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At least 145 records · Page 8Linked to original sources

PubMed1987

[Centrally and peripherally induced anorectic actions of salmon calcitonin (sCT) in rats: separation of its novel derivative [Gly8]-sCT].

It has been reported based on animal studies that salmon calcitonin (sCT), besides hypocalcemic action, exhibits a variety of pharmacological actions. The anorectic action has been observed to ensue not only by central administration but also by peripheral injection, indicating that in clinical use to induce hypocalcemia or for other therapeutic purposes, the anorectic action may develop as a side effect. While studying the anorectic effect of [Gly8]-sCT in rats, a derivative of sCT having rather stronger hypocalcemic potency than the mother molecule, it was found that on peripheral injection, the derivative practically lacks the anorectic effect. Thus, a pharmacological evaluation of the novel peptide was made. When injected subcutaneously in rats at a dose level of 1 U/kg, sCT and the derivative induced similar patterns of hypocalcemia in either of which hypocalcemia reached a peak between 1 and 3 hr after injection. No notable difference existed between the action of the two peptides. In rats which were trained to take the daily food need within 2 hr (17:00 approximately 19:00), an intracerebroventricular injection of 1 U/rat of either peptide 30 min before food presentation significantly reduced both food and water intake, causing a loss of body weight as compared with the control which received the injection of saline alone. By subcutaneous injection of 100 U/kg, sCT was also active to decrease food and water intake. The effect was found to last longer than 24 hr and to cause a marked loss in body weight. In contrast, such effects did not develop in rats treated with the derivative. Both peptides were able to suppress the specific binding of 125I-sCT to the membrane fraction of rat brain and kidney.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1988

[An analysis of the morbid condition in adjuvant arthritic rats and a new method for evaluating anti-rheumatic drugs].

The progress of various symptoms in adjuvant arthritic rats (AA-rats) and the effects of anti-rheumatic drugs were continuously observed on the basis of the Weibull distribution function, and the following results were obtained: 1) The cumulative incidence rates F(t) of various symptoms and abnormalities of measured values gradually increased with the passage of time. The relationship between the F(t) and the days after adjuvant injection indicated a simple Weibull distribution function. On the other hand, the bone damages in the distal limb joints indicated a composite Weibull distribution function with two shape parameters (m1 and m2). It was possible to classify the animals into two groups, fast responders (m1) and slow responders (m2), according to the time of occurrence of bone damages. 2) By using the Weibull probability paper, it was possible to integrate and to evaluate in totality those cases with varying grades of symptoms and cases with different symptoms in the adjuvant-induced syndrome in rats. 3) Azathioprine (AZP) showed an inhibitory effect on the advents of pain and swelling and functional disorders, while indomethacin (IDM), prednisolone (PSL) and gold sodium thiomalate (GST) delayed the advents of these symptoms. As to bone damages in the distal limb joints, IDM, PSL and AZP showed an inhibitory effect in only the fast responder group, while GST showed both an inhibitory and delaying effect in both the fast responder group and the slow one. The above results suggest that the usage of the Weibull distribution function is useful not only for analysis of the morbid condition of AA-rats but also for the evaluation of anti-rheumatic drugs in AA-rats.

Animals↗

PubMed1991

Key role of complement activation and platelet-activating factor in exudate formation in zymosan-induced rat pleurisy.

