bluuebunny/crossref_metadata_2025_split huggingface dataset:
On the mechanism of 5-hydroxytryptamine release by thymoleptics
Authors: Carlsson A , Jonason J , Lindqvist M 
Published: April 2011

Abstract
Rabbits were treated with nialamide followed by chlorimipramine, imipramine, desipramine or amitriptyline. Cortical brain slices were prepared and incubated with Krebs-Henseleit solution. Release of 5-hydroxytryptamine (5-ht) into the incubation medium was measured. Chlorimipramine, imipramine and amitriptyline caused release of 5-ht, whereas desipramine was without effect. The ability of cortical brain slices to retain 5-ht was dependent on energy supply, involving both aerobic and anaerobic metabolism. The data support the view that the antidepressant drugs block the membrane pump of 5-ht neurons. The observations also indicate that 5-ht is involved in thermoregulation.
A simple infrared spectrum retrieval system
Authors: Curry A S , Read J F , Brown C 
Published: April 2011

Abstract
The retrieval of an unknown spectrum from a medium-sized collection (up to 10,000) of infrared curves has been studied and a system based on a film feature card using microfilm storage developed. Tests of alternative methods of coding resulted in the choice of the six most intense absorption peaks in defined areas of the spectrum. Correct identification within 1–2 min is achieved in over 95% of searches. The system is compact, easy to operate, relatively inexpensive and easily perused.
The relation between blood levels and urinary excretion of amphetamine under controlled acidic and under fluctuating urinary pH values using [14C]amphetamine
Authors: Beckett A H , Salmon J A , Mitchard M 
Published: April 2011

Abstract
Plasma, blood cell and urine levels of amphetamine were determined after the oral administration of S-(+)-[14C]amphetamine sulphate to two subjects under conditions of controlled acidic and fluctuating urinary pH. The decline in plasma concentration of the drug was more rapid under the controlled acidic conditions than under conditions of fluctuating urinary pH. Under controlled conditions, the concentration time profiles of drug and metabolite in urine or plasma (as opposed to body levels), were suitable for kinetic analysis. The apparent rate of urinary excretion of amphetamine was proportional to its plasma concentration only under the controlled acidic urinary conditions. Amphetamine was cleared from blood more rapidly than could be accounted for by glomerular filtration under acid conditions, but when urinary pH fluctuated, clearance of the drug could be accounted for by this route.
The carvone and dillapiole content of dill fruits by gas chromatography without preliminary distillation
Authors: Betts T J 
Published: April 2011

Abstract
Cold hexane extracts of sixteen specimens of dried dill fruit were examined for their content of carvone and dillapiole by gas chromatography. Dillapiole was absent from “European dill” (even Indian grown), and present in “Indian dill” (including European grown) in about twice the weight of carvone. These two forms of dill are otherwise less distinct than the forms of fennel which are referred to one species.
A screening method for vasodilator drugs
Authors: Gay W S , Rand M J , Ross P 
Published: April 2011

Abstract
The use of the isolated perfused central artery of the rabbit ear for screening vasodilator drugs is described. The effects of these drugs are shown by reduction of vasoconstrictor responses to intermittent sympathetic stimulation or to injections of noradrenaline or histamine or by reduction of vascular spasms produced by continuous sympathetic stimulation or infusion of 5-hydroxytryptamine. The relative potencies of the vasodilators used against intermittent sym- pathetic stimulation, in order are: adenosine = sodium nitroprusside = CIBA 31,531-Ba [5-amino-l-(l-methylpiperid-4-yl)- 3-(pyrid-4-y1) pyrazole] &gt; glyceryl trinitrate &gt; papaverine = amino-phylline &gt; dipyridamole » sodium nitrite = hydrallazine.
Effect of diazepam and chlordiazepoxide on the metabolism of other drugs
Authors: Jori A , Prestini P E , Pugliatti C 
Published: April 2011

Abstract
Diazepam and chlordiazepoxide, even at high single doses, do not inhibit the metabolic transformation of p-nitroanisol, aniline and aminopyrine by the 9,000 g fraction of rat liver. Although diazepam and chlordiazepoxide increase the sleeping time induced by pentobarbitone, this effect is not explained by an increase in the brain level of pentobarbitone. Repeated administrations of the two benzodiazepines increase the metabolism of p-nitroanisol, aniline, amidopyrine and shorten the sleeping time induced by pentobarbitone in rats. There was a concomitant reduction of the concentration of brain pentobarbitone.
The relation between the bactericidal activities and certain physico-chemical properties of some fluorophenols
Authors: Pinney R J , Walters V 
Published: April 2011

