bluuebunny/crossref_metadata_2025_split huggingface dataset:
Uptake and metabolism of β-phenethylamine and tyramine in mouse brain and heart slices
Authors: ROSS S B , RENYI A L 
Published: April 2011

Abstract
Tritium labelled β-phenethylamine and tyramine were incubated with slices of mouse brain and heart. Cocaine (3 × 10−5M) caused a reduction of 30% in the uptake of tyramine as well as in the formation of its metabolite 4-hydroxyphenylacetic acid. Cocaine had no effect on either the uptake of phenethylamine nor its deamination to phenylacetic acid.
The influence of compression and formulation on the hardness, disintegration, dissolution, absorption and excretion of sulphadimidine tablets
Authors: VAN OUDTSHOORN M C B , POTGIETER F J , DE BLAEY C J , POLDERMAN J 
Published: April 2011

Abstract
Sulphadimidine tablets were prepared with different binding agents and compressed at different compression levels, ranging from 200–2000 MNm2. The disintegration time and dissolution rate of the different tablets were determined. Tablets formulated with gelatin or starch mucilage and compressed at 600 MNm2 were selected for in vivo experiments using a urinary excretion method. Although both tablets complied with the disintegration requirements of the British Pharmacopoeia, dissolution rate and urinary excretion showed a difference in availability of drug from the two tablets.
The polymorphism of sulphathiazole
Authors: MESLEY R J 
Published: April 2011

Abstract
The existence of two species of the low temperature form of sulphathiazole, postulated by Moustafa & Carless (1969) and by Shenouda (1970), has been confirmed. Contrary to the opinions of these workers it is concluded that these are two distinct forms having different lattice structures which give rise to distinguishable X-ray diffraction patterns and infrared spectra. The fact that commercial samples frequently contain both forms casts doubt on the validity of previous solubility measurements and on the use of differential scanning calorimetry as an assay procedure for the low temperature form.
Determination of N-(2-benzoyloxyethyl)-norfenfluramine (JP 992) and its metabolites in urine
Authors: BECKETT A H , SHENOY E V B , BROOKES L G 
Published: April 2011

Abstract
A gas-liquid chromatographic method of determination of norfenfluramine and N-2-hydroxyethylnorfenfluramine is described. Also a method is reported to determine N-(2-benzoyloxyethyl)norfenfluramine and its metabolites containing the m-trifluoromethyl- benzyl and -benzoyl moieties in urine, by oxidation of these to m-trifluoromethyl benzoic acid followed by methylation and gas-liquid chromatography.
Cell culture as a test system for toxicity
Authors: METCALFE SUSAN M 
Published: April 2011

Abstract
Appropriate cell culture systems provide a useful additional method of screening for toxicity, in spite of the obvious problems of relating in vitro effects of test compounds at the cellular level to their effects in the whole animal. It is shown that a wide range of chemically disimilar molecules have a reversible inhibitory activity on the growth of primary cultures of monkey kidney cells. The potency of these compounds correlates with their lipid solubility, suggesting that the cell membranes may be their main site of action. Support for this is obtained by the correlation of inhibitory activity and the ability of the same compounds to stabilize the erythrocyte membrane against hypotonic haemolysis which is known to be a direct effect of interaction with the erythrocyte membrane. It is suggested that the ability of the food additive butylated hydroxytoluene to act as a potent inhibitor of cellular growth may account for its reported ability to prolong the life span of mice.
Some aspects of the metabolism of morphine-N-oxide
Authors: HEIMANS R L H , FENNESSY M R , GAFF G A 
Published: April 2011

Abstract
After administration of morphine-N-oxide (MNO) to rats the opiates appearing in the urine were morphine (61%) and MNO (39%). After administration of morphine, the urinary opiates were morphine (80%) and normorphine (20%). When tacrine was given with morphine the urine also contained MNO (46% of total urinary opiates) and the amount of normorphine was much decreased (to 1%), the remainder being morphine (53%). Tacrine and amiphenazole inhibited demethylation of morphine and codeine by a rat liver fraction in vitro. MNO had weak inhibitory activity. Neither MNO nor codeine-N-oxide were demethylated in vitro.
The metabolism and binding of [14C]mycophenolic acid in the rat
Authors: NERY R , NICE E 
Published: April 2011

