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41.
Jack C. Kim 《Archives of pharmacal research》1994,17(3):204-206
A regioselective preparation of 10-methoxy-11-hydroxyaporphine (“Apocodeine,1b”) from (R,S)-10, 11-dihydroxyaporphine(apomorphine,1a) is described. The isopropylidene ketal ring of 10,11-(isopropylidenyldioxy) aporphine (2) obtained by the isopropylidenation of apomorphine, was regioselectively opened by the ten equivalent of trimethylaluminum
to give 10-hydroxy-11-t-butyloxyaporphine (3). The free 10-hydroxyl position of 3 was methylated with methyl p-toluenesulfonate/NaH, and afforded 10-methoxy-11-t-butyloxyaporphine
(4) in high yield. Selective debutylation gave the desired 10-methoxy-11-hydroxyaporphine (“apocodeine”,1b) in good yield. 相似文献
42.
用体外培养的人的伪表皮作为模型,进行药物毒理学作用的研究,观察了二甲亚砜(DMSO)在不同浓度和不同接触时间条件下,对人的伪表皮细胞脱氧核糖核酸(DNA)、核糖核酸(RNA)和蛋白质合成的影响:随着接触时间的延长,DNA、RNA和蛋白质合成均受抑制。低浓度条件下(1%),DNA、RNA和蛋白质合成增加;在15~50%浓度下,DNA和蛋白质合成抑制,而RNA合成仍增加;在高浓度条件下(70%~100%),DNA、RNA和蛋白质合成均明显抑制。 相似文献
43.
靳培英 《中国新药与临床杂志》1992,(5)
443例(男225例,女218例;年龄36±14a)皮肤病患者,其中150例(扁平疣52例、寻常疣55例、银屑病43例)外用含1.8%十二烷氮(艹卓)酮的1%氟尿嘧啶(5-FU)凝胶作为治疗组,148例外用1%5-FU凝胶及145例外用2.5%5-FU霜作为2个对照组。经双盲对照临床试验,结果表明含1.8%十二烷氮(艹卓)酮的1%5-FU凝胶的疗效明显优于2个对照组(P<0.01及P<0.005)。证明氮(艹卓)酮对5-FU确有渗透促进作用。 相似文献
44.
E M Mathus-Vliegen K van de Voorde A M Kok A M Res 《Journal of internal medicine》1992,232(2):119-127
Dexenfluramine, an effective and safe serotoninergic drug with anorectic and possible food-selection-tuning properties, was investigated in a placebo-controlled study of 1 year's duration in severe and refractory obesity. The aim of the study was to assess weight loss, and changes in cardiovascular risk factors, food intake and eating behaviour. Dexfenfluramine- and placebo-treated patients achieved a similar weight loss (greater than 10% of initial weight, by 39.5 and 30.0%, greater than 20% of initial overweight by 42.1% and 32.5% and greater than 10 kg by 41.4 and 33.3%, respectively, of the initial cohorts). Furthermore, the decreases in weight (10.7 vs. 8.0 kg), in body mass index (3.9 vs. 2.9 kg m2) and in waist/hip ratio (0.04 vs. 0.02) were not significantly different. After discontinuation of the drug, the increase in weight (2.8 vs. 1.0 kg) was significantly higher in the dexfenfluramine-treated group. Except for a borderline better effect on glucose of dexfenfluramine, both groups showed similar beneficial changes in food intake and cardiovascular risk factors. Eating behaviour in response to emotional and external stimuli was comparable in the two groups, but placebo-treated patients had to restrain their eating more in order to achieve the same weight loss. Notwithstanding the fact that weight losses and an associated amelioration of health-risk factors were of similar magnitude in dexfenfluramine- and placebo-treated patients, dexfenfluramine might have a useful role in promoting a less stressed adherence to prolonged restriction of energy intake in the severe and refractory obese subject. 相似文献
45.
46.
