ABSTRACT
New mu-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Among the synthesized compounds, 4-[4-(2-methoxyphenyl)piperazin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide (20 Aa) showed the highest affinity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells, and the highest agonist potency on the MOR in isolated guinea-pig ileum preparation.
Subject(s)
Piperazines/chemical synthesis , Receptors, Opioid, mu/agonists , Animals , CHO Cells , Cricetinae , Enkephalin, Ala(2)-MePhe(4)-Gly(5)-/pharmacology , Guinea Pigs , Humans , Ileum/drug effects , In Vitro Techniques , Indicators and Reagents , Magnetic Resonance Spectroscopy , Male , Mass Spectrometry , Muscle, Smooth/drug effects , Piperazines/chemistry , Piperazines/pharmacology , Receptors, Opioid, kappa/antagonists & inhibitors , Spectrophotometry, InfraredABSTRACT
New fibrates containing piperidine, 4-hydroxypiperidine, piperidin-3-ene, and piperazine moieties in the structures were synthesized and evaluated. Among the synthesized compounds, 2-[3-[1-(4-fluorobenzoyl)-piperidin-4yl]phenoxyl-2-methylpropanoic acid (9aA: AHL-157) showed very superior activities in decreasing triglyceride, cholesterol, and blood sugar compared to bezafibrate in mice and rats.
Subject(s)
Hypoglycemic Agents/chemical synthesis , Piperidines/chemistry , Propionates/chemical synthesis , Animals , Disease Models, Animal , Hypercholesterolemia/drug therapy , Hypertriglyceridemia/drug therapy , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/therapeutic use , Hypolipidemic Agents/chemical synthesis , Hypolipidemic Agents/chemistry , Hypolipidemic Agents/therapeutic use , Male , Mice , Mice, Inbred ICR , Piperazine , Piperazines/chemistry , Propionates/chemistry , Propionates/therapeutic use , Rats , Rats, Sprague-DawleyABSTRACT
Most everyone is well versed about what's happening in Washington and probably in his or her own state capital regarding healthcare reform, but what's happening at the grassroots level--with docs in the trenches? Just how has all the turmoil affected you, your practice, your patients, and your future plans? The answers are surely as varied as the number of physicians reading these words. We interviewed four physicians from different areas and practice settings to get their answers and impressions. Participants were Barton J. Romanek, MD, of Lockhart, Texas; Timothy S. Komoto, MD, of Minneapolis; Dominic B. Brune, MD, of Zanesville, Ohio; and Philip P. Bonanni, MD, of Rochester, New York.
Subject(s)
Health Care Reform/trends , Practice Management, Medical , Public Opinion , Forecasting , Insurance, Physician Services , United StatesABSTRACT
Forty patients underwent coronary revascularization using bilateral internal thoracic artery (ITA) grafts between 1988 and 1992. A total of 111 coronary grafts were performed, or an average of 2.8 grafts per patient. Each patient received bilateral ITA grafts, and in 20 patients an additional 29 grafts were constructed with 18 autologous veins and 11 gastroepiploic arteries. The right ITA was grafted as a free graft in 20 patients. The ITA graft patency rate was 96 per cent (67/70) at the time of hospital discharge. The operative morbidity included 3 reoperations for bleeding, 1 perioperative myocardial infarction, 1 renal failure, 2 postcardiotomy shock, and 1 colon perforation. Two hospital deaths occurred; one due to colon perforation and the other due to postcardiotomy cardiogenic shock. One patient died of cerebral infarction 6 month after the operation. Thirty-four patients were in New York Heart Association functional class I, 2 were in class II and 1 was in class III. Cardiac function evaluated by echocardiography and scintigraphy showed significant improvement postoperatively. These data suggest that the use of bilateral ITA grafts is associated with an acceptable mortality and increases the versatility of arterial grafting.