Abstract
Seventeen h after the intraperitoneal administration of 33 mg/kg of [14C]mycophenolic acid to rats, radioactivity was bound to the tissues of the intestines, bladder, stomach, kidney, liver and lung in decreasing order; no binding to spleen tissue was observed. In vitro incubations of the agent with macromolecules resulted in the binding of radioactivity to salmon sperm DNA and to bovine plasma albumin, the extent of binding being increased and decreased, respectively, in the presence of a rat liver microsomal system. The binding was apparently covalent since repeated purification procedures failed to release the bound radioactivity; heating of [14C]mycophenolic acid bound-DNA in n hydrochloric acid at 100° for 2 h caused the release of the bound radioactivity. Under the conditions described, 43% of the administered radioactivity was excreted in the urine (33%) and faeces (10%); the urine contained free mycophenolic acid (13%), mycophenolic acid glucosiduronate (17%) and an uncharacterized metabolite (3%).
The relation between biological activity and the degree of resolution of optical isomers
Authors: BARLOW R B , FRANKS FIONA M , PEARSON J D M 
Published: April 2011

Abstract
Previous reports of the low stereospecificity of benzhexol can be ascribed to inadequate resolution of the samples tested and a report of much higher stereospecificity has been confirmed. The two enantiomers have been found to differ over 1000-fold in their affinity for the postganglionic acetylcholine receptors of the guinea-pig ileum. Mixtures of the enantiomeric forms of phenylcyclohexyl-glycolloylcholine and of benzhexol have been tested on this preparation and the dose-ratios used to calculate apparent affinity constants. With both pairs the results indicate that the two enantiomers compete with the agonist and with each other and justify the use of the stereo-specific index to set limits to the degree of resolution. For compounds such as these, in which one enantiomer has appreciably higher biological activity than the other, this biological method for assessing stereochemical purity is likely to be at least as satisfactory as any nuclear magnetic resonance method currently in use, because of the very great sensitivity of the stereospecific index to the degree of resolution.
Localization of [3H]pimozide in the rat brain in relation to its anti-amphetamine potency
Authors: SOUDIJN W , VAN WIJNGAARDEN I 
Published: April 2011

Abstract
The pharmacological activity of the neuroleptic agent pimozide is well correlated with the concentration of [3H]pimozide in the brain of the Wistar rat. There is an enhanced uptake and retention of [3H]pimozide in the caudate nucleus, an area in which amphetamine and apomorphine act. Its concentration in the caudate nucleus is not correlated with its anti-apomorphine and anti-amphetamine potency. There are, however, significant shifts in the subcellular distribution of [3H]pimozide in the caudate nucleus, from the mitochondrial fraction to the fraction consisting mainly of submicroscopic nerve endings. These shifts correlate well with its pharmacological activity. This points to the small nerve-endings as being the site of action of pimozide. The drug does not influence either the penetration of (+)-[14C]amphetamine into the brain, or its metabolism, indicating that the anti-amphetamine action cannot be due to a decreased penetration of amphetamine into the brain, although a subcellular redistribution of amphetamine induced by pimozide cannot be excluded.
A modification of rat adjuvant arthritis for testing antirheumatic drugs
Authors: MIZUSHIMA Y , TSUKADA W , AKIMOTO T 
Published: April 2011

Abstract
An inflammation having an acute and a prolonged phase was induced by the injection of carrageenan into the paw of rats inoculated with adjuvant 6 days previously (adjuvant-carrageenan-induced inflammation, ACII). Steroidal and acidic non-steroidal anti-inflammatory drugs were effective on both phases. Basic non-steroidal antiinflammatory drugs were effective only on the acute phase, and cytotoxic drugs only on the prolonged phase. Neither gold nor chloroquine preparations inhibited either phase. Effectiveness of drugs on the acute phase was similar to that on carrageenan oedema. Inhibitory effects of drugs on the prolonged phase were similar to those on the secondary lesions of adjuvant arthritis. The ACII test is considered to have advantages compared with the adjuvant arthritis test in duration of drug administration, in the measurement of intensity of inflammation, in the time for experiment and in analysing the action of drugs.
A new spectrophotometric method for the determination of penicillins
Authors: BUNDGAARD HANS , ILVER K 
Published: April 2011

