PubMed Health⌕ Search

Biomedical subjects

A Ray

Publications and source records attributed to A Ray.

At least 271 records · Page 15Linked to original sources

Autonomic regulation involved in the ocular hypotensive action of beta-adrenergic blocking agents.

The effects of racemic propranolol and some related drugs on the intraocular pressure (IOP) were studied after topical application in rabbits. These drugs produced a significant reduction in IOP with the following order of potency: (-)-propranolol greater than timolol greater than (+/-)-propranolol greater than sotalol greater than (+)-propranolol greater than pranolium. Pretreatment of rabbit eyes with atropine significantly antagonized the ocular hypotensive action of (+/-)-propranolol, timolol and pranolium. Both (+/-)-propranolol and timolol produced a significant increase in pupil diameter in the presence of a submydriatic dose of atropine. The activities of monoamine oxidase and carbonic anhydrase were unaffected by (+/-)-propranolol, timolol and pranolium in-vitro. It is concluded from the results that both cholinergic and adrenergic mechanisms may be involved in the ocular hypotensive effects of the drugs.

Adrenergic beta-Antagonists↗

Nonstereoselective aspects of propranolol pharmacodynamics.

Twenty years after its discovery, the beta-adrenergic blocking agent propranolol continues to interest pharmacologists and clinicians. Its therapeutic profile has extended to areas beyond the purview of the cardiovascular system, and its ocular and central nervous system effects have been well documented. In addition, it still remains a very good pharmacological tool to map out the adrenergic beta-receptors in the body, and stereoisomers of propranolol and other beta-blockers serve as valuable agents to distinguish between the effects related to beta-adrenoceptors and those which are not. The primary purpose of this review is to summarize the evidence indicating that beta-adrenergic blocking agents lack stereoselectivity in some of their effects, including several of considerable therapeutic importance. Because many pharmacological actions of propranolol followed a nonsteroselective pattern, the involvement of beta-adrenoceptors in them was questioned and this led to the search for alternate mechanisms to explain these effects. Studies with propranolol and some related drugs indicated the involvement of a cholinergic mechanism in their antiarrhythmic, ocular hypotensive and some central effects. Also, a presynaptic inhibitory effect at the skeletal neuromuscular junction has been suggested to explain the benefical effect of propranolol and other beta-blockers in tremor. Biochemical studies with these drugs revealed their inhibitory action on the cholinesterase enzyme in blood and other tissues like myocardium and brain. It is thus hypothesized that modulation of cholinergic neurotransmission by propranolol could explain some of its nonstereoselective actions and open new vistas in propranolol pharmacodynamics.

Animals↗

Effect of molecular size on the activity of adriamycin analogues: a quantitative structure-activity relationship study.

The in vitro anti-tumor activity (inhibition of human lymphoblastic leukemia cells) of some adriamycin analogues is found to be significantly correlated with the van Waals volume (VW) of the substituents. Activity is also found to be well correlated with first-order valence molecular connectivity index (1 chi V) but no correlation is found to exist between it and the hydrophobic parameter, log P (P: octanol-water partition coefficient). On the basis of these findings, it is suggested that the activity would be affected by the steric influence and to some extent by the electronic character of the substituents. From the correlating equations, it is observed that the size of C-7 glycoside ring and that of NHR2 group at its third position would greatly affect the activity. The size of C-14-R1 however, is not found to have much effect on the activity.

Antineoplastic Agents↗

Functional scanning electron microscopical observations on the oral roof in an air-breathing teleost, Clarias batrachus (LINN.).

Scanning Electron Microscopical (SEM) as well as light microscopical features of the oral roof including barbels of the air-breathing teleost, Clarias batrachus (LINN.) have been described in relation to its feeding habit. 3 distinct types of taste buds have been recorded for the first time in the barbels, lip, and in and around the teeth bearing suprapharyngeal teeth pad of the fish studied. The taste buds in the barbels and lip are elevated over the epithelium and confer wart like appearance which probably help in mechanoreception in addition to chemoreception. The taste buds in the suprapharyngeal teeth pad slightly rise above the epithelium whereas those in the borders of it do not. They also possess numerous minute papillae in the gustatory pores. These taste buds seem to act as chemoreceptors. SEM and light microscopical observations on the structure and distribution of taste buds in the oral roof clearly reveal that the fish is purely a taste-feeder and scans and gropes the food materials from the bottom of the pond.

