bluuebunny/crossref_metadata_2025_split huggingface dataset:
The assignment of absolute configurations to the individual enantiomorphs of phenylpropylmethylamine and pipradrol hydrochloride
Authors: Hemingway R J 
Published: April 2011

Abstract
The configuration of the C-2 asymmetric centre of (—)-phenylpropylmethylamine (N-methyl-2-phenylpropylamine) has been related by a stereospecific route to that of the analogous centre of (+)-(S)-hydratropic acid. The configuration at the C-2 asymmetric centre of (—)-pipradrol (diphenylpiperid-2-ylmethanol) hydrochloride has been related by a stereospecific route to that of the analogous centre of (+)-(R)-pipecolic acid.
Kinetics of buccal absorption of amphetamines
Authors: Beckett A H , Boyes R N , Triggs E J 
Published: April 2011

Abstract
The buccal absorption of amphetamine, methylamphetamine and dimethylamphetamine in solutions at pH 8·16 and 9·18, was measured in man after 1, 2, 3, 4, 5 and 10 min. The recovery of the drugs from the buccal membrane after uptake was also measured by washing out the mouth for varying times with buffer solutions. An analogue computer model of the biological system was used and the kinetic parameters for the buccal absorption of the amphetamines were calculated.
Inhibition of amine uptake in the mouse heart by some new “thymoleptic” drugs
Authors: Waldeck B 
Published: April 2011

Abstract
A number of new and established thymoleptic drugs were given to mice. Their inhibitory action on the uptake of [3H]metaraminol and [3H]noradrenaline in the heart was investigated. Among the compounds tested a monomethylamino-derivative was in general 2–3 times more potent than the corresponding dimethyl-amino-derivative. The phthalan derivative 3,3-dimethyl-1-(3-methylaminopropyl)-1-phenylphthalan (Lu 3–010) was as efficient as protriptyline in all the tests performed. Changes in the substitution of the phthalan skeleton influenced the activity critically. As it is devoid of anticholinergic activity Lu 3–010 appears to be the most specific inhibitor of the amine transport mechanism of the adrenergic cell membrane found so far.
An investigation of the effects of angiotensin on the release of neurohumoral transmitters at motor, adrenergic and cholinergic nerve terminals
Authors: Hughes I E 
Published: April 2011

Abstract
On the sciatic nerve-gastrocnemius-soleus muscle preparation of the cat, angiotensin (1–5 μg/kg, i.v.) potentiated the twitch response to maximal and submaximal stimulation of the sciatic nerve and produced partial reversal of an incomplete tubocurarine blockade. These actions could not be explained in terms of increased acetylcholine release since they were not seen in isolated motor nerve-striated muscle preparations and were probably secondary to the cardiovascular actions of angiotensin. Blockade of conduction in the postganglionic cholinergic nerves in the guinea-pig isolated ileum preparation by cooling or anoxia antagonized the response of this tissue to angiotensin. These procedures left the response to exogenous acetylcholine unchanged though they removed the cholinergic component of the response to angiotensin which is known to be present in this tissue. No evidence of increase in catecholamine output could be found in preparations of guinea-pig and rabbit vasa deferentia or rabbit duodenum responding to submaximal stimulation of their adrenergic nerves. It is concluded that angiotensin has no direct action on the stores of neurohumoral transmitter at motor, postganglionic cholinergic or postganglionic adrenergic nerves and that its known acetylcholine releasing action in the isolated ileum results from stimulation of the ganglia.
A note on the subcellular distribution of adipose tissue noradrenaline
Authors: Gessa G L , Congiu S , Spano P F , Musinu C 
Published: April 2011

Abstract
The distribution of noradrenaline between the residue and high-speed supernatant of adipose tissue homogenates in rats, guinea-pigs and cats has been examined. Most of the noradrenaline is in the supernatant fraction; little is in the 100,000 g fraction.
Potentiation of acetylcholinesterase by a series of quaternary ammonium compounds
Authors: Roufogalis B D , Thomas J 
Published: April 2011