Abstract
A rapid and convenient method is described for the determination of nine commonly used penicillins. This is based on the spectrophotometric measurement at 325–345 nm of penicillenic acid mercuric mercaptides of the penicillins, formed in quantitative yield on heating at 60° or on standing at 20° in a 1·2 m imidazole and 10−3 m mercuric chloride solution at pH 6·8. The method, which permits detection of concentrations of penicillins down to 0·5 μg/ml, is reproducible. Since the intact penicillin molecule is required for the penicillenic acid formation, the method is highly specific and useful as a means of assessing stability.
Titrimetric determination of sulphate in pharmaceutical products
Authors: ROETS E , VANDERHAEGHE H 
Published: April 2011

Abstract
A method is described for the titrimetric determination of sulphate in pharmaceutical products. After fixation of the base on a cation exchange resin column, sulphuric acid was titrated with barium chloride in the presence of thorin indicator. The titrimetric method was compared with the gravimetric method.
The effect of intra- and extragranular maize starch on the disintegration of compressed tablets
Authors: SHOTTON E , LEONARD G S 
Published: April 2011

Abstract
The effect of maize starch on the particle sizes recovered from sulphadiazine tablets subjected to the B.P. disintegration test has been examined. A size analysis of the resulting suspension was made using a combination of wet sieving techniques and the Coulter Counter. Intragranular starch resulted in the recovery of finer particles than when extragranular starch was used, but the disintegration time was longer with intragranular starch. The use of both intra- and extragranular starch in a tablet gave intermediate disintegration time and mean diameter.
Determination of thermodynamic dissociation constants of local anaesthetic amines: influence of ionic strength
Authors: LEVY RENÉ H , ROWLAND MALCOLM 
Published: April 2011

Abstract
Theoretical calculations, based on the Debye-Hückel theory, indicate that for weak monoprotic bases that do not involve a hydroxyl group (B) a stoichiometric pKa determined at any ionic strength compatible with an accurate determination (μ &lt;0·10) should be no different from the thermodynamic pKa. The pKa's of two local anaesthetic amines were determined at several ionic concentrations. The resultant independence of the acidic dissociation constants on ionic concentration supports the theoretical considerations. The implications of these results in local anaesthetic research are discussed.
Determination of zinc in pharmaceutical preparations by atomic absorption spectrophotometry
Authors: MOODY R R , TAYLOR R B 
Published: April 2011

Abstract
The analysis for Zn content of a variety of pharmaceutical preparations by atomic absorption spectrophotometry is recorded. The method for creams, ointments and pastes involves extraction with ether, dissolving the residue in HCl, followed by suitable dilution of the extract to bring the Zn content within the limits of the calibration graph, and measurement of the Zn content using the 213·9 nm resonance line. For lotions and dusting powders the initial ether extraction is neglected; for liquid preparations a simple dilution is required. The method showed a good degree of accuracy and precision and was specific for Zn no interference being encountered from a variety of metals and other common excipient materials that are used in pharmaceutical preparations.
An improved in vivo procedure for standardization of heparin preparations
Authors: KUO S H , JAQUES L B , MILLAR G J 
Published: April 2011

Abstract
The WHO International Collaborative Study of the Assay of Heparin has demonstrated the unreliability of present assay methods for heparin. An in vivo assay procedure has been redesigned to use standardized dogs in a crossover assay, measuring three coagulation tests and lipoprotein lipase on nine blood samples for each heparin dose. The procedure was tested with five heparin preparations. By the standard method for parallel line assays regression was significant (P &gt; 0·001) for log2 dose-log10 response. Analyses of variance were satisfactory and estimation of potency statistically valid. The potency of each heparin in International units varied with the parameter used. Fiducial limits were ±10% for anticoagulant parameters, ±15% for antilipaemic parameter and reproducibility, 97% for anticoagulant parameters, 87·5% for antilipaemic parameter.
Interaction of glutethimide and phenobarbitone with ethanol in man
Authors: MOULD G P , CURRY S H , BINNS T B 
Published: April 2011

