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[Experimental study of the embryotropic effects of various calcium compounds after peroral administration].

The ion form as calcium bicarbonate appeared to be most favourable for the correction of mineral distillate content with various calcium compounds. An organocomplex compound--calcium lactate can not be considered as an adequate model for the scientific substantiation of hygienic standards for calcium content in drinking water. Completely demineralized water consumed perorally gives a negative embryotropic effect.

Animals

Permanent stained preparations of synovial fluid for detection of calcium compounds using alizarin red S.

Permanent preparations of air dried synovial fluids were prepared by staining calcium compounds with alizarin red S stain; each slide was coverslipped with Permount. Variables studied were: (a) concentration of the solution of alizarin red S, (b) pH of staining solution, (c) time of incubation in staining solution and aqueous and ethanolic content of staining solution. The staining effect of each solution was tested on calcium pyrophosphate dihydrate, calcium oxalate, apatite and monosodium urate (MSU). Of all the solutions, best results were obtained with 0.25% alizarin red S in 50% ethanol at pH 7.0 for 30 min. With this solution, the calcium-containing compounds were well stained. MSU did not stain and still preserved negative birefringence on polarization. Fixation of smears with ethanol served a double purpose: It fixed the slides without dissolving or removing MSU or the calcium compounds, yet it did dissolve five corticosteroids commonly used for intra-articular injection which may interfere with interpretation of compensated polarized light microscopy of synovial fluids.

Anthraquinones

The alkalizing properties of calcium hydroxide compounds.

Calcium hydroxide compounds are available in various forms, such as in aqueous suspensions or as cements, liners, pastes or filled resins. When such compounds are exposed to water, the calcium hydroxide dissociates and the pH value shifts to the basic. In this study the compounds Pulpdent, Dycal, Hydroxyline, Gangraena Merz and Prisma VLC-Dycal were subjected to analysis, including quantitative measurement of the amount and the chronological course of ion release following exposure to water, qualitative analysis of the alkalizing effects at the dentin surface and examination of antimicrobial properties. The results showed that calcium hydroxide compounds differed greatly. The strongest degree of ion release, combined with definite antimicrobial properties, was found for the aqueous calcium hydroxide suspension (Pulpdent). The cement (Dycal) demonstrated significantly weaker activity. The liner and the paste (Hydroxyline and Gangraena Merz), as well as the calcium hydroxide filled resin (Prisma VLC-Dycal), were largely lacking in both ion release and antimicrobial properties under the experimental conditions.

Calcium Hydroxide

The effects of HA compound calcium antagonists on delayed cerebral vasospasm in dogs.

The authors have examined the effects of the HA compounds HA1004(N-(2-guanidinoethyl)-5-isoquinolinesulfonamide) and HA 1077(1-(5-isoquinolinesulfonyl)homopiperazine), which are intracellular calcium antagonists, on delayed cerebral vasospasm from subarachnoid hemorrhage (SAH). The modes of action of these compounds were compared with those of the more commonly used calcium entry blockers. Calcium ionophore A23187 (4.8 X 10(-6) M)-induced contraction of a canine basilar artery strip was completely antagonized by the HA compounds (10(-5) M) but not by the entry-blocking calcium antagonists nicardipine, diltiazem, and verapamil (10(-5) M), suggesting that the HA compounds act differently. Delayed cerebral vasospasm was induced by a "two-hemorrhage" canine model. The magnitude of the vasospasm and the effects of the HA compounds were determined angiographically. On SAH Day 7, a significant vasospasm was observed in every dog. The diameter of the basilar artery had diminished to 59% +/- 2% (mean +/- standard error) of the control value obtained before SAH (on Day 1). The intravenous administration of HA 1004 caused a mild dilation of the basilar artery of 10% and 11% at doses of 3 and 10 mg/kg, respectively; however, HA 1077 produced a more marked dilation of 19% and 27%, respectively, at the same doses. Both of these drugs lowered mean arterial blood pressure to about 80% and 50% at doses of 3 and 10 mg/kg, respectively. Intracisternal administration of the HA compounds (6 mg) completely reversed cerebral vasospasm without much effect on the blood pressure. The intracellular calcium antagonists of the HA compound group appear to be promising agents for the treatment of intractable cerebral vasospasm.

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine

[Differential staining of calcium compounds in histologic sections].