Subject(s)
Coronary Artery Bypass/methods , Thoracic Arteries/transplantation , Aged , Coronary Artery Bypass/mortality , Female , Follow-Up Studies , Heart/physiopathology , Humans , Male , Middle Aged , Postoperative Complications , Survival RateABSTRACT
A 58-year-old woman who could not be weaned from cardiopulmonary bypass was treated with a biventricular assist device (BVAD) using a centrifugal pump for the left side and a pneumatic pulsatile pump for the right side. At the initiation of the BVAD support, predominant right ventricular failure was recognized and therefore weaning was begun from the left side. The left ventricular assist device was discontinued after 87 h and the patient was finally weaned from the right ventricular assist device after 205 h. Despite the complete recovery of cardiac function, the patient developed renal failure followed by an intractable infection and died of multiple organ failure on the 59th postoperative day (POD).
Subject(s)
Cardiac Output, Low/therapy , Heart-Assist Devices , Postoperative Complications/therapy , Aortic Valve/surgery , Blood Coagulation Factors/analysis , Blood Pressure , Cardiac Output , Cardiac Output, Low/blood , Cardiac Output, Low/physiopathology , Female , Heart Ventricles , Humans , Middle Aged , Mitral Valve/surgeryABSTRACT
In this study, the relationship among the chemical composition and the physical and chemical properties of four photo-cured composites and one heat curing composite for crown and bridge were investigated. Five composites were composed of the base monomer, UDMA, TriEGDMA, 1, 3-BDMA, 1, 4-BDMA, 1, 10-DDMA, 1, 12-DDDMA or those mixture, and the composite-filler consist of the resin (TMPTMA, UDMA, 1, 10-DDMA or 1, 12-DDDMA) and micro-silica particles. Four photo-curing composites had a high elastic modulus and Vickers hardness and a low thermal expansion coefficient and water sorption compared with the heat-cured composite (Is). The effects of filler contents in the composites examined were positively on the elastic modulus and the hardness, and were inversely on the bending strength and the thermal expansion coefficient of the cured products. While the organic phase in the composite fillers had effect on the abrasive resistance of the composites. But no significant correlation between the abrasive resistance and the filler contents and the physical properties of the materials tested was noted.
Subject(s)
Composite Resins , Crowns , Denture BasesABSTRACT
The purpose of this study is to clarify the superiority of five polyfunctional acrylates to composite filler and comonomer system, and the reasonable concentration of catalyst, Camphor quinone/Dimethylamino-ethylmethacrylate (CQ/DMAEMA), in the photocured resin for crown and bridge. The results are summarized as follows: 1. The influence of acrylate resin matrix of composite fillers was found in the elastic modulus (Em), Knoop hardness (Hk) and the wear resistance (Rw) of the photocured resin. Two photocured resins including Dipentaerythrytol hexaacrylate (DPHA) or DPHA-4(3-acryloxy propyl) tetramethylol methane (DPHA-APTM) composite fillers showed a higher Em, Hk and Rw but slightly lower tensile strength (Ts) and bending strength (Bs) than the one which included Bis-2-methacryloxyethyl 2, 2, 4-trymethyl hexamethylene diurethane (UDMA) or Trimethylolpropane trimethacrylate (TMPTMA) under a wet condition. And these two resins showed as a high water sorption value (Ws) as that of the photocured resin of UDMA. 2. The conversion of polymerization, cured depth and physical properties (Em, Hk and Rw) of the photocured resins were examined. They increased up to 0.5/1.0 or 1.0/1.0 in proportion to the increase of the concentration of the catalysts (CQ/DMAEMA). 3. When DPHA was added into the photocured resins consisted with UDMA monomer and DPHA or DPHA-APTM composite fillers, these resins showed a higher Em, Hk and Rw than the photocured resin with only UDMA as monomer. No significant difference of Ts and Bs between the photocured resins with and without DPHA was observed under a dry condition, but the values of Ts and Bs decreased in proportion to the increase of DPHA monomer under the wet condition. The residual monomer of the photocured resins was less than 1.2 per cent.