Abstract
Interactions of ethanol with glutethimide and phenobarbitone in man were examined by means of psychomotor tests and measurement of ethanol and glutethimide in body fluids. Blood ethanol was about 11% higher overall when glutethimide and ethanol were given than in controls given ethanol alone, and 30% higher at 105 and 135 min. When phenobarbitone and ethanol were given there was a slight but significant reduction in blood ethanol. In the presence of ethanol there was a fall in plasma and urinary glutethimide. Changes in blood ethanol were reflected by changes in reaction time tests. Changes in plasma glutethimide were reflected by changes in tracking efficiency and finger tapping speed. These studies illustrate the need to assess drug concentrations in other interaction studies with ethanol and depressant drugs.
Effects of solubilization on drug diffusion
Authors: BLOOR J R , MORRISON J C 
Published: April 2011

Abstract
The diffusion of ephedrine, sulphathiazole, chloramphenicol, paracetamol, isoniazid and amphetamine in solutions of Tween 40, Tween 80 and cetomacrogol 1000 have been studied. With the exception of isoniazid, the observed diffusion coefficients, corrected for resistance to flow, depend upon the surfactant used and both the drug and surfactant concentration. The effect of drug solubilization upon the diffusion coefficient is also discussed.
Homologues of benzilylcholine mustard
Authors: YOUNG J M , HILEY ROBIN , BURGEN A S V 
Published: April 2011

Abstract
Seven homologues of the alkylating muscarinic antagonist benzilylcholine mustard (BCM) have been prepared. The rate of reaction of the aziridinium ion derivatives with water is largely independent of the structure, whereas the rate of reaction with the muscarinic receptor drops markedly when the N-alkyl group is larger than n-propyl. PrBCM is practically equiactive with BCM. Recovery from block caused by PrBCM was first-order with a half-time of 32 h at 37°.
Inhibition of dopadecarboxylase in the rat by a series of benzyloxyamines
Authors: LAZARE R , WATSON P A 
Published: April 2011

Abstract
A series of eleven benzyloxyamines has been evaluated for in vitro and in vivo inhibition of dopa decarboxylase. The effect of these inhibitors on the rise in [14C]amines in the brain after [14C]dopa has also been assessed. Of these compounds, 3,4-dihydroxybenzyloxyamine appears to be a potent selective peripheral inhibitor of dopa decarboxylase. Its activity is similar to that of Ro 4–4602 [N1-(dl-seryl)-N2-(2,3,4-trihydroxybenzyl) hydrazine].
Abolition of the morphine effect on body temperature in midbrain raphe lesioned rats
Authors: SAMANIN R , KON S , GARATTINI S 
Published: April 2011

Abstract
The hyperthermia and the hypothermia elicited by 5 mg/kg, i.p. or 30 mg/kg i.p. of morphine in rats are abolished by a previous lesion of the midbrain raphe resulting in a lowering of forebrain 5-HT and 5-hydroxyindolacetic acid. Lesions lateral to the midbrain raphe which do not modify brain 5-HT are without effect on body temperature changes induced by morphine. Animals lesioned in the midbrain raphe are still able to respond with a hyperthermia or with a hypothermia when they are treated respectively with 2,4-dinitrophenol or phentolamine.
The effect of fourteen day treatment with diuretics on mouse blood sugar and glucose tolerance
Authors: FOY J M , FURMAN B L 
Published: April 2011

Abstract
Treatment of mice for 14 days with ethacrynic acid or frusemide (100 mg/kg daily orally) increased the fasting blood sugar and liver glycogen. Oral glucose tolerance was altered so that blood sugar concentrations in drug-treated groups were significantly above control values. The failure of the drugs to affect intravenous glucose tolerance and sensitivity to insulin or to tolbutamide suggested that the decrease in the oral glucose tolerance was attributable to some effect of the drug treatments on the rate of absorption of glucose from the gastrointestinal tract. Treatment with hydrochlorothiazide (100 mg/kg daily orally) exerted no effect on blood sugar, liver glycogen or glucose tolerance.
The relation between the subcellular distribution of [3H]reserpine and its proposed site of action
Authors: WAGNER LORIN A , STITZEL ROBERT E 
Published: April 2011