Involvement of complement and platelet-activating factor (PAF) in zymosan-induced rat pleurisy was examined. Only a very low level of complement remained in the exudate at 1-5 hr after zymosan injection, indicating that complement activation had occurred during this period in the pleural cavity. When rats were injected with cobra venom factor (CVF) 24 hr prior to the zymosan injection to deplete complement, the exudate volumes at 0.5 and 5 hr after zymosan injection were significantly reduced. Furthermore, combined treatment with CVF and CV-6209, an antagonist of PAF, also significantly suppressed the exudation but to no further extent than the suppression by CVF alone, suggesting that the level of complement depletion achieved was sufficient to halt PAF synthesis/release. To see if complement activation is involved in PAF production, we examined the PAF production by resident leukocytes in response to zymosan in vitro. When pleural leukocytes were stimulated with zymosan in the presence of rat serum, PAF-like activity both in the medium and in the cellular fraction increased. If the serum was heat inactivated, no PAF-like activity was detected. These results suggest that initial activation of the complement system may occur in the pleural cavity by zymosan and that the activated complement may then stimulate the production of PAF, which in turn elicits the exudate.

Animals↗

PubMed1979

High thyroid radiation dose associated with 131-I-19-iodocholesterol adrenal scanning.

We have examined two patients undergoing 131I-19-iodocholesterol adrenal scans in order to assess thyroidal radiation dose. Thyroid uptakes of 3--5% of the administered 2 mCi dose were found despite prior administration of Lugol's iodine. Analysis of serum samples over a ten day period after iodocholesterol injection indicated that less than 10% of the radioactivity was free iodide. Kinetic results showed a high value for the thyroid/plasma 131I ratio indicating thyroid retention of 131I. This was substantiated by thyroid scintigrams. The thyroid radiation dose was estimated to be 200--250 rad for the two patients. The associated carcinogenic risk is of sufficient magnitude, in our opinion, to warrant regular follow-up of all patients who have undergone 131I-19-iodocholesterol adrenal scanning.

19-Iodocholesterol↗

PubMed1990

Bioavailability of iron and cyanide from 59Fe- and 14C-labelled hexacyanoferrates(II) in rats.

"Soluble" (KFe(III)[Fe(II)(CN)6]) and "insoluble Prussian blue" (Fe(III)4[Fe(II)(CN)6]3 labelled with 59Fe either in the ferric (Fe(III)) or ferro (Fe(II)) position and 14C in the cyanide group were synthesized and administered intraperitoneally or orally to adult female rats with normal body iron stores. Following i.p. injection of KFe[Fe(CN)6], the colloidal complex is disintegrated into ferric iron and hexacyanoferrate(II) anion almost completely. About 96% of the ferric iron was retained in the body. Nearly 90% of both ferrous iron and cyanide were excreted with the urine within 7 days after i.p. injection, indicating that most of the undissociated hexacyanoferrate(II) anion ([Fe(CN)6]4-) was excreted through the kidney. Only 9% of the ferrous iron from [Fe(CN)6]4- was found mainly in carcass, liver and gut. As the 59Fe/14C-ratios in organs were found close to 1.0, the dissociation of the hexacyanoferrate(II) anion can only be small in vivo. No detectable 14CO2-activity (less than 0.01%) was monitored in the breath of rats after i.p. injection of the 14C-labelled KFe[Fe(CN)6], also indicating that no significant amounts of cyanide were released after parenteral administration. After oral administration of the soluble and insoluble Prussian blue, 0.3-0.7% of the ferric iron was absorbed and retained mainly in carcass, liver and blood. Only 0.06-0.18% of the ferrous iron was absorbed and mostly excreted with the urine (0.05-0.15%), so that only 0.01-0.03% of the oral ferrous 59Fe was retained in the body after 7-10 days. Very small fractions of 14C-label from the 14CN-group of the soluble and insoluble hexacyanoferrate(II) were observed in the exhaled air (0.04-0.08% of the oral dose). From the 14CO2-exhalation, the 14C-urine excretion and the distribution of iron in blood and organs it can be concluded that the hexacyanoferrate(II) moiety disintegrated only to a small extent in the intestinal tract after oral administration. From a dose of 36 mg hexacyanoferrate(II)/kg, an amount of free (non-complex bound) cyanide can be calculated which is in maximum two orders of magnitude below the LD100-level. Thus, the very low bioavailability of iron and cyanide from hexacyanoferrate(II) compounds after oral application is demonstrated in rats. In the case of a severe nuclear accident, appropriate doses of "soluble" and "insoluble" Prussian blue can be used as safe and effective antidote against radiocaesium contamination.

