1-乙基-6-氟-1,4-二氢-4-氧代-7-(4-芳酰硫代氨甲酰基-1-哌嗪基)-3-喹啉羧酸的合成及抗菌作用

Thirteen new 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-aroyl-thiocarbamoyl- 1 piperazinyl)-3-quinoline carboxylic acids were prepared, Their structures were characterized by elemental analysis, IR, HNMR and MS spectra.Preliminary pharmacological tests indicated that some of compounds Ia～m possess strong inhibiting activity against Escherichia coli, Bacillus subtilis and Proteus at concentration of 100 μg/ml.     

Basal metabolism adds a significant offset to unloaded myocardial oxygen consumption per minute.

Myocardial oxygen consumption (MVO2) includes components for 1) mechanical energy generation, 2) activation, and 3) basal metabolism. Whereas the first two components are expected to increase in proportion with heart rate, a significant basal level of metabolism would consume oxygen even if the heart rate were zero. Contrary to this expectation, however, a previous study reported that, during unloaded beats, MVO2 per beat (which includes basal metabolism) was independent of heart rate. Accordingly, unloaded MVO2 per minute would extrapolate to zero at zero heart rate; this result is unexpected considering basal metabolism. To resolve this inconsistency, we varied heart rate over a wide range after inducing atrioventricular block in eight isolated cross-circulated canine hearts that contracted isovolumically. We examined whether a term representing rate-independent basal metabolism was needed to describe MVO2 per minute. Mechanical energy generated by the left ventricle was evaluated from the pressure-volume area, which was altered by changing isovolumic ventricular volume over at least five levels at each heart rate. Contractility, evaluated by the slope of the end-systolic pressure-volume relation, did not vary significantly with heart rate in this study. In contrast to the previous report, unloaded MVO2 per beat (i.e., MVO2 extrapolated to a pressure-volume area of zero) was not constant but fell monotonically with increases in heart rate in every heart. We considered that this trend was caused by a significant rate-independent basal level of MVO2 per minute. Multiple linear regression analysis confirmed that this rate-independent basal term differed significantly from zero in seven of the eight hearts studied.(ABSTRACT TRUNCATED AT 250 WORDS)     

Criteria for evaluating the clinical and practical utility of models used by nurses

Arguably, nursing, like all health care disciplines, is an applied science. Essentially, this refers to the application of theory in order to understand and respond to the health problems of clients. These theories may be drawn (borrowed) from any applied science, or generated inductively from clinical nursing practice. Alternatively, nurses may attempt to apply deductive theory (global theoretical frameworks) known as nursing models. In this paper, all theoretical approaches, irrespective of origin, are referred to as models used by nurses. Thirteen criteria by which clinicians, and others, can evaluate the clinical and practical utility of models used by nurses which are expressed in the form of questions are identified and discussed. The criteria are an extension, both in detail and in number, of those developed by Reynolds and Cormack and subsequently applied by those writers to the Johnson Behavioural System Model of Nursing. The value, or otherwise, of individual models, or of models in general, will not be discussed in this paper. However, the authors propose that if the evaluation criteria described here are applied to existing models, serious deficits will be identified in relation to their clinical and practical utility.     

Identification of MEN1 gene mutations in sporadic carcinoid tumors of the lung

Lung carcinoids occur sporadically and rarely in association with multiple endocrine neoplasia type 1 (MEN1). There are no well defined genetic abnormalities known to occur in these tumors. We studied 11 sporadic lung carcinoids for loss of heterozygosity (LOH) at the locus of the MEN1 gene on chromosome 11q13, and for mutations of the MEN1 gene using dideoxy fingerprinting. Additionally, a lung carcinoid from a MEN1 patient was studied. In four of 11 (36%) sporadic tumors, both copies of the MEN1 gene were inactivated. All four tumors showed the presence of a MEN1 gene mutation and loss of the other allele. Observed mutations included a 1 bp insertion, a 1 bp deletion, a 13 bp deletion and a single nucleotide substitution affecting a donor splice site. Each mutation predicts truncation or potentially complete loss of menin. The remaining seven tumors showed neither the presence of a MEN1 gene mutation nor 11q13 LOH. The tumor from the MEN1 patient showed LOH at chromosome 11q13 and a complex germline MEN1 gene mutation. The data implicate the MEN1 gene in the pathogenesis of sporadic lung carcinoids, representing the first defined genetic alteration in these tumors.      

Anxiolytic-like effects of yohimbine in the murine plus-maze: strain independence and evidence against α2-adrenoceptor mediation

The influence of ₂-adrenoceptor antagonists in animal models of anxiety is quite inconsistent, with results spanning the full range of effect from anxiogenesis to anxiolysis. In the present study, an ethological technique was used to examine the effects of yohimbine (0.5–4.0 mg/kg) on plus-maze behaviour in DBA/2 mice. Results indicated significantanxiolytic-like effects on standard spatiotemporal measures at 2.0–4.0 mg/kg, and on risk assessment measures across the entire dose range. Full-scale follow-up studies with T1 and BALB/c strains confirmed that this action of yohimbine in the murine plus-maze is not peculiar to DBA/2 mice. The more selective ₂-adrenoceptor antagonist, idazoxan (0.63–5.0 mg/kg), exerted much weaker behavioural effects in the maze while the ₂-adrenoceptor agonist, clonidine (0.01–0.1 mg/kg), produced a profile consistent with non-specific behavioural disruption. Data are discussed in relation to the possible involvement of 5-HT_1A receptor mechanisms in the observed anxiolytic-like effects of yohimbine in the murine plus-maze.