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At least 415 records · Page 23Linked to original sources
PubMed1998

Dopamine D2-receptor density in humans as assessed with SPET and the new high-affinity ligand 123I-NCQ298: a pilot study.

Astra (S)-3-[123I]iodo-5,6-dimethoxyl-N-[(1-ethyl-2-pyrrolidinyl)methyl] -salicylamide (123I-NCQ298) is a new high-affinity D2-receptor ligand for use in single photon emission tomography (SPET) studies. We have studied the biodistribution and absorbed radiation dose of 123I-NCQ298 in humans. The mean effective dose for adults was 0.055 mSv MBq(-1). Brain uptake and clearance was measured with a head dedicated SPET camera. 123I-NCQ298 showed specific uptake in the basal ganglia with a low clearance rate (time constant of 9-34 h). The extrastriatal binding was variable (average 30%, maximum 60% of that in the basal ganglia at 1 h), but with a clearance rate twice that of the basal ganglia. The fairly high level of extrastriatal binding precluded the use of a quotient between the basal ganglia and cerebellum-to-frontal cortex 123I-NCQ298 concentration as a measure for basal ganglia D2-receptor density. Chronic schizophrenic patients treated with conventional neuroleptics had a decreased affinity for 123I-NCQ298 in the basal ganglia in the range 10-60% of the median value for the control, untreated subjects.

Adult↗
PubMed1982

Glucuronidation of morphine in human liver and interaction with oxazepam.

Morphine is primarily metabolized through glucuronidation by a microsomal UDP-glucuronyltransferase. With the use of 14C-morphine the activity of this enzyme was measured in hepatic microsomes from ten kidney transplant donors with total cerebral infarction and four icteric patients with pancreatic carcinoma. In the former livers the rate of glucuronidation varied from 1.08 to 8.67 nmol per mg microsomal protein per min, with a mean value of 3.83. These values were somewhat higher than in the liver biopsies from the four cancer patients. Oxazepam, at 1/10 the concentration of morphine, inhibited the morphine glucuronidation by 35%. The inhibition was competitive. Salicylamide also inhibited the morphine glucuronidation but only at concentrations considerably higher than morphine. The relevance of the in vitro data for the in vivo situation is unclear, since the concentrations employed in this study are several-fold higher than those encountered in the plasma of patients treated with these drugs.

Drug Interactions↗
PubMed1973

The effects of a new alpha- and beta-adrenoceptor antagonist (AH5158) upon the general and coronary haemodynamics of intact dogs.

AH5158, a salicylamide derivative, said to be a blocker of alpha- and beta-adrenoceptors, has been studied in intact anaesthetized dogs. At a dose of 2.5 mg/kg intravenously, the drug increased cardiac output and caused a late fall in mean systemic and pulmonary arterial pressure. Coronary sinus flow increased, as did cardiac oxygen extraction. External cardiac efficiency decreased. Blood glucose and non-esterified fatty acid values increased, but cardiac extraction of these did not change.

Adrenergic alpha-Antagonists↗
PubMed1995

Functional dopamine D2 receptors on rat vagal afferent neurones.

1. In the present study in vitro electrophysiology and receptor autoradiography were used to determine whether rat vagal afferent neurones possess dopamine D2 receptors. 2. Dopamine (10-300 microM) elicited a temperature- and concentration-dependent depolarization of the rat isolated nodose ganglion preparation. When applied to the tissue 15 min prior to agonist, raclopride (10 microM), clozapine (10 microM) or a mixture of raclopride and clozapine (10 microM each) all produced a threefold parallel shift to the right of the dopamine concentration-response curve. In contrast, SCH 23390 (100 nM), phentolamine and propranolol (1 microM each) failed to antagonize the dopamine-mediated depolarization. 3. [125I]-NCQ 298 (0.5 nM), a D2 selective radioligand, bound topographically to sections of rat brainstem. Densitometric quantification of autoradiograms revealed 93.8 +/- 0.5% specific binding of this salicylamide radioligand, as determined by raclopride (10 microM, n = 10 animals). Binding was highest in the nucleus tractus solitarius (NTS), particularly the medial and gelatinous subnuclei. In addition, specific binding was also observed in the interpolar spinal trigeminal nucleus and the inferior olive. 4. Unilateral nodose ganglionectomy caused a 36.6 +/- 3.0% reduction in specific binding in the denervated NTS compared to the contralateral NTS. Furthermore, the loss of binding was confined to the dorsal aspect of the medial subnucleus of the NTS. Sham surgery had no effect on the binding of [125I]-NCQ 298 in rat brainstem. 5. The present data provide evidence for the presence of functionally relevant dopamine D2 receptors on both the soma and central terminals of rat vagal afferent neurones. In addition, the majority of D2 receptors in the rat NTS appear to be located postsynaptically with respect to vagal terminals, and are presumably located either on ascending glossopharyngeal terminals, descending terminals from higher brain regions or on neuronal cell bodies within the NTS.