Abstract
The antibacterial activities, as demonstrated by the Rideal-Walker coefficients and viable counts, of mono-, 2,4,5– tri-, 2,3,5,6- tetra- and pentafluorophenol increase with the number of substituent fluorine atoms. The thermodynamic activities (Ferguson values) range from 0·083 to 0·022, and indicate a non-specific physical mode of action. Linear correlations occur between the equitoxic concentrations of the compounds to Escherichia coli (99·9% mortality after 50 min contact) and their molecular weights, number of fluorine substituents and water solubilities. A similar relation exists between the molar concentrations at the Rideal-Walker end points and the oleyl alcohol-water partition coefficients; no correlation occurs between toxicity and the cyclohexane-water partition coefficients. The surface tensions of equitoxic solutions vary between 57·5 and 63·2 mNm−1 (dynes/cm).
Antituberculosis activity of some nitrofuran derivatives
Authors: Bruhin H , Bühlmann X , Hook W H , Hoyle W , Orford B , Vischer W 
Published: April 2011

Abstract
A series of 4,6-disubstituted 2-(5-nitrofurfurylidenehydrazino)-1,3,5-triazines has been synthesized. Some of these compounds possessed good antibacterial activity against Mycobacterium tuberculosis in vitro and moderate activity in vivo (the activity in vivo was observed only with high dosages compared with compounds in clinical use and the results were also irregular). The most active compounds are triazinylhydrazones of 5-nitro-2-furaldehyde in which the triazine ring is substituted with two amino-groups, at least one of which is an (α-branched chain alkyl)- or cycloalkylamine. Structure- anti-tuberculosis activity relations for these compounds are discussed.
Quality control of white soft paraffin
Authors: Longworth A R , French J D 
Published: April 2011

Abstract
Samples of white soft paraffin complying with pharmacopoeial requirements vary in their physical properties. Some samples produce hard waxy lumps and permit excessive separation of liquid components (bleeding). Measurement of melting and congealing points and consistency by penetrometer failed to reveal these differences. The viscosity of samples after 20 min shear (1159s−1) is related to lump formation as detected by usual examination of samples heated and cooled without stirring and spread on a tile after gentle mixing.
Some physico-chemical properties of SKF 525-A in aqueous solution
Authors: Florence A T 
Published: April 2011

Abstract
The properties of solutions of SKF 525-A (β-diethylaminoethyl diphenylpropylacetate hydrochloride) have been investigated using surface tension, light scattering and microelectrophoretic techniques. The interaction of the drug with cholesterol and lecithin monolayers was studied by a surface balance method. SKF 525-A is more surface-active than chlorpromazine, and forms micelles containing 22 monomers in 0·9% NaCl solution. It increases the surface pressure of L-α-lecithin monolayers spread on water and both L-α-lecithin and cholesterol monolayers spread on 0·9% NaCl solutions at 1–2 × 10−6M concentration levels. Because of the surface-active properties of SKF 525-A caution is urged in the interpretation of enzyme inhibition results as surfactants are well known as a class to greatly affect enzyme systems.
The solubility of dodecane in water-amide mixtures
Authors: McDonald C 
Published: April 2011

Abstract
The solubility of dodecane has been determined in formamide, and in mixtures of water with formamide, N-methylformamide (NMF), and dimethylformamide (DMF) by a radiotracer method at 15°, 25° and 35°. The solubility of dodecane increases as the concentrations of the amides increase. The standard free energies (ΔG°), partial enthalpies (ΔH°), and standard entropies (ΔS°), of solution of dodecane have been calculated for the various systems. Positive values of ΔG° and negative values of ΔH° and ΔS° decrease numerically as the concentrations of amides increase.
The effects of P-2-AM on the release of acetylcholine from the isolated diaphragm of the rat
Authors: Goyer Robert G 
Published: April 2011

Abstract
Release of acetylcholine from rat isolated diaphragm preparations stimulated through the phrenic nerve was investigated in the presence of P-2-AM 0·01–100 mM. At 1 mM, the release of acetylcholine was increased by 157%, while higher concentrations resulted in a decrease. The findings indicate that the biphasic action of P-2-AM can be explained, at least in part, by variations in the quantal release of acetylcholine—an effect involving a presynaptic action.
The inhibitory effect of non-steroidal anti-inflammatory agents on aggregation of red cells in vitro
Authors: Görög P , Kovács Iren B 
Published: April 2011

