New uracils as anticonvulsants & their monamine oxidase & succinate dehydrogenase inhibitory activity.
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Biomedical subjects
Publications and source records attributed to R C Gupta.
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The effect of daily dermal spray of malathion for four weeks in recommended (0.5 and 1.0 per cent) and higher (5.0 per cent) concentration on various enzymes in Bubalus bubalis species were studied. The higher concentration of 5.0 per cent showed lethal effect after 2 to 3 exposures. The cholinesterase activity in both RBC (RChE) and plasma (PChE) were inhibited with all the concentrations. There was also significant (P less than 0.05) elevation in the activities of serum aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase with 1.0 and 5.0 per cent spray and enzyme activities remained altered even during post-medication. The extent of various biochemical changes were dose and time dependent.
An oral dose of 0.5 mg/kg/day malathion continuously administered for one year has been investigated to produce no change in biochemical (RChE, PChE, aspartate- and alanine aminotransferases, blood glucose, serum urea and plasma total proteins) or haematological (Hb, PCV, tRBC and tWBC) parameters and, therefore, considered to be "no-effect-level" in Bubalus bubalis. However, the administration of higher doses (1.0 and 1.5 mg/kg/day) produced significant (P less than 0.05) changes in all biochemical parameters studied. With these doses leucocytosis was evident among haematological parameters measured.
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The significance of osteomedullography was studied in 17 patients with diaphyseal fractures of long bones to determine a rational form of treatment for delayed healing and non-union. Positive osteomedullographic signs were noted in 6 cases of delayed healing and negative signs in 11 cases. All the positive cases united by prolonging the period of immobilization in plaster. Seven of the 11 negative cases were treated by bone grafting. Three patients treated by prolonged immobilization in plaster have not shown evidence of union even after a period of 20 weeks. This simple investigation could be useful in avoiding undue loss of time in the management of delayed union and non-union.
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The case history of a 45-year-old female patient who sustained a fracture of the right navicular sesamoid bone, probably due to sudden stretching of the tibialis posterior muscle, is described, and the literature briefly reviewed.
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We have found that, although the binding of particulate antigen-antibody complement complexes such as EAC to lymphoblastoid Raji cells is mediated largely through receptors for C3b, the binding of complement-containing soluble complexes such as those prepared with aggregated human IgG (AHG) occurs also via receptors for C1q. Evidence supporting this conclusion included: (1) Binding of AHG to Raji cells takes place after incubation in EDTA serum; (2) Binding of AHG does not occur in C1q deficient EDTA serum but does take place after addition of C1q; (3) The extent of binding of AHG in EDTA serum is a function of the amount of C1q present; (4) Raji cells can bind up to 5-4 times 10(5) molecules of 125I C1q per cell which can be blocked by unlabelled C1q; (5) AHG pre-incubated with C can bind to a T-cell line MOLT, which lacks receptors for C3b but possesses receptors for C1q to the same extent as Raji cells; (6) Immunoassays for immune complexes in human sera yield similar results whether Raji cells, MOLT cells or C1q precipitation is used for assay; (7) EAC-Raji cell rosettes can be inhibited with inulin-treated, C1q deficient serum containing C3b or C3d whereas binding of AHG or immune complexes in patient samples to Raji or MOLT cells is not inhibited by this reagent. We conclude that receptors for C1q on certain B and T lymphocytes may play an important role in physiologic functions of lymphocytes depending on binding of soluble immune complexes to their surfaces.
The synthesis and pharmacological activity of some 3-tertiary amino-1-aryloxy- or 1-aryl-, 1-thiophenoxy and 1-anilino-propan-2-ols and -propanes, particularly those derived from N-phenylpiperazines are described. Effect of substituents (nature/position) on the phenyl ring, the phenoxy ring as well as alteration in the hydroxylic function vis-à-vis the structure-activity relationships (SAR) are discussed. In general, the 1-aryloxy compounds have hypotensive activity--this being more pronounced in those carrying an o-substituent on the phenyl ring, while m and p-substituted derivatives have their effect primarily on the CNS. Variations in the phenoxy moiety do not significantly alter the intrinsic activity. The 1-aryl compounds, on the other hand, have significant CNS activity, which is markedly affected by the substituents on the 1-aryl residue.
In a study of the usefulness of two widely performed tests for immune complexes (IC) in the assessment of disease activity of lupus nephritis the Raji cell assay detected IC in sera of 14 of 32 patients and the monoclonal rheumatoid factor (MRF) test in only five. There was a close correlation of levels of IC with number of organ systems showing disease activity and with serum complement levels and a somewhat less significant correlation with serum levels of anti-DNA. Although in a few patients levels of IC closely paralleled improvement in renal function with treatment, there was no overall correlation of changes of levels of IC with changes in creatinine clearance. Measurement of circulating IC in lupus nephritis cannot at present be justified as a worthwhile clinical measurement in the management of such patients.
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As epidurography uses a water-soluble contrast medium in the diagnosis of disc lesions, this procedure can be repeated, unlike conventional myelography which uses an oily contrast medium. Successful employment of epidurography before and after traction in 14 cases of adult prolapsed intervertebral disc syndrome is described.
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Levels of immune complexes (IC) were determined by the Raji-cell and C1q-binding radioimmunoassays in the sera of eighteen patients with Behçet's disease. Eight patients (44%) were found to have significantly elevated levels of IC (range 56 to 1600 microgram equivalent aliquots of heat aggregated IgG (AHG/ml) by the former test and nine by the latter (7 to 500 microgram equivalent AHG/ml). The presence of IC showed a significant correlation with disease activity score (P = 0.003, Mann-Whitney Rank Sum Test). Abnormal values of IC tended to remain abnormal when sera were retested after 1 year. There was no correlation between IC and duration of disease or any specific organ involvement. The IC were found predominantly in fractions of about 19S and greater when fractionated by sucrose density gradient or Sephadex column techniques. The results suggest the possibility that IC may contribute to the pathophysiology of Behçet's disease.