Afferent Pathways↗
PubMed1982

Renal glucuronidation of morphine in the human foetus.

The glucuronidation of morphine was investigated in kidney microsomes from human foetuses. This reaction was found to be catalyzed in all specimens investigated and the UDP-glucuronyltransferase activities varied between 0.18 and 0.30 nmol per min. per mg microsomal protein. Intraindividual comparisons with the hepatic glucuronidation rates revealed the renal enzyme rate to be about 50 percent of the hepatic. Oxazepam, and to a lesser extent salicylamide, inhibited the glucuronidation of morphine in kidney microsomes in similarity to what previously was shown in human foetal liver microsomes.

Female↗
PubMed1979

The interaction of ouabain and salicylate on sheep cardiac muscle.

1. The action potential duration in sheep ventricular fibres is rapidly diminished on exposure to 10(-6) M-ouabain. However, if 10--20 mM-sodium salicylate is added to the ouabain solution, glycoside-induced shortening is prevented, and a substantial increase in duration then occurs. Sodium salicylate also reverses the shortening effect of ouabain if applied after the glycoside has been allowed to act alone. 2. Sodium salicylate alone produces a much smaller prolongation than in the presence of ouabain. Alone and in the presence of ouabain it eventually increases the threshold and produces inexcitability. 3. Three other surface charge agents have been compared with salicylate: aminonaphthalene sulphonate, sodium dodecylsulphate and salicylamide, were unable to counter the actions of ouabain at the concentrations used. Since they also produced no changes in excitability it is likely that they did not bind significantly to the cell membrane. 4. In Purkinje fibres the reversal potential for the pacemaker current, iK2, is initially shifted in a negative direction in the presence of 10(-6) M-ouabain and 10 mM-salicylate instead of the positive shift expected with ouabain alone at this concentration. 5. In guinea-pig ventricle, salicylate alone reduces the duration of the action potential. This effect is rapidly reversible. Toxic levels of ouabain also reduce the action potential duration but this effect takes several hours to reverse. By contrast, the effects of salicylate and ouabain applied together are readily reversible. 6. It is suggested that the mechanism of these effects may depend on the ability of a surface negative charge agent like salicylate to increase the surface K+ concentration at the membrane and so protect the sodium-potassium pump from inhibition by large doses of ouabain.

Action Potentials↗
PubMed1982

Cortical-evoked potentials and saliva levels as basis for the comparison of pure analgesics to analgesic combinations.

Cortical-evoked potentials, pain ratings and thresholds of sensation were monitored after tooth pulp stimulation under the influence of marketed mixtures of analgesics. Simultaneously the saliva levels of the individual pharmacological active components of these mixtures were measured by high-performance thin-layer chromatography. The action of the mild analgesics in the mixtures was calculated from the linear correlations of changes in cortical-evoked potential with saliva levels of the analgesics. The ineffectiveness of low doses of salicylamide in the combinations was demonstrated by this method. None of the investigated combination products was superior to the same doses of either acetylsalicylic acid, paracetamol or phenazone.

Adult↗
PubMed1987

Metabolism of reverse triiodothyronine by isolated rat hepatocytes.

Reverse triiodothyronine (rT3) is metabolized predominantly by outer ring deiodination to 3,3'-diiodothyronine (3,3'-T2) in the liver. Metabolism of rT3 and 3,3'-T2 by isolated rat hepatocytes was analyzed by Sephadex LH-20 chromatography, high performance liquid chromatography, and radioimmunoassay, with closely agreeing results. Deiodinase activity was inhibited with propylthiouracil (PTU) and sulfotransferase activity by sulfate depletion or addition of salicylamide or dichloronitrophenol. Normally, little 3,3'-T2 production from rT3 was observed, and 125I- was the main product of both 3,[3'-125I]T2 and [3',5'-125I]rT3. PTU inhibited rT3 metabolism but did not affect 3,3'-T2 clearance as explained by accumulation of 3,3'-T2 sulfate. Inhibition of sulfation did not affect rT3 clearance but 3,3'-T2 metabolism was greatly diminished. The decrease in I- formation from rT3 was compensated by an increased recovery of 3,3'-T2 up to 70% of rT3 metabolized. In conclusion, significant production of 3,3'-T2 from rT3 by rat hepatocytes is only observed if further sulfation is inhibited.