Animals↗

Effect of medium hypertonicity on reovirus translation rates. An application of kinetic modeling in vivo.

Translation rates were determined for host and virus mRNAs in reovirus-infected SC-1 cells in hypertonic medium. The effect of low doses of cycloheximide on these translation rates was also measured. The results show that hypertonicity selectively stimulates viral translation relative to host translation. Moreover, in hypertonic medium, host translation is slightly stimulated by low doses of cycloheximide, whereas viral translation is markedly inhibited. This effect of cycloheximide is precisely the opposite to what was previously observed in isotonic media [Walden, W. E., Godefroy-Colburn, T., & Thach, R. E. (1981) J. Biol. Chem. 256, 11739-11746]. It is shown that both these effects of hypertonicity are predicted by the message competition/discrimination model previously described and thus provide support for the applicability of certain aspects of the model to translation rates in vivo.

Animals↗

Reversed-phase high-performance liquid chromatographic method for the assay of oxytetracycline.

The British Pharmacopoeia monograph for oxytetracycline calcium describes an high-performance liquid chromatographic (HPLC) assay which requires packing of the column by the analyst. Presented in this report is an HPLC method for the assay of oxytetracycline which employs a commercially available reversed-phase column and a solvent system which gives improved separation of the antibiotic from common impurities. Results obtained using this method for both bulk and dosage forms of oxytetracycline are in accord with the results of the microbiological assays.

Bacillus↗

Effect on mast cell histamine of inhibiting histamine formation in vivo with alpha-fluoromethylhistidine.

An irreversible inhibitor of histidine decarboxylase, alpha-fluoromethylhistidine (FMH), was used to inhibit histamine formation by mast cells in vivo. Even at doses of FMH sufficient to reduce histamine formation more than 95%, the ability of mast cells to synthesize histamine recovered rapidly. It was possible, however, to sustain levels of histamine-forming activity below 10% of normal with continuous administration of FMH from subcutaneously implanted osmotic pumps. Administration of FMH under these conditions did not deplete significantly mast cell histamine but did prevent the increase in total mast cell histamine that occurs over 14 days and also prevented the reconstitution of mast cell histamine stores after depletion by treatment with polymyxin B.

Animals↗

Effect of actinomycin-D on the fat body RNA content in Dysdercus koenigii (Heteroptera: Pyrrhocoridae).

The effect of actinomycin-D on the RNA content of the total fat body was studied on day 3, 4, 5 and 6 of the first reproductive cycle in the females. Actinomycin-D exhibited its highest inhibitory effect in insects injected on day 4 and a lower degree of the effect was seen in insects injected on day 5. These results suggest that by the end of day 4, a major quantity of DNA-dependent RNA, necessary for vitellogenin synthesis, has already been synthesised and accumulated.

Adipose Tissue↗

Cholinergic involvement in the modulation of oxotremorine-tremor in mice by propranolol.

Propranolol in low doses antagonized and in higher doses facilitated oxotremorine-induced tremor (Oxo-tremor) in mice. Atropine blocked Oxo-tremor, an effect that was reversed by propranolol. Atropine pretreatment also antagonized the potentiating effect of propranolol on Oxo-tremor. Propranolol inhibited mice brain cholinesterase at doses which enhanced Oxo-tremor. Timolol and sotalol produced a dose-dependent antagonism of Oxo-tremor, whereas practolol failed to produce a similar effect. None of these three agents produced any significant enhancement of Oxo-tremor. These results suggest the involvement of a peripheral mechanism for the antagonism and a central cholinergic mechanism for the facilitation of Oxo-tremor by propranolol.

Adrenergic beta-Antagonists↗

U1 small nuclear RNA-like sequences in human high molecular weight RNA.

Human U1 small nuclear RNA synthesis was shown earlier to be very sensitive to UV radiation. This led us to test for the possible presence of U1 RNA-like sequences in large RNAs. Human RNA was analyzed in gel blots hybridized with U1 DNA probes. A high molecular weight, heterodisperse RNA population was detected, which hybridizes both to a U1 RNA-coding region single-stranded DNA probe, and to a U1 gene fragment that contains only 6 nucleotides of flanking sequence. These large RNAs can be hybrid selected using immobilized U1 DNA, and have an average size of several kilobases. Additional observations support the claims that the high molecular weight RNA hybridization signal is not an aggregation artifact and that it is sequence specific.