Animals↗

PubMed1985

Orbital decompression in endocrine exophthalmos of Graves' disease.

Transantral decompression was performed bilaterally in 27 and unilaterally in 3 patients with endocrine exophthalmos of Graves' disease. In 28 patients there was an immediate reduction of proptosis and in about half of the patients in addition a marked decrease in chemosis and conjunctival injection indicating that these signs were mostly due to orbital vascular congestion. In one patient with exophthalmos of more than 2 years duration and progressive swelling of the eye muscles no response was observed. In another patient decompression did not reduce proptosis which, however, 4 months later responded to retrobulbar irradiation. In one further patient much more marked reduction of proptosis and disappearance of persistent periorbital swellings were obtained after glucocorticoid treatment given half a year after decompression. Postoperatively diplopia occurred in about half of the patients but corrective operations were required only in a quarter of the patients. Transantral decompression is an effective method for rapid treatment of progressive exophthalmos of Graves' disease. In patients with unilateral exophthalmos the asymmetry may be reversed after unilateral operation. The authors use decompression not only in the most severe cases (categories 5 and 6a-c according to the classification of the American Thyroid Association) but also in less severe cases (categories 2b-c and 3b-c) when there is a steady progression as a primary treatment possibly combined with other forms of therapy.

Adult↗

PubMed1988

A review of the animal pharmacology of roxatidine acetate.

Roxatidine acetate (TZU 0460/HOE 760) [N-(3-[3-(1-piperidinylmethyl)-phenoxy]-propyl)acetoxyacetamide hydrochloride] is a specific and competitive H2-receptor antagonist with a chemical structure different from those of cimetidine, ranitidine and famotidine. Roxatidine acetate and its main metabolite roxatidine inhibit histamine-induced gastric acid secretion in vitro with a potency greater than that of cimetidine, and in the range of that produced by ranitidine. Gastric acid secretion following stimulation with dibutyryl cyclic adenosine monophosphate remains unaffected by roxatidine acetate. In vivo experiments in rats and dogs confirm these in vitro findings. Thus, in rats roxatidine acetate inhibits gastric acid secretion with similar values following intraduodenal or intraperitoneal injection, indicating excellent absorption of the drug from the gastrointestinal tract. In all studies it was shown that roxatidine acetate was more potent than cimetidine. In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies. Extensive general pharmacological studies with roxatidine acetate demonstrate the lack of effects on the central nervous system, on gastrointestinal motility, the autonomic nervous system and the cardiovascular and urogenital systems. Studies on the pharmacokinetics and metabolism of roxatidine acetate demonstrate that there is a presystemic deacetylation producing the main metabolite roxatidine, which is responsible for the in vivo effects of the drug.

Animals↗

PubMed1979

The efficacy of intra-articularly administered MYC 2095, triamcinolone hexacetonide and placebo in gonarthritis. A combined double-blind clinical trial.

We report the results of a double-blind three-centre study, employing a cross-over design, set up to compare the efficacy of intra-articular injections of Myc 2095 (20 mg), triamcinolone hexacetonide (Lederspan) (20 mg) and placebo in 40 patients with synovitis of the knee joint. Each patient included in the study contributed data on 2 of the 3 treatment variables being compared. Seven clinical parameters were assessed every 6 weeks, while the doctor's and the patient's assessments were scored. Intra articular treatment both with Myc 2095 and triamcinolone hexacetonide proved to be effective. Placebo response was also very high. After the first Myc 2095 injection, improvement in "tenderness", "pain under load" and "swelling and hydrops" was significantly superior to that following placebo treatment. The evaluation of the second injections indicated a marked carry-over effect from the first course. This was also evident from the doctor's and patient's assessments. The importance of including a placebo in the evaluation of anti-phlogistic drugs in clinical trials, emerged from this study.