Abstract
Aggregation of red cells of rat in saline suspension was induced by gelatin, high molecular weight dextran and fibrinogen. Except chloroquine, non-steroidal anti-inflammatory agents (NAIA) inhibited macromolecule-induced red cell aggregation in vitro. Glucocorticoids failed to inhibit red cell aggregation even in large concentrations. Of many drugs examined, only the NAIA and certain antihistamines, having experimental anti-inflammatory effects proved to be effective inhibitors of gelatin-induced red cell aggregation, in vitro.
Evidence that the hypotensive action of methyldopa is mediated by central actions of methylnoradrenaline
Authors: HENNING M , RUBENSON A 
Published: April 2011

Abstract
Mean arterial blood pressure was recorded in conscious normotensive rats through indwelling arterial catheters. The effect of l-α-methyldopa (α-MD) (400 mg/kg, i.p.) was studied in animals pretreated with α-methyl-m-tyrosine (400 mg/kg i.p.) 27 and 15 h before α-MD, α-methyl-p-tyrosine methylester (H 44/68) (250 mg/kg, i.p.) 1 h before α-MD, and dl-α-hydrazino-α-methyl-β-(3,4-dihydroxyphenyl) propionic acid (MK 485, 100 mg/kg, i.p.) 30 min before α-MD. This pretreatment, which resulted in a severe depletion of endogenous catecholamines, did not alter the hypotensive effect of α-MD. The effect of α-MD (200 mg/kg, i.p.) was studied 30 min after pretreatment with the dopamine β-hydroxylase inhibitor, bis (4-methyl-l-homopiperazinyl-thiocarbonyl) disulphide (FLA-63) (25 mg/kg, i.p.). The hypotensive response to α-MD was completely abolished in these experiments. The formation of α-methylnoradrenaline from α-MD was prevented after FLA-63 but there was a significant increase in the amounts of α-methyldopamine formed.
The influence of hexobarbitone on calcium ion movements in isolated heart muscle
Authors: HAACKE H , VAN ZWIETEN P A 
Published: April 2011

Abstract
In beating atria (frequency 180/min) sodium hexobarbitone (7·8 × 10−4M) inhibited the rate of uptake of 45Ca2+ from the medium without influencing the total calcium content of the tissues. Concomitantly, the so-called exchangeable calcium fraction was diminished although not at equilbrium. In resting left auricles the barbiturate did not affect 45Ca+-uptake or the exchangeable calcium fraction. It seems likely that the barbiturate reduces membrane permeability towards Ca2+ during excitation without influencing the permeability at rest.
Interaction of preservatives with cetomacrogol
Authors: KAZMI S J A , MITCHELL A G 
Published: April 2011

Abstract
The interaction of a number of commonly used preservatives (benzoic acid, p-hydroxybenzoic acid, methyl p-hydroxybenzoate, propyl p-hydroxybenzoate and chloroxylenol with the non-ionic surfactant cetomacrogol was examined and a comparison made of various methods of expressing this interaction. It is suggested that the Scatchard equation is the most satisfactory equation for describing the binding data. Binding parameters determined from a Scatchard plot in the concentration range of free preservative appropriate for antimicrobial activity can be used to calculate the total concentration of preservative required in the surfactant system.
The effect of drugs upon the uptake of 5-hydroxytryptamine and metaraminol by human platelets
Authors: AHTEE LIISA , SAARNIVAARA LAILA 
Published: April 2011

Abstract
The abilities of some tricyclic and bicyclic antidepressive drugs and an α-receptor blocking agent, phenoxybenzamine, to inhibit the uptake of 5-hydroxytryptamine (5-HT) and (—)-metaraminol into human platelets have been compared in vitro. All the drugs inhibited the uptake both of 5-HT and of metaraminol into platelets. But there were differences in their abilities to inhibit the uptake of these two monoamines. The desmethylated antidepressive drugs were more potent inhibitors of metaraminol uptake than were their tertiary analogues, whereas imipramine, a tertiary amine, was by far the best inhibitor of 5-HT uptake. The order of the activities of the antidepressive drugs in inhibiting the uptake of 5-HT and metaraminol into platelets paralleled their potencies in blocking the uptake of 5-HT, and noradrenaline or metaraminol into nerve endings. It is suggested that the uptake of 5-HT and metaraminol into platelets is a useful model for the neuronal uptake of 5-HT and noradrenaline, respectively.
The effect of brocresine (NSD-1055) on the histidine decarboxylase activity in the rat gastric mucosa
Authors: MESCH H , SEWING K-FR 
Published: April 2011