Abstract
Eleven spiran, and two non-spiran, quaternary ammonium compounds have been examined and some of these compounds found to potentiate the hydrolysis of acetylcholine by acetylcholinesterase at high substrate concentrations. The experiments were made in three reaction media, each differing in its ionic composition. The results obtained in these media differ both quantitatively and qualitatively. The mechanism of the potentiation is discussed in terms of the effect of quaternary ammonium compounds on the deacetylation step of acetylcholine hydrolysis.
Application of the analogue computer to pharmacokinetic and biopharmaceutical studies with amphetamine-type compounds
Authors: Beckett A H , Tucker G T 
Published: April 2011

Abstract
The kinetics of absorption, metabolism, and excretion of (+)-amphetamine and (+)-methylamphetamine, after oral administration of “free” dosage forms to man, under controlled acidic urine conditions, have been examined using an electronic analogue computer. This device has also been used to determine the in vivo rate of release of the drugs from hard gelatin capsule dosage forms and prolonged-release preparations. In vivo drug release from the prolonged-release preparations was correlated with in vitro drug release data.
The effect of temperature on end-plate depolarization of the rat diaphragm produced by suxamethonium and acetylcholine
Authors: Harris J B , Leach G D H 
Published: April 2011

Abstract
End-plate depolarization in the rat isolated diaphragm by suxamethonium and acetylcholine was measured at 37° and 20° using a modification of the method of Fatt (1950). At 20° the response of the motor end-plates to the depolarizing activity of acetylcholine and suxamethonium was enhanced. Since the presence of neostigmine in the bath fluid did not modify the response of the motor end-plates to the depolarizing activity of suxamethonium at 37°, the results suggest the enhanced response of the motor end-plates at 20° is due to a change in the properties of the motor end-plate, and not to a change in the activity of cholinesterases present in the tissues.
The effects of tremorine and oxotremorine in hyperthyroid mice
Authors: Waite R , Spencer P S J 
Published: April 2011

Abstract
Hyperthyroid mice exhibit only transient low-level tremor and hypothermia in response to tremorine and oxotremorine, yet the peripheral effects of these two agents are similar in intensity and duration to those elicited in control animals. These findings support the theory that tremor and hypothermia are both central effects and separate from the peripheral muscarinic actions of tremorine and oxotremorine. Of several possible explanations for the reduction in tremor and hypothermia, the most likely appears to be a potentiation of central adrenergic mechanisms in the hyperthyroid mice.
Role of pH in the coacervation of the systems: Gelatin - water - ethanol and gelatin - water - sodium sulphate
Authors: Khalil Saleh A H , Nixon J R , Carless J E 
Published: April 2011

Abstract
Phase boundary determination, coacervate volume measurements and analysis of the phases have been made to assess the influence of pH on the coacervation of gelatin solutions by ethanol and sodium sulphate. Coacervation was found to be pH dependent. In the ethanol system coacervation was noticeable only within a pH range in the vicinity of the isoionic point; at other pH values either a viscous gel phase or floccules occurred. In the sodium sulphate system, coacervation occurred at all pH values examined. The effect of pH in changing the overall charge on the gelatin molecule is explained in relation to the formation of gelatin coacervates. Finally, the role of the coacervate phase in the microencapsulation of oil and solid particulates is discussed.
Use of the analogue computer to examine the quantitative relation between urinary pH and kidney reabsorption of drugs partially ionized at physiological pH
Authors: Beckett A H , Boyes R N , Tucker G T 
Published: April 2011

