6-(4-酰基-1-哌嗪乙酰氨基)-3,4-二氢-2(1H)-喹啉酮类化合物的合成及正肌力活性初探

目的 :寻找具有正性肌力活性的化合物。方法 :根据文献报道的二氢喹啉酮类正性肌力药物的结构特点 ,设计、合成了其类似物。以苯胺为起始原料经多步合成 ,对所得化合物用离体豚鼠心脏与主动脉观察了心肌收缩力、扩血管作用及心率。结果 :合成了 1 0个 6 ( 4 酰基 1 哌嗪乙酰氨基 ) 3 ,4 二氢 2 ( 1H) 喹啉酮类化合物 ( 4a～ 4j) ,均为未见文献报道的化合物。结论 :初步药理试验表明 ,化合物 ( 4h)显示了正性肌力及扩血管活性。     

Chronic beta 1-adrenoceptor antagonist treatment sensitizes beta 2-adrenoceptors, but desensitizes M2-muscarinic receptors in the human right atrium.

1. In 64 patients undergoing coronary artery bypass grafting the effects of chronic beta 1-adrenoceptor antagonist (metoprolol, atenolol, bisoprolol) treatment on right atrial beta-adrenoceptor and muscarinic M2-receptor number and functional responsiveness were investigated. 2. The beta 1-adrenoceptor antagonists increased right atrial beta 1-adrenoceptor number, did not affect beta 2-adrenoceptor number, and decreased muscarinic M2-receptor number. 3. Concomitantly, activation of right atrial adenylate cyclase by 10 microM GTP, 10 microM isoprenaline and 1 microM forskolin was enhanced and inhibition by 100 microM carbachol was diminished. 4. On isolated, electrically driven right atria the beta 1-adrenoceptor-mediated positive inotropic effect of noradrenaline was - even with beta 1-adrenoceptor number increased - not altered, while the beta 2-adrenoceptor-mediated effect of procaterol was markedly enhanced. However, the carbachol-induced negative inotropic effect was decreased. 5. It is concluded that chronic beta 1-adrenoceptor antagonist treatment increases beta 1-adrenoceptor number and concomitantly sensitizes beta 2-adrenoceptor function, but desensitizes muscarinic M2-receptor function in the human heart.     

Ocular and orbital lesions: surface coil MR imaging

Nine lesions, four ocular (three melanomas, one hemangioma) and five orbital (two perioptic meningiomas, one hemangioma, one pseudotumor, one mucocele), were evaluated by magnetic resonance surface coil imaging at 1.5 T. Small ocular lesions with 3.9-4.5-mm-elevation were demonstrated. The use of two different pulse sequences resulted in separation of melanoma from adjacent retinal detachment. Contrast obtained between orbital lesions and the adjacent normal structures was better than that demonstrated with high-resolution computed tomography.     

Diagnosis and Therapeutic Consequences of Intramural Aortic Hematoma

The classical triad of sudden devastating chest pain, electrocardiographic absence of acute myocardial Infarction, and Identification of an upstream flap in the ascending aorta by transesophageal echocardlography (TEE) Indicates aortic type A dissection requiring emergent surgery. Among 34 patients presenting with clinical signs and symptoms of an aortic dissection, three did not show the mandatory flap in the upstream aorta. The only echocardlographic finding was aortic wall thickening Indicating an intramural hematoma. Two of these patients showed early aortic ectasia and one showed a pericardial effusion. Despite the missing flap echocardiographlcally, surgery was performed in all three patients. The surgical approach was the same as that for patients with a type A dissection. Two patients are doing well after the procedure, and one patient died after reoperation. The postoperatlve histologic work-up confirmed that there was no intimal tear or dissection of the intimal layer. We conclude that the echocardiographic finding of an Intramural hematoma combined with typical clinical signs of chest pain, with myocardial infarction ruled out, requires emergent surgical intervention. (J Card Surg 1994;9:508–515)     

Selective regulation of beta 1- and beta 2-adrenoceptors in the human heart by chronic beta-adrenoceptor antagonist treatment.

