7-Arylidenenaltrexones as selective delta1 opioid receptor antagonists

A series of 7-arylidinenaltrexones (2a-m) related to the prototypical delta1-selective antagonist, 7-benzylidenenaltrexone 1 (BNTX), have been synthesized in an effort to develop more selective ligands. Testing in smooth muscle preparations revealed that members of the series exhibited varying degrees of selectively for delta receptors, with the o-methoxy (2e) and o-chloro (2j) congeners being most potent and most selective (Ke approximately 0.8 nm). Evaluation of 1, 2e, and 2f sc in mice using the tail-flick procedure indicated that they are selective delta1 opioid receptor antagonists in the lower dose range. At high doses these ligands, including BNTX, exhibited decreased delta1 selectivity due to increases in the ED50 ratios of [D-Ser2,Leu5]enkephalin-Thr6 and morphine. It is concluded that 2e and 2f possess in vivo selectivity similar to that of BNTX, but are less potent as delta1 antagonists.     

A clinicopathological study on the papillary muscle dysfunction

A total of 11 cases of papillary muscle dysfunction (PMD) was found among 600 consecutive autopsy (1.8%). There were 5 men and 6 women, with their ages ranging from 64 to 92 years. Auscultation and phonocardiograms revealed holosystolic murmurs in 9 cases and early systolic murmurs in 2. There were accentuated 1st sound in 8 cases, 3rd sound in 7, and 4th sound in 5. PMD was classified into 3 types according to the clinical course and pathologic examinations. In type A (6 cases), myocardial infarction (MI) preceded the occurence of mitral regurgitation (MR) by 3 or 4 years, with pathological verification of old MI. In type B (1 case), MR developed during acute MI. In type C (4 cases), pathological examinations disclosed various degrees of myocardial fibrosis, in which clinical diagnosis was MR of unknown etiology. In a total of 113 cases of MI, 36 cases (32%) showed papillary muscle infarction (PMI), which occurred with significantly high incidence in (1) male, (2) large MI, and (3) subendocardial or lateral MI. Among 36 cases of PMI, 9 cases developed PMD, which showed high incidence in inferior MI and in female. Various other factors concerning PMD and PMI were examined, and it was pointed out that not only PMI but also severe lesions in corresponding ventricular wall were necessary for the development of PMD.     

Notch effect on torsional fatigue of austenitic stainless steel: Comparison with low carbon steel

Notch effect in austenitic stainless steel under cyclic torsion is quite different depending on the superposition of static tension. In pure torsion, the rubbing of the serrated factory-roof type crack faces delays the crack growth along the notch root. Thus, the lifetime in notched specimen becomes longer than in smooth specimen. However, in cyclic torsion with static tension, the flat crack path and mean tensile stress reduce the influence of the crack face contact. Accordingly, shorter lifetime resulted from higher strain concentration at the notch root. Crack growth in low carbon steel under cyclic torsion is highly affected by the ferrite/pearlite banded microstructure besides the addition of static tension. Because of a small amount of the crack face contact, the reduction of lifetime in notched specimen is revealed irrespective of superposition of static tension.     

Morphological and functional factors predicting bladder deterioration after spinal cord injury

PURPOSE: We investigated factors predictive of morphological and functional deterioration of the bladder in patients with spinal cord injury. MATERIALS AND METHODS: Urological evaluation, including excretory urography and urodynamic studies, was performed once a year in 66 patients. Bladder compliance was used as an index of bladder function. RESULTS: Mean age of the patients with worsening bladder form and function was significantly greater than that of those with no change. In patients with worsening bladder function intermittent catheterization was performed less frequently and mean catheterization volume was greater compared to those with improvement and no change. Catheterization was less frequent and at long intervals in patients with a high urethral closure pressure. CONCLUSIONS: High storage pressure due to a high urethral closure pressure is believed to cause deterioration of bladder form and function.     

Markedly increased accumulation of Tc-99m DTPA in a patient with neurofibromatosis

A key issue in nucleic acid-based assays related to infectious disease testing and genetic testing is the sample preparation. This has to be convenient, efficient and suitable for automation. We describe a new method based on the use of glass magnetic particles. The steps involved are the lysis of bacterial cells and viral particles by chaotropic salts, binding of released nucleic acids to the magnetic glass particles, the removal of inhibitors and the release of purified nucleic acids ready for PCR amplification. The method fulfills most of the requirements for sample preparation such as sensitivity, universality and suitability for automation.     

Difference in immunologic responses between pancreatic and islet transplantation in "low responder" rat combinations with class I MHC disparity

Tricuspid pouch sometimes causes subpulmonary obstruction in association with transposition of the great arteries, but rarely does so without transposition. A 5-year-old girl with isolated ventricular septal defect exhibited dynamic right ventricular outflow tract obstruction caused by pouches in the anterior and septal tricuspid leaflets. Echocardiography clearly demonstrated features of the tricuspid pouches. Ventricular septal defect closure resulted in disappearance of the tricuspid pouches and resolution of subpulmonary obstruction.