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Antiserum against purified beta-lactamase from Proteus vulgaris GN7919 cross-reacted with beta-lactamases produced by strains of Pseudomonas cepacia in a neutralization test. Anti-P. cepacia beta-lactamase serum, however, did not show any cross-reactions with P. vulgaris beta-lactamases. Each of these enzymes can hydrolyze cefuroxime and cefotaxime.

The present paper demonstrates a handheld computer system for use in perinatal care. The features of the system are as follows: The gestational age and fetal body weight were determined by analyzing the data from ultrasonography with the high-order regressive equation. The combined use of the linear regressive equation and Ott's equation was more useful in precisely calculating the fetal abdominal circumference. In order to decrease input error, attempts were made to minimize key-operations for data-entry. The use of the screen edition system also made it easier to correct input error. It was concluded that this system was practical and easy to handle, and would be a useful aid in clinical care.

To estimate regional left ventricular (LV) diastolic filling patterns in hypertrophic cardiomyopathy (HCM), a computer-assisted method by applying "sector analysis" to ECG forward and reverse gated radionuclide ventriculography was developed. Fourteen patients with HCM (four with localized septal hypertrophy, seven with apical hypertrophy and three with septal and apical hypertrophy according to echocardiography) were observed at rest. After establishing serial 20 msec imaged frames, the LV region of interest was subdivided into eight sectors radiating from the geometric center. A time-activity curve was generated for each sector and was fitted by third-order harmonics of the Fourier series. From each fitted curve, the regional peak filling rate (rPFR) and the time of rPFR (rTPFR) in the forward gating method and regional atrial contribution to filling (rAC/FV) in the reverse gating method were calculated. The coefficient of variance of rTPFR was used as an index of LV diastolic asynchrony. In HCM, a prominent delay of rTPFR was observed in the hypertrophied regions. The coefficient of variance of rTPFR correlated inversely with global LVPFR (r = -0.62, p less than 0.05), indicating that diastolic asynchrony is one of the determinants of the LV early filling rate. Regional AC/FV was augmented in the hypertrophied regions, indicating the important role of atrial systolic LV filling for slowed early filling. Thus, this new method provides valuable information concerning regional diastolic LV wall mechanics in HCM.

A dry powder of betel nuts, piper betel leaves and lime was administered to rats. Epidermal thickening was frequently observed in the upper digestive tracts of rats in groups fed the betel nut diet mixed with lime and the betel leaves diet, and a forestomach papilloma was seen in 1 rat given betel leaves diet. These epidermal changes were scarcely seen in rats given either betel nut or normal diet alone.

A 41 year-old male was admitted to our hospital, because a suspicious shadow in the right lower lung field was on X-ray. Investigations could not confirm cancer but were highly suggestive of it. Finally, right lower lobectomy was performed, and the histopathological finding of the tumor resected were a mixture of epithelial components in myxomatous tissue, so a diagnosis of pleomorphic adenoma of the lung was made.

The carcinogenicity of the pyrrolizidine alkaloids senkirkine and symphytine was studied in male inbred ACI rats. Animals were divided into 3 groups: Group I received ip injections of freshly prepared senkirkine at a dose of 10% of the median lethal dose (LD50) twice weekly for 4 weeks and then once a week for 52 weeks. Group II received ip injections of symphytine at a dose of 10% of the LD50 by the same injection schedule as in group I. The control group was given ip injections of a 0.9% NaCl solution following the same injection schedule as in experimental groups. All group I rats survived for more than 290 days after the start of injections, and 9 of 20 rats developed liver cell adenoma. All group II animals survived for more than 330 days after the start of injections. Of 20 rats, 4 had liver tumors, 3 had hemangioendothelial sarcomas, and 1 had liver cell adenoma. The hemangioendothelial sarcomas showed metastasis in the lungs of 2 rats. The control group had no liver tumors.