1. In 44 patients undergoing coronary artery bypass grafting, the effect of chronic administration of the beta-adrenoceptor antagonists sotalol, propranolol, pindolol, metoprolol and atenolol on beta-adrenoceptor density in right atria (containing 70% beta 1- and 30% beta 2-adrenoceptors) and in lymphocytes (having only beta 2-adrenoceptors) was studied. 2. beta-Adrenoceptor density in right atrial membranes and in intact lymphocytes was assessed by (-)-[125I]-iodocyanopindolol (ICYP) binding; the relative amount of right atrial beta 1- and beta 2-adrenoceptors was determined by inhibition of ICYP binding by the selective beta 2-adrenoceptor antagonist ICI 118,551 and analysis of the resulting competition curves by the iterative curve fitting programme LIGAND. 3. With the exception of pindolol, all beta-adrenoceptor antagonists increased right atrial beta-adrenoceptor density compared to that observed in atria from patients not treated with beta-adrenoceptor antagonists. 4. All beta-adrenoceptor antagonists increased right atrial beta 1-adrenoceptor density; on the other hand, only sotalol and propranolol also increased right atrial beta 2-adrenoceptor density, whereas metoprolol and atenolol did not affect it and pindolol decreased it. 5. Similarly, in corresponding lymphocytes, only sotalol or propranolol increased beta 2-adrenoceptor density, while metoprolol and atenolol did not affect it and pindolol decreased it. 6. It is concluded that beta-adrenoceptor antagonists subtype-selectively regulate cardiac and lymphocyte beta-adrenoceptor subtypes. The selective increase in cardiac beta 1-adrenoceptor density evoked by metoprolol and atenolol may be one of the reasons for the beneficial effects observed in patients with end-stage congestive cardiomyopathy following intermittent treatment with low doses of selective beta 1-adrenoceptor antagonists.     

保存12周的红细胞

现代液体红细胞保存体系运行良好,使一个国家供应的异体红细胞安全、廉价,并且有效率达到95％。现代红细胞保存系统在临床上用途广泛,如可为自身输血提供血液,可为战场上的手术输送血液,避免献血者接触新生儿,显然如果延长红细胞的保存期将会有更大的益处。然而,由于衰老的红细胞具有使血流不畅,细胞破裂后一些有毒性的脱出物可能使外伤病人的死亡率增加和导致输血相关急性肺损伤(TRALI),进一步研究建立更好的红细胞保存体系仍然很重要。     

Was und zu welchem Ende lernen wir?

Ohne Zusammenfassung     

The efficacy of bismuth subsalicylate in the treatment of acute diarrhoea and the prevention of persistent diarrhoea

A controlled, randomized, double-blind study in Bangladeshi children (ages 4-36 mo) with acute diarrhoea was undertaken to determine whether bismuth subsalicylate (BSS) would prevent the development of persistent diarrhoea (PD) in young children. The children were randomized to two groups: 226 were given liquid oral BSS, (as Pepto-Bismol), 100 mg/kg/d for 5 d; 225 were given placebo of identical appearance. On admission to the study, the two groups were comparable both clinically and microbiologically. Rotavirus was found in 56% of all the children, and enterotoxigenic E. coli in 31% of a subsample studied. Children treated with BSS had less severe and less prolonged illness than those treated with placebo (p = 0.057). There was, however, no difference in the development of PD between the two groups (8% and 11%). Unexpectedly, patients treated with BSS gained significantly more weight (2.3%) than those treated with placebo (0.5%; p < 0.001) during the course of the study. No toxicity of BSS was detected. Conclusion: Treatment with BSS had a modest therapeutic effect on acute diarrhoea, as has been previously demonstrated, but with no suggestion of a therapeutic effect on the prevention of persistent diarrhoea in this group of patients.     

Spider phobics more easily see a spider in morphed schematic pictures

Background  

A dominant view in numerical cognition is that numerical comparisons operate on a notation independent representation (Dehaene, 1992). Although previous human neurophysiological studies using scalp-recorded event-related potentials (ERPs) on the numerical distance effect have been interpreted as supporting this idea, differences in the electrophysiological correlates of the numerical distance effect in symbolic notations (e.g. Arabic numerals) and non-symbolic notations (e.g. a set of visually presented dots of a certain number) are not entirely consistent with this view.