Abstract
The amount of [3H]reserpine retained after injection is greater in the heart, a tissue with a high density of adrenergic innervation than in femoral muscle. Subcellular distribution studies emphasized that 15 and 60 min after injection of [3H]reserpine it could not be shown to be uniquely associated with the noradrenaline-containing granules. The possibility existed that the large amount of reserpine bound to cellular lipids at these times might mask a more specific binding. A reduction in the dose and a lengthening of the time between drug administration and tissue measurement to 18 h revealed a small amount of [3H]reserpine to be bound more firmly to the microsomal or amine granule-containing fraction. Prior saturation of tissue binding sites by treatment with large amounts of unlabelled reserpine or tetrabenazine decreased the retention of subsequently injected [3H]reserpine. This decreased tissue retention resulted in an increase in the formation of [3H]trimethoxybenzoic acid.
A model is proposed relating tissue distribution and binding to reserpine's mechanism of action.
The quantitative determination of fluocinolone acetonide and acetonide acetate in formulated products by high pressure liquid chromatography
Authors: BAILEY F , BRITTAIN P N 
Published: April 2011

Abstract
A chromatographic procedure for the determination of fluocinolone acetonide and acetate is described. The method employs high speed liquid chromatography through a Permaphase ODS column with an aqueous methanol eluant phase. The application of the method to the determination of fluocinolone acetonide and acetate in cream, and ointment formulations, is described.
Effect of frusemide on the reactivity of rat portal vein
Authors: BLAIR-WEST J R , MCKINLEY M J , MCKENZIE J S 
Published: April 2011

Abstract
Short lengths of rat portal vein were suspended in Krebs bicarbonate solution. Contractile responses to noradrenaline and angiotensin II and the parameters of spontaneous contractions were determined before and after addition of frusemide at 10–6 and 10–4 g/ml. Frusemide at 10–6 g/ml slightly suppressed the amplitude of spontaneous contractions and slightly decreased the responses to noradrenaline and angiotensin II. At 10–4 g/ml the drug had a much greater inhibitory effect on endogenous and exogenous stimulation. The concentrations used appear to be similar to those achieved during effective diuretic and hypotensive treatment. It is postulated that frusemide may have a direct inhibitory action on the reactivity of vascular smooth muscle mrticularlv in the capacitance vessels.
On the localization of the hypotensive effect of L-dopa
Authors: HENNING M , RUBENSON A , TROLIN G 
Published: April 2011

Abstract
Mean arterial blood pressure was recorded in anaesthetized rats before and after a mid-collicular transection of the brain (decerebration). Basal blood pressure was not changed by the decerebration. Injection of l-dopa (200 mg/kg, i.p.) after peripheral dopa decarboxylase inhibition by l-α-hydrazino-α-methyl-β-(3,4-dihydroxyphenyl) propionic acid (MK 486, 100 mg/kg, i.p.) resulted in a significant reduction of arterial pressure to the same level in both control (sham- operated) and decerebrated rats after 30 min. In other experiments, anaesthetized rats were spinalized at C7-Th1. Basal blood pressure became significantly lower than in control and decerebrated rats and l-dopa after MK 486 in the same doses did not affect blood pressure. Biochemical determinations of noradrenaline and dopamine showed that administration of l-dopa after MK 486 to decerebrated rats in the same doses as in the blood pressure experiments resulted in a pronounced increase of dopamine in both parts of the brain.
On the inducing activity of eucalyptol
Authors: JORI A , DI SALLE E , PESCADOR R 
Published: April 2011

Abstract
Eucalyptol increases the microsomal activity of rat liver after a single dose given subcutaneously. Further doses do not enhance the effect. Eucalyptol does not affect the concentration of cytochrome P450 in liver microsomes. In this it differs from pheno- barbitone. Both drugs increase the biliary flow but only pheno- barbitone enhances the excretion of conjugated bilirubin after an intravenous load of bilirubin. The results suggest that the induction of liver microsomal enzymes elicited by eucalyptol differs from that elicited by phenobarbitone.
Determination of thermodynamics of halogen groups in solutions of drug molecules
Authors: Davis S S 
Published: April 2011

Abstract
The contribution of the halogen groups (F, Cl, Br, I) to solute activity and partition coefficients has been investigated using literature data. The activity coefficient for an aromatic solute at infinite dilution is increased as the size of the halogen group increases. Partition coefficients are affected similarly but there is variation among group values for a given halogen. This is related to group position and the partition solvent. Preferred group values for partition have been selected and for different solvent systems mean preferred values can be calculated for two general solvent classifications; polar and non-polar. There is excellent correlation between group values and the size of the halogen function as given by surface area. The group values for non-polar solvents are related to those of the polar solvents through the Hammett electronic substituent constant. The use of the group values in structure-activity relations is discussed with reference to the thermodynamic model of Higuchi and Davis.