Carcinoma↗

Cloning and analysis of pif, replication and leading regions of the F plasmid.

We describe the molecular cloning of BglII fragments of the hybrid plasmid pRS5 (pSC101 and EcoRI fragments of F; f7, f5, f3 and f6). The clones isolated were examined for the expression of F-specified replication, incompatibility, mobilization and inhibition of T7 bacteriophage multiplication. Proteins directed by the BglII clones were labelled in Escherichia coli K12 maxicells and analyzed by SDS-polyacrylamide gel electrophoresis. The sizes of previously reported proteins, encoded by the replication, incompatibility and leading regions encompassed by these plasmids have been confirmed in this study. In addition, the results demonstrate that a pif gene, which encodes an 80,000 dalton polypeptide essential for the inhibition T7 phage multiplication, is located on the BglII fragment that spans the junction of EcoRI fragments f7 and f5.

Bacterial Proteins↗

Molecular analysis of F plasmid pif region specifying abortive infection of T7 phage.

We report the molecular cloning of the pif region of the F plasmid and its physical dissection by subcloning and deletion analysis. Examination of the polypeptide products synthesized in maxicells by plasmids carrying defined pif sequences has shown that the region specifies at least two proteins of molecular weights 80,000 and 40,000, the genes for which appear to lie in the same transcriptional unit. In addition, analysis of pif-lacZ fusion plasmids has detected a pif promoter and determined the direction of transcription across the pif region.

Bacterial Proteins↗

Transcriptional analysis of the leading region in F plasmid DNA transfer.

Transcriptional activity associated with the leading region (53.8-66.7F) in F DNA transfer has been shown by RNA-DNA hybridization studies to occur on the anterior segment extending from 59.4 to 66.7F. Promoter-probe analysis of cloned leading region segments detected two promoters within the transcribed portion of the leading region. The promoter active across the 64.7F EcoRI site on the transferred F strand was associated with the expression of two polypeptides, 6d and 13.5p, located between 64.7-66.6F. However, no definite role could be ascribed to the second promoter operative through the 66.6F Bg/II site located in close proximity to oriT, the origin of transfer.

Bacterial Proteins↗

Stabilization of the cloning vector pACYC184 by insertion of F plasmid leading region sequences.

The leading region of the F plasmid is, by definition, the first part of the plasmid DNA to be transferred to the recipient cell during conjugation. Restriction fragments of the leading region, when cloned into the plasmid vector pACYC184, extended the maintenance of the normally unstable p15A-derived vector replicon in rec+ Escherichia coli K-12 cells. Mutations in the host's general recombination systems were found to influence the maintenance of these hybrid plasmids.

Base Sequence↗

Cloning and molecular analysis of the finO region from the antibiotic-resistance plasmid R6-5.

The cloning of the finO region from the antibiotic-resistance plasmid R6-5 is reported. On the basis of DNA deletion analysis and Tn5 transposon insertional mutagenesis of finO+ chimeric plasmids, finO has been located within the coordinates 94.0-94.85 on the R6-5 map. A 32,000-Da polypeptide (32K), which is encoded within 92.75-94.25R6-5, has been identified and shown not to be associated with the FinO phenotype.

Chromosome Mapping↗

Pyrimidine nucleotide metabolism in cardiac hypertrophy.

Cardiac hypertrophy was induced in rats either by isoprenaline treatment or by experimental abdominal aortic stenosis. In both models, the UTP content increased in the hypertrophying heart, while the ATP level remained depressed. The rate of net synthesis of uracil nucleotides, estimated by phosphate incorporation into alpha-phosphate groups, was largely increased during the first stage of hypertrophy (X 3.6 and 2.6, respectively). At identical stages of hypertrophy, the rate of synthesis of ribosomal RNA, measured after continuous intracardiac infusion of 3H-uridine, was increased by 1.6 and 2.5 times. A comparison of the changes in time course of the levels of UTP and RNA and their turnover suggests that the metabolism of uracil nucleotides and that of ribosomal RNA are closely interrelated. The increase in the rate of synthesis of pyrimidine is interpreted as an adaptational change in nucleotide metabolism in response to the increased requirement of precursors for RNA synthesis. The possible limiting role of pyrimidine nucleotides in the hypertrophic process is discussed.

Adenosine Triphosphate↗