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At least 415 records · Page 23Linked to original sources
PubMed1978

Effect of cicloxilic acid on the bile lipid composition in cholelithiasis.

5 patient with cholesterol gallstones were treated with cis-2-hydroxy-2-penyl-cyclohexanecarboxilic acid (cicloxilic acid) 240 mg daily for one year. Before treatment and after 1 month's, 3 months' and 1 year's treatment gallbladder bile was withdrawn by duodenal tube after i.v. cerulein stimulation. The bile was assayed for lipids and the lithogenic index was determined. The pool of bile acids was also determined and liver function tests performed. The results show a gradual lowering of the mean lithogenic index in the course of treatment. The blood chemistry values remained within strictly normal limits.

Adult↗
PubMed1982

Cardiovascular effects of GABA, GABA-aminotransferase inhibitors and valproic acid following systemic administration in rats, cats and dogs: pharmacological approach to localize the site of action.

The cardiovascular effects of GABA, sodium valproate (VPA) and inhibitors of GABA-aminotransferase (GABA-T), namely aminooxyacetic acid, gabaculine, gamma-acetylenic GABA, gamma-vinyl GABA and ethanolamine-O-sulphate (EOS), were studied in anesthetized rats, cats and dogs. All compounds were administered intravenously in dose levels previously shown as anticonvulsant active. In rats and cats, GABA (100-1000 mg/kg) caused a sustained fall of blood pressure and heart rate. A similar reaction was observed in dogs following maintenance infusion of the amino acid. The prolonged cardiovascular depression in response to GABA could be attenuated by subsequent administration of picrotoxin and bicuculline as well as by alpha-methyltyrosine, corynanthine, chlorpromazine and tripelennamine. Phentolamine, yohimbine, propranolol, vagotomy, atropine, cyproheptadine, apomorphine and haloperidol did not antagonize the cardiovascular effects of GABA. Administration of GABA-T inhibitors provoked prolonged hypotension and bradycardia, which could be partially counteracted by picrotoxin, bicuculline and, except in the case of EOS, by chlorpromazine. VPA, in high doses (300-400 mg/kg) exerted similar cardiovascular effects in rats as observed with GABA and GABA-T inhibitors. The prolonged cardiovascular depression caused by VPA could be counteracted by bicuculline and partially by chlorpromazine. Apomorphine led to a considerable potentiation of the effects of VPA. It is concluded that GABA, GABA-T inhibitors and VPA may induce cardiovascular depression at least in part by activation of GABA receptors and that the response is mediated predominantly by the central adrenergic system. Some indication was found that an interaction with peripheral histamine contributes to the cardiovascular effects of GABA.

4-Aminobutyrate Transaminase↗
PubMed1975

Plasminogen-plasmin system IX. Specific binding of tranexamic acid to plasmin.

Interactions between tranexamic acid and protein were studied in respect of the antifibrinolytic actions of tranexamic acid. Tranexamic acid did neither show any interaction with fibrinogen or fibrin, nor was incorporated into cross-linked fibrin structure by the action of factor XIII. On the other hand, tranexamic acid bound to human plasmin with a dissociation constant of 3.5 X 10-5 M, which was very close to the inhibition constatn (3.6 X 10-5 M1 for this compound in inhibiting plasmin-induced fibrinolysis. The binding site of tranexamic acid on plasmin was not the catalytic site of plasmin, because TLCK-blocked plasmin also showed a similar affinity to tranexamic acid (the dissociation constant, 2.9-4.8 x 10-5m). in the binding studies with the highly purified plasminogen and TLCK-plasmin preparations which were obtained by affinity chromatography on lysine-substituted Sepharose, the molar binding ratio was shown to be 1.5-1.6 moles tranexamic acid per one mole protein. On the basis of these and other findings, a model for the inhibitory mechanism of tranexamic acid is presented.

Antifibrinolytic Agents↗
PubMed2005

Self-assembled peptide tubelets with 7 A pores.

Here we report the preparation and structural characteristics of self-assembling peptide tubelets composed of 32-membered rings formed of alternating alpha-amino acids and cis-3-aminocyclohexanecarboxylic acids. The tubelets possess a partial hydrophobic core environment, provided by the projection of the cyclohexane C2 methylene moiety into the lumen, and a Van der Waals pore diameter of about 7 A.

Amino Acids↗
PubMed1983

Aurintricarboxilic acid as a tool for investigating the template-bound and unbound forms of RNA polymerase I in permeabilized cells.

The presence of template-bound and unbound RNA polymerase I in permeabilized cells was investigated. The two enzyme forms were defined on the basis of their different susceptibilities towards aurintricarboxilic acid (ATA). It was found that addition of ATA to permeabilized cells suppresses initiation of new RNA chains by RNA polymerase I but has no effect on the activity of the enzyme already engaged in transcription. This last activity is not affected even after washing the permeabilized cells for removal of the ATA. The RNA polymerase I activity solubilized from permeabilized cells pre-treated with ATA is 60-70% of that obtained from non-treated controls. The decrease of the solubilized enzyme activity was observed after purification of the enzymes by DEAE-Sephadex columns and cannot be attributed to the presence of inhibitory or activating factors in the enzyme preparations. The simplest interpretation of these findings is that two distinct RNA polymerase I fractions, showing different sensitivities towards ATA are present in permeabilized cells. These fractions should represent the template-bound and unbound RNA polymerase I. The results also show that the amount of ATA-insensitive activity is lower in nuclei than in permeabilized cells, suggesting that detachment of template-bound enzyme occurs during nuclei isolation.

Animals↗