The chronic effects of the oral administration of OPC-8212 (3,4-dihydro-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-2(1H)-quinolinon e) on resting hemodynamics and exercise capacity were assessed in 15 patients with congestive heart failure (NYHA II-IV). Doses of 30 or 60 mg per day were given per os over 3.0 weeks on average (range 2-6 weeks). Multigated radionuclide ventriculography and multistage exercise testing were performed before and during OPC-8212 therapy to assess the changes in left ventricular volume and exercise capacity respectively. Systolic blood pressure showed a slight increase (from 123 +/- 3 to 129 +/- 4 mmHg) during OPC-8212 therapy, while heart rate was unchanged (69 +/- 3 vs 67 +/- 3 beats/min). The left ventricular end-diastolic volume index decreased from 127 +/- 9 to 107 +/- 7 ml/m2, and ejection fraction and the P/V index (the ratio of peak systolic pressure to left ventricular end-systolic volume index) increased during OPC-8212 therapy (from 27% +/- 3% to 30% +/- 4% and from 1.5 +/- 0.2 to 2.0 +/- 0.3 mmHg/ml/m2 respectively). NYHA functional class was improved in 9 of 15 patients, and the average peak work load achieved during exercise testing increased from 27 +/- 6 to 47 +/- 7 W. No significant adverse effect was observed in any patient. These results indicate that OPC-8212 enhances the inotropic state and, hence, reduces heart size with no change in heart rate. Moreover, it increases exercise capacity. Thus, OPC-8212 is an inotropic agent with promise for application in the long-term treatment of congestive heart failure.

Cefoperazone, a new semisynthetic cephalosporin, has a broad spectrum of antibacterial activity. It is as active as cefazolin and cefamandole against gram-positive bacteria and is more active than cefazolin and cefamandole against such gram-negative bacilli as Escherichia coli, Klebsiella pneumoniae, Proteus species, Pseudomonas aeruginosa, Citrobacter freundii, Enterobacter cloacae, and Serratia marcescens. The superiority of cefoperazone over cefazolin and cefamandole with respect to activity against P. aeruginosa by more than 200-fold was especially remarkable. As with other beta-lactam antibiotics, there was only a small spread between the minimum inhibitory concentrations and the minimum bactericidal concentrations of cefoperazone and a significant decrease in activity with an increase in inoculum size. Activity was not altered significantly by the addition of human serum to the test medium. Cefoperazone is relatively stable to hydrolysis to beta-lactamases produced by gram-negative bacteria. Relative rates of hydrolysis of cefoperazone by cephalosporinases are 7.0 to 0.01, with reference to cephaloridine hydrolysis (base, 100). Cefoperazone is also more stable than penicillin G and cephaloridine to various types of penicillinases.

The activity of cefoperazone against a strain with an inducible cephalosporinase and a mutant that produces the enzyme constitutively indicates that the low inducer activity of this antibiotic plays an important role in its activity against Enterobacter cloacae.

The purified cephalosporinase from Proteus vulgaris hydrolyzed a variety of cephalosporins, including cefuroxime, at a high level; its activity was inhibited by clavulanic acid.

The effect of the fecal stream on the induction of intestinal tumors was studied in 3 groups of SD rats. Rats in group 1 were subjected to single-barreled colostomies for the complete exclusion of the fecal stream at the proximal one-third level of the colons and were given consecutive iv injections of methylazoxymethanol acetate. Rats in group 2 were given methylazoxymethanol acetate alone. Rats in group 3 were not treated and served as controls. Tumors were noted in the small and large intestines of almost all rats in both groups 1 and 2. Even animals with single-barreled colostomies frequently developed tumors in the colon distal to the colostomy where the mucosa did not have contact with the fecal stream. These results indicated that carcinogens could probably reach the intestinal mucosa via the vascular system as well as by biliary transport.

The enzymic inactivation of cephamycins, i.e. cefoxitin, cefmetazole, cefotetan and cefbuperazone, was investigated by means of bioassay, high pressure liquid chromatography (HPLC) and spectrophotometric analysis using three types of cephalosporinase (CSase, RICHMOND type Ia, Ib and Ic) and one penicillinase (PCase, TEM type). These four cephamycins were not inactivated by Ic CSase and TEM type PCase or producers of these enzymes. However, the inactivation of cefmetazole and cefoxitin was noted when they were incubated in the cultures of CSase (Ia and Ib)-producers or incubated with a large amount of these purified enzymes although the inactivation of cefbuperazone was not noted. HPLC of culture fluid or enzyme solution which contained cefmetazole or cefoxitin and were incubated at 37 degrees C showed that metabolites of cefmetazole or cefoxitin appeared as the drug disappeared. In addition, the appearance of metabolites corresponded to the loss of the drug's bioactivities and the absorption of iodine. UV and IR spectra of cefmetazole which were taken after incubation with the purified CSase showed the cleavage of the beta-lactam ring.