MARINA GOBBO LAURA BIONDI FERNANDO FILIRA TOM PIEK RANIERO ROCCHI 《Chemical biology & drug design》1995,45(5):459-465
Syntheses are described of the endo-Lys8a-vespulakinin 1 and of cyclo-Thr6- and cyclo-Nε-Lys-bradykinin. The linear peptides covering the entire sequences of endo-Lys8a-VSK-1 and Thr6-BK, and the decapeptide containing all residues constituting Lys-BK, with a Arg-Lys peptide bond involving the ε-amino function of lysine, were prepared by the solid-phase procedure based on Fmoc chemistry. Cyclization was carried out by the diphenylphosphorazide method. The amino-terminal octapeptide sequence of vespulakinin 1, Fmoc-Thr(tBu)-Ala-Thr(tBu)-Thr(tBu)-Arg(Pmc)-Arg(Pmc)-Arg(Pmc)-Gly-OH, and its Nα-Boc-[(Gal β)Thr3, (Gal β)Thr4]-analogue, were used to prepare Nα-(1–8 VSK 1)-cyclo-Nε-kallidin and Nα-[(Gal β)Thr3, (Gal β)Thr4, 1–8 VSK 1]-cyclo-Nε-kallidin. Peptides and glycopeptides were characterized by amino-acid analysis, optical rotation, analytical HPLC and FAB-MS. Consistent with previous findings, preliminary pharmacological experiments on smooth muscle preparations showed that the cyclic, or partially cyclic, analogues were significatively less potent than the linear ones. © Munksgaard 1995. 相似文献
47.
K.M. SIVANANDAIAH V.V. SURESHBABU S.C. SHANKARAMMA 《Chemical biology & drug design》1995,45(4):377-379
Deprotection of the tert-butoxycarbonyl group during solid-phase synthesis of peptides can be conveniently and efficiently carried out using a neutral reagent, silicon tetrachloride/sodium iodide (iodotrichlorosilane). This simple and rapid method has been advantageously employed during the solid-phase synthesis of the pituitary hormone, oxytocin. 相似文献
48.
Peter Schnider MD Joachim Maly PhD Josef Grünberger PhD Susanne Aull MD Karl Zeiler MD Peter Wessely MD 《Headache》1995,35(5):269-272
A considerable proportion of headache patients fulfill the criteria of "drug abuse" (definition according to the International Headache Society [IHS] criteria). These patients exhibit markedly reduced vigilance and continuous performance, as shown by the results of critical flicker frequency (CFF) analysis.
The present study deals with the question whether this impairment of vigilance and continuous performance is reversible. Forty-eight headache patients with drug abuse were investigated three times by means of CFF analysis: immediately before (A), immediately after (B), and 3 weeks after having finished (C) inpatient drug withdrawal.
Immediately after withdrawal, a significant decrease of headache intensity was observed. The CFF values, however, remained unchanged at a depressed level, probably due to withdrawal medication and the initial sedative side effects of thymoleptic agents (given as prophylaxis).
Three weeks after withdrawal, however, the CFF values were significantly improved, and were now within a range not far from the normal values known from a healthy general population. Thus, even after many years of drug abuse, headache patients have a good chance to improve their vigilance and continuous performance and to reach normal or close to normal levels. 相似文献
The present study deals with the question whether this impairment of vigilance and continuous performance is reversible. Forty-eight headache patients with drug abuse were investigated three times by means of CFF analysis: immediately before (A), immediately after (B), and 3 weeks after having finished (C) inpatient drug withdrawal.
Immediately after withdrawal, a significant decrease of headache intensity was observed. The CFF values, however, remained unchanged at a depressed level, probably due to withdrawal medication and the initial sedative side effects of thymoleptic agents (given as prophylaxis).
Three weeks after withdrawal, however, the CFF values were significantly improved, and were now within a range not far from the normal values known from a healthy general population. Thus, even after many years of drug abuse, headache patients have a good chance to improve their vigilance and continuous performance and to reach normal or close to normal levels. 相似文献
49.
Objective To identify the direct causes of drug relapse and abstainers’ demand, and to develop programs for the prevention of drug relapse. Methods Abstainers in a Compulsive Detoxification Center in Wuhan City, capital of Hubei Province were randomly selected. An investigation on the direct causes of drug relapse and abstainers’ demands was conducted with multiple-choice questionnaires and face to face interviews. Data were analyzed with SPSS 12.0. Results The direct causes leading to drug relapse included: temptation to use drug again by themselves or by their drug mates, seeking pleasure and ecstasy from drug use, relatively well off living, mental stress, irritation, demoralization, family conflicts, unemployment, feeling distrusted by the family, lack of care and love from the family, and discrimination by others. abstainers’ demands after detoxification and returning to the society included: care and support from the family, employment assistance, changing living environment, understanding by others, support from the society, and keeping far away from drugs. Conclusions Environmental factors are the direct causes of drug relapse, and negative irritation is its predisposing causes. Leaving former residence, more care and help given by both the family and the society and raising their overall quality of life are the demands of abstainers. 相似文献
50.