An experimental protocol is proposed for the differentiation of calcium-hydrogen-phosphate, tri-calcium-phosphate, calcium-oxalate, calcium-urate and fatty acidic calcium. For tissue fixation calcium acetate-formaldehyde is recommended in which fatty acids and earth-metal urates form insoluble calcium-salts which can be demonstrated in paraffin sections.

Animals

Alizarin red S staining as a screening test to detect calcium compounds in synovial fluid.

A simple, rapid screening method using alizarin red S stain and ordinary light microscopy to detect microcrystalline or noncrystalline calcium phosphate salts was used on wet drop preparations of synovial fluids. This proved to be helpful in detecting apatite crystal clumps and small calcium pyrophosphate dihydrate (CPPD) crystals missed by polarized light. The staining was positive in 100% of synovial fluids from patients later proven to have apatite and/or CPPD deposition diseases. Apatite and CPPD crystals were commonly found together in the same fluids. In addition, some synovial fluids from patients with osteoarthritis, renal failure dialysis, rheumatoid arthritis, and gout also exhibited positive staining. The correlation of positive alizarin red S staining with radiologic evidence of osteoarthritis suggests that apatite crystals might be related to articular cartilage degeneration in different rheumatic diseases.

Anthraquinones

Physicochemical, pharmacological and pharmacokinetic study of a new GABAergic compound, calcium acetylhomotaurinate.

It has been shown that calcium acetylhomotaurinate (Ca AOTA; Meram Patent, France) decreased voluntary ethanol intake in rats (1); this was antagonized by bicuculline. Homotaurine did not have this effect. We thought this was due to a different blood-brain barrier crossing ability for the two drugs. The present study was, therefore, planned to confirm blood-barrier crossing by Ca AOTA and to study the drug's physicochemical and pharmacokinetic characteristics. Both in vitro and in vivo (i.p.) administration of Ca AOTA increased the accumulation of [3H] GABA in rat striatal synaptosomal preparations. The chemical study confirmed Ca AOTA's great stability in biological and hydrophilic media, excluding a "homotaurine-dispensing" effect. The molecule was totally dissociated in such media, but the absence of any detectable acid form at any pH indicates that ion pairs are formed to cross barriers, and/or that a carrier system is used. The pharmacokinetic study showed short half-lives (5 and 30 min for the distribution and elimination phases) and small distribution volumes. However, the elimination phase distribution volume was dose-dependent, a further argument for a carrier transport system. From the present study it appears that Ca AOTA is an extremely stable drug, totally dissociated in hydrophilic media, which acts centrally as a GABA agonist after crossing the blood-brain barrier. It is not a precursor of homotaurine and presumably crosses barriers with the help of a transporter.

Acamprosate

Modulation of ileal calcium transport by phosphate-exchanging compounds.

Calcium transport in the ileal-ligated loop was studied in the adult rat in the presence of either phosphate alone or phosphate-binding compounds, namely either hydroxylated or aminated substances. Sorbitol or creatine (50 mM) added to a 10-mM CaCl2 solution, which was instilled into ileal loop, markedly enhanced calcium transport, as determined by 45Ca radioactivity appearing in plasma and from 45Ca radioactivity disappearing from the loop. The presence of both compounds maintained Ca soluble in an instilled solution at a constant concentration, whereas with a control solution the Ca concentration progressively decreased towards zero after an incubation period of 60 min. Phosphate, which was either simultaneously added with sorbitol or creatine or which was present as sorbitol or creatine phosphate, led to an equally marked decrease in calcium transport. Calcium transfer was even more reduced when phosphate alone was present with calcium in the ileal loop, in the absence of sorbitol. Similar to the above phosphate-binding compounds, adenosine and its constitutive component, ribose, increased calcium transfer, whereas adenine, the other constitutive component of adenosine, was ineffective. Guanosine was twice more active than adenosine in stimulating ileal calcium transport. Interestingly, the structure of guanosine allows the binding of two phosphates, with one binding site being on the ribose and the other on the guanine base moiety. Thus guanosine is capable of binding a greater amount of phosphate than the two other aminated compounds examined, namely adenosine and alanine, when transphosphorylation from ATP is studied with intestinal microvilli preparations.(ABSTRACT TRUNCATED AT 250 WORDS)

Adenosine