Adult↗

PubMed1988

Chemonucleolysis for sciatica. A critical review.

Intradiscal injection of chymopapain for the treatment of sciatica due to disc herniation has been used for more than 25 years, but is still under debate. We review the indications, complications, and clinical results, and discuss the tissue effects of chymopapain. The results following surgical disc removal versus chymopapain injection indicate that surgery with removal of the disc hernia through a small laminotomy remains the documented treatment of choice for patients with proven disc herniation and sciatica in whom conservative treatment has failed.

Chymopapain↗

PubMed1985

Failure of injection of rat placental lactogen to inhibit prolactin in vivo.

In an attempt to demonstrate a negative feedback of rat placental lactogen (rPL) on prolactin secretion, pregnant rats were hysterectomized and injected intraperitoneally with placental extracts. Hysterectomy alone prolonged the incidence of nocturnal prolactin surges and injection of placental extracts did not alter this response. However, the absence of rPL in the serum following the injections indicated a primary reason why no inhibition was seen. Only when rPL was given intravenously was there detectable amounts found in the blood. The slow disappearance of rPL from the circulation following hysterectomy in Day 11 pregnant rats suggests that the lack of rPL in the blood following ip injection of placental extracts is not due to rapid clearance of rPL from blood. The failure to show a negative feedback of rPL on prolactin in vivo may be due primarily to the lack of appearance of rPL in the circulation following an ip injection of placental extracts.

Animals↗

PubMed1975

Thyroid metabolism in the recessive sex-linked dwarf female chicken. 3. The influence of exogenous thyroid hormones in glycogen metabolism.

The influence of exogenous thyroid hormones on glycogen-body and liver glycogen was studied in fasted and full-fed 3 wk. old dwarf and non-dwarf White Leghorn chickens. The results indicated that in contrast to normals, the glycogen-body of the dwarf was still physiologically active at age 3 wks. and they also exhibited a relatively higher liver glycogen concentration. The liver glycogen concentration was significantly higher in T3-treated, full-fed dwarf chickens when compared with other groups. The data were interpreted to suggest that the differential response observed in both dwarf and non-dwarf chickens of increasing liver glycogen levels with T3 and T4 injections indicated that the proper ratios of serum T3:T4 were probably more vital to the normal metabolic functions than changes in the individual concentrations of either T3 or T4.

Animals↗

PubMed1975

Relief of pain following upper abdominal operations by thoracic epidural block with etidocaine.

Bupivacaine and etidocaine were compared in 0.375% and 0.5% solutions (without adrenaline) in a double-blind study in thoracic epidural analgesia following upper abdominal surgery. Special regard was taken to duration and adequacy of analgesia and changes in motor function. Duration of analgesia was roughly comparable for all four solutions. Bupivacaine 0.375% and etidocaine 0.5% seemed to be appropriate concentrations for adequate pain relief. Motor function, as assessed by changes in FVC, FEV1 and PEFR was not influenced to any greater extent. A progressive fall in FVC with successive injections, indicating increasing motor weakness, did not occur.

Abdomen↗

PubMed1975

Lysosomal degradation of cell organelles. II. Ultrastructural analysis of uptake and digestion of intravenously injected microsomes and ribosomes by Kupffer cells.