Animals↗
PubMed1980

An improved colorimetric method for the determination of plasma paracetamol.

The commonly used nitration colorimetric method for urgent paracetamol estimation suffers from interference by salicylates and salicylamide. This communication describes a simple modification which eliminates this interference without affecting either the recovery or precision of the method. The results obtained were briefly compared with those obtained by an established gas chromatographic procedure.

Acetaminophen↗
PubMed1982

Effect of taurine on the gastric absorption of drugs: comparative studies with sodium lauryl sulfate.

In order to clarify the mechanism of taurine-induced enhancement of drug absorption, some comparison was made between the actions of taurine and sodium lauryl sulfate (SLS), an anionic surfactant, by using the loop of rat stomach in situ. SLS enhanced the gastric absorption of aspirin and salicylamide, and the SLS-induced enhancement seems to be Na+-dependent. SLS failed to enhance the absorption of both drugs when NaCl was completely replaced by mannitoL or in the presence of ouabain even in the NaCL medium. In addition, even at the lower concentration of 0.05 mM, SLS enhanced the absorption of the two drugs, the extent of which is nearly corresponding to those of taurine. The actions of SLS and taurine on drug absorption are considered to have some similar points. The mechanism of the action was discussed in relation to the cyclic AMP system.

Absorption↗
PubMed2004

Grinding-induced equimolar complex formation between thiourea and ethenzamide.

We prepared and characterized a grinding-induced equimolar complex of thiourea with ethenzamide. When thiourea and ethenzamide were co-ground at a molar ratio of 3 : 1, new powder X-ray diffraction (PXRD) peaks were observed in addition to PXRD peaks of thiourea crystals. The optimum stoichiometry of the new structure was confirmed as 1 : 1 mol/mol. Effect of grinding time on the thiourea-ethenzamide equimolar complex formation was investigated by using PXRD, differential scanning calorimetry and Fourier transform infrared spectroscopy. The equimolar crystal structure was confirmed by X-ray diffraction measurements of the single crystal which was recrystallized from ethanol. It was found that the intermolecular hydrogen bond formations between thiourea and ethenzamide molecules contributed to the equimolar complex formation. The complex formation was not observed in the cases where benzamide, salicylamide or 3-ethoxybenzamide was co-ground with thiourea. 2-Alcoxyl benzamide structures should be required for the grinding-induced equimolar complex formation with thiourea.

Salicylamides↗
PubMed1978

Studies on combination dosing (III). Aspirin and ethenzamide.

In our studies with drug combinations, we search for mixtures which would enhance the effectiveness of the related active substances. Ethenzamide was found to possess a specific suppressive effect on the gastric damage induced by aspirin. Such effect could not be demonstrated in analgesic agents such as salicylamide, bucetin, acetaminophen and phenacetin. The combination of aspirin with ethenzamide had a potentiating effect on analgesic activity and reduced motor incoordination and loss of righting reflex. We calculated the safety margins of various ratios of combinations and concluded that the best was aspirin and ethenzamide at a ratio of 2:3.

Analgesics↗
PubMed1989

Hypocalcemic action of the several types of salicylic acid analogues.

The present study was performed to see the structure-activity relationships on the aspirin-induced hypocalcemia. Several kinds of salicylic acid (SA) analogues administered orally with a stomach tube. In general, the drugs were suspended in the 2% CMC solution. At the scheduled times after the treatment, 60 microliters of the blood was collected to determine the level of calcium. Aspirin, sodium salt of o-hydroxybenzoic acid (Na-salicylate), sodium salt of m- and p-hydroxybenzoic acid (HBA), 2,5-dihydroxybenzoic acid (DHBA), PAS sodium dihydrate (PAS-Na), salicylamide (SAM) and 2% CMC control were used. Hypocalcemia was induced by aspirin and Na-salicylate but not by m- and p-HBA-Na. In addition, DHBA and PAS caused hypocalcemia when they were administered intravenously but not orally. These results suggest that the carboxyl group must be adjacent to the hydroxyl group on the benzene ring to induce this type of hypocalcemia and that the SA structure would be able to induce hypocalcemia, even in the presence of the additional third substituent on the same ring. On the comparison between aspirin-DL lysine (water soluble aspirin) and SA-DL lysine, SA-DL lysine, which is not an inhibitor of PG synthetase, was more effective on the hypocalcemic action than ASP-DL lysine. The phenomenon was observed at the stage especially immediately after intravenous injection, when the acetyl group may be more responsible to acetylate the PG synthetase in the aspirin-DL lysine group. The present results seems to be consistent with the previous hypothesis that PGs are not involved in the process of aspirin-induced hypocalcemia in the rat.