A biologically inert photolabile precursor of carbamoylcholine has been synthesized; it is photolyzed to carbamoylcholine, a well-characterized acetylcholine analogue, with a half-time of 40 microseconds at pH 7.0 and a quantum yield of 0.8. The compound, N-(alpha-carboxy-2-nitrobenzyl)carbamoylcholine, was synthesized from (2-nitrophenyl)glycine. The photolysis rates (of five compounds) and the biological activity (of two compounds) were determined, and both properties were found to depend on the nature of the substituents on the photolabile protecting group. Laser pulse photolysis at wavelengths between 308 and 355 nm was used to investigate the wavelength dependence, quantum yield, and rate of the photolysis reaction. Photolysis products were isolated by high-performance liquid chromatography and identified by chemical and spectroscopic analysis and by their ability to activate the nicotinic acetylcholine receptor. BC3H1 muscle cells containing those receptors and a cell-flow method were used in the biological assays. The approach described may be useful in the preparation and characterization of other photolabile precursors of neurotransmitters that contain amino groups. The importance of these rapidly photolyzed, inert precursors of neurotransmitters is in chemical kinetic investigations of the reactions involving diverse neuronal receptors; such studies have been hampered because the available techniques have an insufficient time resolution.

For determining an indication of percutaneous transluminal angioplasty (PTCA), a 73-year-old-man with silent ischemia and with ventricular premature complexes (quadrigeminy) were performed cardiac nuclear studies. This case had 99% stenosis in LCX (#11) and 90% stenosis in RCA (#1), and demonstrated akinetic wall motion in left ventricular (LV) inferior and posterior regions. Exercise-redistribution Tl-201 studies indicated myocardial viability in a portion of the inferior wall but not in the posterior wall. To estimate the potential contractile function in the regions with akinesis, from the list-mode data of radionuclide ventriculography, those of postsinus beats and postextrasystolic beats were separately selected and were analyzed for investigating LV wall motion and LV ejection fraction (EF). With the post-extrasystolic potentiation, LVEF increased from 36% to 45% and the systolic wall motion was augmented in the inferior wall but not in the posterior wall. From these findings we recognized the existence of myocardial viability in a portion of the inferior wall. After PTCA for the RCA lesion, improvements of the myocardial Tl-201 distribution and LV wall motion in the inferior wall were definitely observed and hence LVEF increased by 16% to contribute to an increase in exercise performance. Thus, this case indicates that the postextrasystolic potentiation is useful for determining an indication of PTCA in patients with LV asynergy, demonstrating the myocardial viability and the potential LV function.

Cefoperazone (T-1551, CFP) a new semisynthetic cephalosporin, has a broad spectrum of antibacterial activity. We investigated the affinity of CFP to penicillin-binding proteins (PBPs) and the inhibition of peptidoglycan synthesis by CFP. CFP had high affinities for Escherichia coli PBP-3, -1Bs, -2, and -1A, in descending order, and low affinities for PBP-4, -5, and -6. Similarly, CFP showed high affinity for Pseudomonas aeruginosa PBP-3, -1A, -1B, -2, and -4, in descending order. It is known that E. coli PBP-3 and P. aeruginosa PBP-3 participate in cell division. These results are in good agreement with the formation of filamentous cells of E. coli and P. aeruginosa treated with CFP. CFP had lower inhibitory activities on D-alanine carboxypeptidase IA and IB of E. coli than that of penicillin G, but its inhibitory activities on the cross-link formation in peptidoglycan synthesis were the same as those of penicillin G and higher than those of ampicillin.

The long-axis (L-A) tomograms of the heart in thallium-201 SPECT have been conventionally reconstructed as those parallel to the midventricular vertical or horizontal L-A plane. We developed a new algorithm for reconstructing the rotated L-A tomograms around the L-A to longitudinally observe thallium-201 myocardial distribution and to provide an optimal view of the cardiac apex. After determining the orientation of the L-A and reconstructing the short-axis (S-A) tomograms using standard techniques, the coordinates of the S-A planes were transformed to the polar coordinates whose origin is located at the position of the L-A in each plane. Then, "radial L-A tomograms", i.e. midventricular L-A planes oriented at the angle of every 6 degrees to the midventricular horizontal L-A plane, were reconstructed. Also, we developed a new technique for analyzing thallium-201 distribution of the L-A tomograms. For the basal 2/3 regions, two profiles which consist of the pixels with maximum count on the upper and lower myocardial portions of the lines (spaced at 1 pitch) vertically to the L-A were computed. For the remaining apical 1/3 regions, the semi-circumferential maximum-count profile from the values of 30 radii spaced at 6 degrees interval were computed. Based on these profiles, a 2D polar representation was then generated. From the study using a cardiac phantom with an apical small infarction, the usefulness of this new tomographic method for the detection of apical myocardial ischemia was demonstrated. The application to the exercise/redistribution studies in patients with effort angina indicated that radial long-axis tomography provides precise information about the longitudinal extent of perfusion defects, particularly in the apical regions.