug Abuse     

金尔伦治疗急性颅脑损伤的剂量效应研究

目的探讨金尔伦(盐酸纳洛酮)在治疗大鼠液压脑损伤后神经功能恢复和病理损害程度的剂量效应.方法将104只SD大鼠随机分为4组,伤后早期分别腹腔注射0.03 mg/Kg(小剂量组)、0.3 mg/Kg(中剂量组)、3 mg/Kg(大剂量组)金尔伦和等量生理盐水(对照组),连续7 d.结果中、大剂量组动物伤后脑神经功能恢复、脑水肿减轻程度及光、电镜检查显著优于对照组及小剂量组.结论伤后早期使用中剂量和大剂量金尔伦(盐酸纳洛酮)对大鼠液压颅脑损伤有明显的治疗效果.     

外周伤害性刺激及吗啡对大鼠丘脑束旁核痛抑制-兴奋神经元电活动的影响

应用细胞外微电极技术,观察和记录了Pf痛反应神经元对伤害性夹尾、伤害性电刺激坐骨神经和检验性刺激及脑内微量注射吗啡前后电活动变化的情况。在67只Wistar大鼠右侧Pf内记录了309个痛反应神经元,其中PI-EN64个,占神经元总数的20.71%。PI-EN对伤害性夹尾和电刺激坐骨神经均发生特异性的抑制-兴奋反应,对非伤害性刺激则不发生反应。伤害性刺激诱发放电之前有     

盐酸纳洛酮治疗急性脑卒中致意识障碍40例疗效观察

目的　探讨盐酸纳洛酮治疗急性脑卒中致意识障碍的疗效。方法　应用盐酸纳洛酮治疗急性脑卒中有意识障碍患者40例 ,与同期该类患者 40例常规治疗为对照。结果　治疗组疗效较对照组好 ,治疗组转醒时间明显小于对照组 (P <0 .0 1)。结论　盐酸纳洛酮治疗急性脑卒中致意识障碍 ,可明显缩短患者的转醒时间 ,显著提高疗效。     

Analgesia produced by intrathecal administration of the kappa opioid agonist, U-50,488H, on formalin-evoked cutaneous pain in the rat

The antinociceptive activity of the selective k opioid agonist U-50,488H, given intrathecally (i.t.) against chemically induced cutaneous pain in rats, was assessed from cumulative dose-response experiments and the formalin test. Three successive i.t. doses of 5, 10 and 35 nmol of U-50,488H produced a gradual reduction of pain scores which was statistically significant at all observation periods. This effect was antagonized significantly by 3 mg/kg i.p. of the opiate antagonists, naloxone and WIN 44,441-3. The analgesia profile showed a clear dose-response relationship. A dose producing 50% ‘maximum posible analgesia’ of 6.20 nmol (95% confidence interval: 3.05–12.59 nmol) was calculated. The results indicated that cutaneous pain of a chemical/inflammatory nature is highly sensitive to activation of k receptors of the spinal cord dorsal horn.     

可乐定透皮贴剂联合芬太尼静脉自控镇痛用于原发性高血压病人术后镇痛

目的 观察可乐定透皮贴剂联合芬太尼静脉自控镇痛(PCIA)用于原发性高血压(EH)病人术后镇痛的效果.方法 择期全麻下行腹腔镜胆囊切除术病人60例,均合并EH,依据术后镇痛方法的不同,随机均分为三组,肌注哌替啶组(P组)、芬太尼PCIA组(F组)和可乐定透皮贴剂联合芬太尼PCIA组(CF组).使用芬太尼1.0mg稀释至100ml,PCIA均采用负荷量-持续背景量-PCA量模式,背景剂量芬太尼20 μg/h,PCA追加剂量5 μg,锁定时间15 min.记录病人术后镇痛4、8、24、48 h VAS及Ramsay镇静评分,并记录不良反应和处理措施.监测入院时、术后24、48 h血浆内皮素(ET)及降钙素基因相关肽(CGRP)浓度、血糖(Glu),同时记录MAP、HR.结果 镇痛期间F、CF组VAS低于P组(P<0.01),CF组低于F组(P<0.05).Ramsay镇静评分F组高于P组(P<0.01),CF组高于F组(P<0.05),三组均无过度镇静.CF组MAP、HR术后较入院时明显降低(P<0.01),血浆ET、血浆CGRP浓度与入院时比较差异无统计学意义.术后ET、Glu浓度和MAP、HR F组低于P组,CGRP浓度高于P组(P<0.05).术后ET、Glu浓度和MAP、HR P组>F组>CF组;术后CGRP浓度:CF组>F组>P组(P<0.05).不良反应发生率三组差异无统计学意义.结论 对高血压病人,可乐定透皮贴剂增强芬太尼PCIA镇痛作用,使血流动力学更稳定.