Flumazenil exerts intrinsic activity on sleep EEG and nocturnal hormone secretion in normal controls

The physiological function of benzodiazepine (BDZ) receptors includes regulation of sleep and neuroendocrine activity. Most of the pharmacological effects of BDZ are blocked by flumazenil. However, recent neurological and behavioral studies suggest that flumazenil has its own central intrinsic activity. This issue was addressed in a study of the sleep EEG and the nocturnal secretion of growth hormone and cortisol in ten normal male controls, who were given flumazenil either alone or in combination with the BDZ agonist midazolam, placebo and midazolam alone. Flumazenil prompted an increase in sleep onset latency, a decrease in slow wave sleep and an increase in wakefulness. Plasma cortisol concentrations after flumazenil administration were lower than after midazolam. Both flumazenil and midazolam decreased nocturnal growth hormone secretion. After simultaneous application of both BDZ receptor ligands the growth hormone blunting was amplified. Our study demonstrates that at the level of the sleep EEG and neuroendocrine activity flumazenil is capable of exerting both agonistic and inverse agonistic or antagonistic effects.Parts of this study were presented at the 69th Meeting of the Deutsche Physiologische Gesellschaft, Freiburg, 6–8 March, 1991     

Effect of pindolol on endocrine and temperature responses to buspirone in healthy volunteers

Ten healthy subjects received buspirone (30 mg orally) with and without pre-treatment with the 5-HT1A receptor antagonist, pindolol (80 mg over 3 days). Following pindolol treatment the growth hormone and hypothermic responses to buspirone were significantly decreased. There was also a delay in the onset of the prolactin response to buspirone but the total amount of prolactin secretion, calculated as area under the curve, was not significantly reduced. The data suggest that the growth hormone and hypothermic responses to buspirone in humans are mediated by 5-HT1A receptors, but an explanation founded on pharmacokinetic factors cannot presently be excluded. Both this latter possibility and the lack of selectivity of pindolol for 5-HT receptors indicate the need for the further neuroendocrine studies of the mode of action of buspirone, preferably with more selective 5-HT1A receptor antagonists.     

Human Y-79 retinoblastoma cells express functional corticotropin-releasing hormone receptors

In human Y-79 retinoblastoma cells corticotropin-releasing hormone (CRH) produces a marked and rapid increase of adenylate cyclase activity. The concentration of the peptide producing half-maximal stimulation is 60 nM. The effect of CRH is significantly antagonized by the specific CRH receptor antagonist alpha-helical CHR 9-41 and is mimicked by sauvagine and urotensin I, two peptides displaying sequence homology with CRH. These results demonstrate the presence of functional CRH receptors in human Y-79 retinoblastoma cells and suggest that this cell line may be a suitable model in which to study the action of CRH on human retinal cell function.     

对500名广州妇女关于激素替代疗法态度的调查

【目的】了解广州妇女对激素替代疗法 (HRT)的态度。【方法】对 5 0 0名妇女进行面对面的问卷调查 ,记录她们对绝经症状以及激素替代疗法的认识和态度。【结果】 5 9%的妇女认为对绝经症状应该求医 ,41%妇女采取消极忍耐的态度 ,76 2 %的人选择妇科就诊 ,19 8%的妇女选择内外科或精神科 ;仅有 2 2 1%的妇女听说过HRT。绝经后妇女应用HRT的有5 9% ,2 4 4%的人不知道HRT的益处 ,知道可以预防骨质疏松和心血管疾病的分别有 17 8%和 10 8% ,5 9 8%的人不知道HRT的副作用 ,13 6 %的人不知道在哪科医生的指导下应用HRT ,40 4%的人不知道何时开始应用HRT。【结论】我们认为广州妇女的围绝经期保健意识不强 ,对HRT的了解很少 ,对HRT的利弊认识不足 ,有必要开展这方面的科普教育工作。     