Rough and smooth microsomes, "mixed" or total microsomes, and ribosomes were isolated from one single rat liver and subsequently injected intravenously into a series of inbred rats. The uptake and the degradation of the injected organelles by Kupffer cells were followed by means of electron microscopic analysis. By 1 minute after injection, microsomes were seen attached to the surface of Kupffer cells separated by a gap of 200 to 300 A. No attachment to hepatocytes, fat-storing cells, or endothelial cells was seen. By 5 and 10 minutes, most microsomes were phagocytosed and sequestered in large numbers within single membrane-enclosed vacuoles or phagosomes. The engulfment proceeded by two mechanisms: (1) most frequently, flaplike processes of cytoplasm embraced aggregates of microsomes, concomitant with the formation of indention of the cytoplasm; (2) occasionally, single microsomal profiles were taken up by bristle-coated endocytic vacuoles. Ribosomes were also seen penetrating into the wormlike structures (micropinocytosis vermiformis) at the cell surface. At 30 minutes after injection, clear signs of alteration were noted starting with vesicle aggregation, clumping, and elongation of the microsomal profiles. The ribosomes were quickly stripped from their microsomal membranes and marginated to the inside of the vacuoles but separated from the limiting membrane by a distance of 200 to 300 A. By 1 and 2 hours, disruption of the vesicles into membrane fragments and formation of dense material in and between the profiles occurred. By 8 hours it was difficult to recognize the degradation products as membrane derivatives. The digestive vacuoles retained their size at this time interval. Typical pentalaminar structures were observed. By 14 to 24 hours the digestive vacuoles became electron lucent and appeared to shrink, and in addition to containing various types of granular material, many were laden with lipid-like droplets presumed to be conglomerates of phospholipid remnants. Rough microsomes, when compared to smooth microsomes, gave rise to more granular material within the digestive vacuoles. Ribosomes were still identifiable 24 hours after injection, indicative of a somewhat slower rate of degradation. Accumulation of various types of lipid-like droplets in the "residual bodies" was typical after microsomal injections. It is concluded that although microsomes appear to be phagocytosed at a quicker rate than mitochondria, they are digested within the lysosomal apparatus of the Kupffer cells at a somewhat slower rate. This especially seems to be the case for ribosomes. Heterophagy of microsomes is one source of residual bodies.

Animals↗

PubMed1975

The matrix of the optic vesicle-presumptive lens interface during induction of the lens in the chicken embryo.

The cell coats of the presumptive lens cells and the extracellular interface between the lens rudiment and optic vesicle were investigated in the chicken embryo throughout the period during which lens induction is presumed to take place. Histochemical methods showed that the cell coats contained both glycoproteins and glycosaminoglycans. Autoradiography after [3H]glucosamine injection indicated incorporation of the precursor with subsequent localization primarily at the cell surface. No obvious changes in the properties of the coat were noted with the progression of early lens morphogenesis. The extracellular matrix at the interface between ectoderm and optic vesicle also contained glycoprotein and glycosaminoglycan. There was a heavy concentration of [3H]glucosamine-containing macromolecules in the area. Electron microscopy revealed that the interface consisted of the basement membrane systems of lens and optic vesicle, fused with their external fibrillar layers. In contrast to the findings on cell coats the density of the interfacial matrix increases appreciably during the lens induction period. Evidence suggests that the cells of the two ocular epithelia are themselves the source of the matrix materials. It is proposed that the macromolecules excreted by the epithelial cells into the interface interact at different concentrations to form aggregates of various structure by a process of self-assembly. This may be reflected in the different ultrastructure of the layers of the interfacial matrix. Quantitative changes in the density of the matrix, leading to increased adhesion between lens rudiment and optic vesicle, may restrict the lateral spreading of the lens cells and so fix the basal area of the lens rudiment. This, together with continued cell replication, may produce the cell crowding, placode formation and invagination characteristic of lens morphogenesis.

Amylases↗

PubMed1975

Plasma levels following administration of sodium meclofenamate by various routes.

Sodium meclofenamate, an anti-inflammatory and anti-anaphylactic agent, was administered to cattle intravenously, orally and by intraruminal injection. Plasma levels of the free drug were estimated fluorimetrically at intervals after administration by each route. Levels fell rapidly, particularly during the first hour after intravenous injection. Differences between those plasma levels resulting from oral administration and those following intraruminal injection indicated that direct passage into the abomasum was achieved by the former method. Simultaneous intravenous and intrauminal injections achieved immediate high plasma levels and maintained levels adequate for efficacy for 24 h.