Animals↗
PubMed1980

Analgesic nephropathy induced by common proprietary mixtures.

Renal papillary necrosis has been induced in 36.4% to 75% of rats which were gavage-fed with analgesic mixtures containing proprietary combinations of aspirin, paracetamol, phenacetin, phenazone, salicylamide and caffeine. These findings support the recent recommendations of the National Health and Medical Research Council which suggest that the free availability of analgesic mixtures be restricted.

Acetaminophen↗
PubMed1976

Application of a vidicon spectrometer for simultaneous multicomponent drug determinations.

A rapid scanning vidicon spectrometer has been evaluated for the simultaneous determination of drugs in mixtures, without a separation step. Spectral data in the ultraviolet region are collected on-line with a small computer at repetition rates of 100 scans per second. Absorbance data at several wavelengths are processed by matrix equations to resolve them into the concentration of each component in each mixture. Results are reported for two-component mixtures of procainamide and N-acetylprocainamide in serum, for two-component aqueous mixtures of butabarbital and seconbarbital, and for seven-component aqueous mixtures of phenobarbital, diphenylhydantoin, aminophylline, acetaminophen, salicylamide, phenylbutazone, and secobarbital. We conclude that the computer-inter-faced vidicon spectrometer is a viable tool for simultaneous multicomponent determinations.

Acetaminophen↗
PubMedDate not supplied

In vitro released interferon-gamma in the diagnosis of drug-induced anaphylaxis.

A 17-year-old Japanese male was referred with acute urticaria and anaphylaxis after the administration of PL (salicylamide, acetaminophen, anhydrous caffeine and promethazine methylene disalicylate) and Bufferin (aspirin and dialminate) for headache and a high grade fever. The results of prick test, patch test and drug-induced lymphocyte stimulation test with PL and Bufferin were all negative. The patient's peripheral blood mononuclear cells (PBMC) were cultured with or without PL for 72 hours, and the activity of interferon-gamma (IFN-gamma) in the culture supernatant was measured with EIA. A significantly high level of IFN-gamma was detected in PBMC from the patient, but very little in those from healthy control subjects with a history of exposure to PL. This finding may indicate the presence of drug-specific IFN-gamma producing T cells in patients with an anaphylactic shock reaction to medication. Assays that measure the drug-induced IFN-gamma production may thus be a useful diagnostic tool not only for identifying delayed-type hypersensitivity (DTH) to drugs, but also for predicting anaphylactic shock reaction to drugs.

Acetaminophen↗
PubMedDate not supplied

The influence of anti-inflammatory drugs on the values of xylose test in man.

Anti-inflammatory drugs influence intestinal absorption. Acetylsalicylic acid, indomethacin, and PAS decrease significantly the values of xylose test in man. Paracetamol decreases the values of the test in two thirds of the subjects. Salicylamide, phenylbutazone, and sulfadimethoxine do not possess this action.

Acetaminophen↗
PubMed1975

Influence of adrenal dysfunction on activity and pharmacokinetics of some neutropic drugs. II. Influence of chronic premedication with dexamethasone on pharmacodynamic activity and pharmacokinetics of drugs.

The influence of long-term administration of dexamethasone on pharmacodynamic activity and biotransformation of salicylamide and hexobarbital, including their absorption, distribution and excretion, were studied. Activities of the following enzymes were also determined: beta-glucuronidase (E.C.3.2.1.31), uridinediphosphoglucose dehydrogenase (E.C.1.1.1.22), uridinediphosphoglucuronyl transferase (E.C.2.4.1.17), uridinediphosphoglucuronic pyrophosphatase (E.C.3.6.1.9), and hexobarbital oxidase.

Adrenal Gland Diseases↗