带血管甲状腺-甲状旁腺移植术5例报告

用带血管的胎儿甲状旁腺移植术治疗甲状旁腺机能低下症,共行手术6次(腹腔内移植5次,股三角区移植1次),6次中有3例术后发生4次排斥反应。经1年8月至3.5年随防,疗效显著者2例,有效2例,失败1例。本文讨论了有关甲状旁腺移植的手术方法、注意事项、免疫抑制剂应用等问题。     

LHRH-A对孕中期大鼠抗妊娠作用的研究

本文观察了[D-Ala⁶,Pro⁹-Ethylamide¹⁰]-LHRH(LHRH-A)对孕中期大鼠的抗妊娠作用。结果显示:在孕9～11d sc 200μg/d LHRH-A,血浆孕酮水平自第二次给药后明显下降(P<0.05),给药大鼠均流产终止妊娠;LHRH-A的抗妊娠作用可被醋酸甲地孕酮所拮抗;LHRH-A对体外培养的假孕大鼠和孕d 9大鼠黄体细胞分泌孕酮有明显的直接抑制作用。     

Carbohydrate metabolism in children receiving growth hormone for 5 years

Carbohydrate metabolism was evaluated by fasting and postprandial glucose, insulin, and hemoglobin (Hb)A_1c levels in children with chronic renal insufficiency and various other growth disorders treated with growth hormone. Mean fasting and postprandial glucose remained unchanged throughout the 5-year study period in all four study groups. Median fasting insulin levels rose from lownormal levels into the normal range after 5 years of growth hormone. Average fasting insulin level after 5 years was 10 mU/l. Median postprandial insulin values also rose, yet remained within the normal range at the 5-year mark. Mean Hb A_1c levels remained within low to middle end of the normal range in the patients with growth hormone deficiency, Turner syndrome, and idiopathic short stature. Mean Hb A_1c levels at the 5 years were slightly elevated to 6.3% for the patients with chronic renal insufficiency.     

质粒pGH/BL_(21)在大肠杆菌中表达条件的研究

目的　寻找质粒 pGH/BL2 1在大肠杆菌中的最佳表达条件。方法　当它在大肠杆菌中表达时 ,考查不同IPTG诱导浓度及不同的诱导时间对表达产物的影响 ,表达产物的量以SDS -PAGE电泳方法分析。结果　该基因的最佳表达条件为 :IPTG诱导浓度 1.0mmol/L ,诱导时间 4h。结论　IPTG对不同的基因在不同的表达体系中需不同的诱导条件 ,只有找到它的最佳诱导条件才能保证终产物的最大产率     

生长激素在体外对人胃癌细胞的作用

目的　研究重组人生长激素 (rhGH)在体外对人胃癌细胞生长的影响。方法　实验分组 :对照组、rhGH组、奥沙利铂 (L OHP)组和rhGH L OHP组 ,利用体外细胞培养、MTT比色技术及流式细胞仪等方法 ,测定不同浓度的rhGH对人胃癌细胞株BGC82 3生长曲线、细胞抑制率、细胞周期和增殖指数 (PI)的影响。结果　rhGH在体外无明显促进BGC82 3细胞分裂增殖 ,rhGH组与对照组、rhGH L OHP组与L OHP组比较差异均无显著性 (P >0 .0 5 ) ,且生长曲线没有升高 ;rhGH L OHP组与对照组比较或rhGH L OHP组与对应的rhGH组配对比较 ,细胞抑制率增加 ,阻滞于G0 ～G1期的细胞数增加 ,S期细胞明显减少 ,PI明显降低 (P <0 .0 1)。rhGH L OHP组与L OHP组比较 ,细胞抑制率呈现升高趋势 ,而PI呈下降趋势 ,提示rhGH与抗肿瘤药合用可以增强抗肿瘤药对肿瘤细胞的杀伤作用。结论　rhGH在体外无明显促进胃癌细胞的分裂增殖 ,与抗肿瘤药合用可提高抗肿瘤药的疗效。