Abstract
The effect of the histidine decarboxylase inhibitor brocresine (NSD-1055) on the specific histidine decarboxylase in the gastric mucosa was investigated in rats. The inhibiting potencies of brocresine were compared after oral and intraperitoneal administration with and without 2-deoxy-d-glucose. Furthermore, different doses of brocresine were added directly to an incubation medium containing an homogenate of the gastric mucosa of untreated animals. The gastric histidine decarboxylase of the brocresine-pretreated animals was not inhibited. Addition of brocresine to the incubation medium produced a dose dependent blockade of the enzyme. 50% inhibition was accomplished by a concentration of 1·4 times 10−6M. The results demonstrated an inhibition of the rat stomach histidine decarboxylase in vitro, but not in vivo, indicating the inability of brocresine to interfere with the biosynthesis of histamine in the rat stomach.
The effect of solvents on the potency of chlordiazepoxide, diazepam, medazepam and nitrazepam
Authors: CRANKSHAW D P , RAPER C 
Published: April 2011

Abstract
ED50 values for loss of righting reflex in mice have been determined for a series of benzodiazepines after intraperitoneal injection of the drugs in various vehicles. The vehicles used greatly modified the ED50 values obtained. The effects obtained were due either to a failure of the vehicle to achieve or maintain complete solubilization of the drug, or to the pharmacological action of the vehicle modifying that of the drug. Diazepam, medazepam and nitrazepam are insoluble in water, but are soluble in dimethylsulphoxide (DMSO) and in aqueous vehicles containing glycofurol or propylene glycol. Chlordiazepoxide hydrochloride is water-soluble. Similar ED50 values were obtained in experiments where the benzodiazepines were injected in an aqueous carboxymethylcellulose suspension and in experiments where the drugs were dissolved in DMSO. Lower ED50 values were obtained when the drugs were dissolved in vehicles containing propylene glycol or glycofurol. The increase in potency of the benzodiazepines could be ascribed either to the solubilization of the drugs or to the synergistic pharmacological activity of the solvents. An ED50 value for diazepam, which was not influenced by the pharmacological activity of the solvent, could be obtained using the vehicles containing either glycofurol or propylene glycol. For medazepam and nitrazepam, the solvent mixtures containing propylene glycol and glycofurol respectively were required to avoid drug-solvent interactions.
Antihypertensive and noradrenaline-depleting effects of guanethidine metabolites
Authors: MAÎTRE L , STAEHELIN M , BRUNNER H 
Published: April 2011

Abstract
The antihypertensive and myocardial noradrenaline-depleting activities of the three identified guanethidine metabolites were compared with those of guanethidine itself. Metabolite A (guanethidine-N-oxide) and Metabolite B [2-(6-carboxylamino)ethylguanidine] both showed approximately 1/30th of the antihypertensive effect of guanethidine in rats. Metabolite A, but not Metabolite B, caused a depletion of cardiac noradrenaline stores. The intensity of this effect was between 1/10th and 1/30th that of guanethidine. Metabolite C [(6-carboxyhexyl)-2-iminoimidazolidine] was inactive on both parameters. [3H]Noradrenaline uptake into isolated bovine nerve granules was not impaired by either guanethidine or its metabolites. It is concluded that the antihypertensive and myocardial noradrenaline depleting effects of guanethidine are produced by the unchanged drug rather than by one of the identified metabolites.
Identification in hashish of tetrahydrocannabinol, cannabidiol and cannabinol analogues with a methyl side-chain
Authors: VREE T B , BREIMER D D , VAN GINNEKEN C A M , VAN ROSSUM J M 
Published: April 2011

Abstract
The cannabis constituents Δ1-tetrahydrocannabinol, cannabidiol and cannabinol are accompanied by their homologues with an n-propyl and with a methyl side-chain. The identification procedure by combined gas chromatography-mass spectrometry in hashish and marihuana is described and the consequences for cannabis use are discussed.
Kinetics of dextrose degradation under autoclaving conditions
Authors: TAYLOR R B , JAPPY B M , NEIL J M 
Published: April 2011