Administration, Oral↗

PubMedDate not supplied

Evaluation of alkylated derivatives of 99mTc-propylene amine oxime (99mTc-PnAO).

Several lipophilic di-alkylated derivatives of propylene amine oxime (PnAO were complexed to 99mTc. Assessment of the 99mTc-PnAO derivatives included biodistribution and qualitative autoradiography. All of the derivatives studied penetrated the intact blood-brain-barrier, with the 99mTc-dibutyl-PnAO complex exhibiting the lowest initial brain uptake while the 99mTc-diethyl-PnAO and the 99mTc-dipropyl-PnAO complexes possessing nearly identical initial brain uptake as compared to 99mTcPnAO. Qualitative autoradiographs revealed significant loss of image resolution with extended time post injection indicative of rapid radiopharmaceutical washout. Although increasing alkyl chain length did not enhance initial brain uptake, the data demonstrates that limited modification of the PnAO ligand structure can be performed without decreasing cerebral uptake of the respective 99mTc complex.

Animals↗

PubMed1992

Individual molecular species of phosphatidylcholine and phosphatidylethanolamine in myelin turn over at different rates.

Phosphatidylcholine (PC) and phosphatidylethanolamine (PE) of the myelin membrane exhibit heterogeneity with respect to metabolic turnover rate (Miller, S. L., Benjamins, J. A., and Morell, P. (1977) J. Biol. Chem. 252, 4025-4037). To test the hypothesis that this is due to differential turnover of individual molecular species (which differ in acyl chain composition), we have examined the relative turnover of individual molecular species of myelin PC and PE. Phospholipids were labeled by injection of [2-3H]glycerol into the brains of young rats. Myelin was isolated at 1, 15, and 30 days post-injection, lipids were extracted, and phospholipid classes were separated by thin-layer chromatography. The PC and PE fractions were hydrolyzed with phospholipase C, and the resulting diacylglycerols were dinitrobenzoylated and fractionated by reverse-phase high performance liquid chromatography. The distribution of radioactivity among individual molecular species was determined. The labeled molecular species of myelin PC were 16:0-16:0, 16:0-18:0, 16:0-18:1, and 18:0-18:1, with most of the label present in 16:0-18:1 and 18:0-18:1. Changes in distribution of label with time after injection indicated that 16:0-18:1 turned over more rapidly than 18:0-18:1. The labeled molecular species of myelin PE were 18:0-20:4, 18:1-18:1, 16:0-18:1, 18:0-18:2, and 18:0-18:1. As with myelin PC, 16:0-18:1 (and 18:1-18:1) turned over more rapidly than 18:0-18:1. The relative turnover of individual molecular species of PC in the microsomal fraction from forebrain was also examined. The molecular species profile was different from myelin PC, but again, 16:0-18:1 turned over more rapidly than the other molecular species. Thus, within the same membrane, individual molecular species of a phospholipid class are metabolized at different rates. Comparison of our results with previous studies of turnover of molecular classes of phospholipids indicates that in addition to polar head group composition (Miller et al., 1977), fatty acid composition is very important in determining the metabolic fate of a phospholipid.

Animals↗

PubMed1992

The effects of intraocular gases on rabbit blood-retinal barrier permeability.

The effects of intravitreal expansile gases, sulfur hexafluoride and octafluoropropane, as well as air and needle insertion alone were assessed by iris fluorescein angiography and blood-retinal barrier permeability determination. Iris angiography, at 3 days after injection, indicated no differences between experimental and paired control eyes. Vitreous fluorophotometry on day 1, day 4 and day 7 after gas or sham injection also showed no differences between paired control and experimental eyes regardless of which experimental condition was employed. The results indicate that these gases are non-toxic to the blood-retinal barrier over a 7 day time course.

Animals↗