Abstract
The kinetics of the decomposition of dextrose have been investigated over a temperature range of 106° to 127°. The reaction is shown to exhibit an induction period with respect to 5-hydroxymethylfurfural production which is due to the formation of an intermediate compound. A reaction mechanism is proposed which appears consistent with the experimental measurements. Rate constants are calculated for the various reaction steps and the activation energies associated with these steps are reported.
Increased release of xylocholine (TM10) from guinea-pig vas deferens treated with amphetamine sulphate
Authors: DEAN H G , HUGHES I E 
Published: April 2011

Abstract
Although both NN-diethyl- and NN-dimethyl-, N-methyl-[14C]-2-(2,6-xylyloxy) ethylammonium iodide (14C-1DE10 iodide and 14C-TM10 iodide; xylocholine) are taken up by guinea-pig vas deferens to a similar extent in vitro, only TM10 reduced the response of the vas deferens to electrical stimulation. Prior incubation of vas deferens with 14C-1DE10 iodide or with 14C-TM10 iodide followed by measurement of the amount of each of these compounds eliminated from the tissue by repeated washing with Krebs solution, shows both compounds to be strongly retained by the tissue. Incorporation of 10−5 g/ml amphetamine sulphate in the wash fluid failed to modify the release of 14C-1DE10 iodide but produced a short-lived increase in the amount of 14C-TM10 iodide eliminated which reached a maximum approximately 10 min after administration of amphetamine. The additional 14C-TM10 iodide eliminated by amphetamine was about 5% of the total tissue 14C-TM10 iodide content; the possible role of this fraction is discussed in relation to the adrenergic neuronblocking action of 14C-TM10 iodide.
Automatic weight-control in a rotary tabletting machine
Authors: RIDGWAY K , DEER J J , FINLAY P L , LAZAROU C 
Published: April 2011

Abstract
A Manesty “Betapress” 16-station high speed rotary tabletting machine has been fitted with pressure rolls containing piezoelectric transducers in the axles. The compaction force exerted at each tablet compression event produces an electrical pulse which can be fed to an integrated-circuit pulse-discriminating unit. If, for any reason, the quantity of powder in any die is such that an over- or under-pressure occurs on compaction, the resultant incorrect-magnitude pulse is used to operate a stepping motor which adjusts the feed screw of the rotary machine in the correct direction to restore the desired operating conditions and maintain weight constancy. The degree of over- or under-pressure needed to cause corrective action is readily adjustable. An electromagnetically-operated solenoid valve is also controlled by the pulse-discriminator, so that tablets of incorrect weight are deflected by an air jet as they leave the die table. The ejection force can also be monitored and the signal used to operate an alarm if the force should become too large due to punch-sticking.
X-ray analysis of Th 1165a and salbutamol
Authors: BEALE J P , STEPHENSON N C 
Published: April 2011

Abstract
Two drugs, Th1165a* and salbutamol,† having a promising potential as bronchodilators and producing low cardiac stimulation, have been examined for their structural features. These were found to be similar and have been noted as possibly characteristic of the particular β2-adrenoceptor site. Th1165 consists of two enantiomers possessing an (R-R) or (S-S) configuration about the two centres of asymmetry.
The effects of eserine and neostigmine on the guinea-pig ileum and on ilial longitudinal muscle strips
Authors: COX B , LOMAS D M 
Published: April 2011

Abstract
Eserine and neostigmine produced spasms of the guinea-pig isolated ileum that were concentration-related (4 ng-16 μg/ml). Hexamethonium (100 μg/ml) and tetrodotoxin (100 ng/ml) reduced the spasmogenic activity of both drugs. Neostigmine, but not eserine, overcame the hexamethonium antagonism. Pretreatment of the ileum with dyflos (1 μg/ml for 10 min) did not affect the action of either eserine or neostigmine, therefore the spasm was not due to inhibition of cholinesterase. The residual response to eserine or neostigmine after tetrodotoxin was abolished by hyoscine (4 ng/ml). Isolated longitudinal muscle strips were so prepared to be innervated or denervated. Both types of strip gave similar bradykinin maxima but the response of the denervated strip to eserine and neostigmine was reduced to 40% of the innervated strip and the remaining response was blocked by hyoscine (2 ng/ml). It is concluded that eserine and neostigmine have an indirect action on the smooth muscle of the ileum that is the result of acetylcholine release from cholinergic nerves. Inhibition of cholinesterase would not seem to be important for this action. A second component of the action of these two drugs appears to be a direct effect on the muscarinic receptors of the smooth muscle.