Abstract
A method, involving the use of an analogue computer, is described for determining a quantitative relation between measured urinary pH and the kidney tubular reabsorption of certain drugs under normal conditions of fluctuating urinary pH. The method is based on the use of drug excretion versus time profiles under normal conditions and of absorption, metabolism and excretion rate constants, determined under conditions of controlled urinary pH, e.g. constant acidic pH (&lt;5) in the case of basic drugs. In support of the theoretical treatment, experimental results, using amphetamine as a model drug, are presented. The implications of the method are discussed with respect to the evaluation of drug formulations under normal urinary pH conditions.
The quantitative measurement of motor inco-ordination in naive mice using an accelerating rotarod
Authors: Jones B J , Roberts D J 
Published: April 2011

Abstract
A simple modification of the standard rotarod apparatus is described which eliminates the necessity of time-consuming training and consequently gives a truer measure of motor co-ordination since any effects on memory are avoided. The sensitivity and reproducibility of the procedure are much greater than those obtained with constant speed rotarods and less animals are required to obtain statistically significant results.
The stability of sucrose monolaurate: Rate of formation of lauric acid
Authors: Anderson R A , Polack A E 
Published: April 2011

Abstract
At concentrations below the critical micelle concentration, sucrose monolaurate hydrolyses to give lauric acid at first-order rates. At concentrations above the critical micelle concentration first-order kinetics are not obeyed. In systems buffered to pH values sufficiently high for the liberated lauric acid to ionize, the laurate ions appear to form mixed micelles with the ester and these carry negative charges. Coulombic repulsion of hydroxyl ions by these negative charges protects neighbouring ester molecules from attack and so reduces hydrolysis rates.
The effects of drug-induced adrenocortical deficiency and of mineralocorticoid drugs on anaphylaxis in the guinea-pig
Authors: HICKS R 
Published: April 2011

Abstract
Administration of adrenocortical inhibitors [metyrapone, amphenone-B, or 1,1-dichloro-2,2-di(p-chlorophenyl)ethane (DDD)] decreased anaphylactic preconvulsion times in guinea-pigs. Simultaneous corticotrophin treatment potentiated the effect of metyrapone. Metyrapone induced adrenocortical deficiency, and changed the character of corticosteroid secretion from predominantly glucocorticoid to mineralocorticoid. Mineralocorticoid treatment decreased preconvulsion times. Mepyramine prevented the effect of mineralocorticoids on anaphylaxis but did not modify the effect of metyrapone which probably resulted from glucocorticoid lack, but mineralocorticoid secretion may have contributed. Mineralocorticoids probably potentiated the histaminic component of anaphylaxis.
The colloidal properties of chlorhexidine and its interaction with some macromolecules
Authors: Heard D D , Ashworth R W 
Published: April 2011

Abstract
Surface tension, conductivity and dye solubilization experiments show that, in aqueous solution, chlorhexidine diacetate forms micelles and has a molar critical micellar concentration (CMC) of 0·010–0·011 at 25°. Similarly, the digluconate salt has a molar CMC of 0·0066. Above its CMC, the freely soluble digluconate salt solubilizes the less soluble diacetate salt. The formation of micelles does not affect the rate of hydrolysis of chlorhexidine to p-chloroaniline. It is suggested that the micelles formed by chlorhexidine resemble those formed by many dyes rather than those of colloidal surfactants. Equilibrium dialysis experiments show that 1·0 and 3·0% polysorbate 80 inactivates 37·5 and 70·0% respectively of the chlorhexidine in a 0·10% solution of the diacetate salt.
Gelatin coacervate microcapsules containing sulphamerazine: Their preparation and the in vitro release of the drug
Authors: Nixon J R , Khalil Saleh A H , Carless J E 
Published: April 2011

Abstract
An improved method is described for the preparation of gelatin coacervate microcapsules containing sulphamerazine as a fine deflocculated powder. The factors which control both the coacervation step and the recovery of the microcapsules are discussed. The in vitro release of sulphamerazine from microcapsules of different wall thickness which had been hardened by formaldehyde under different conditions has been studied. The method of preparation gave a high percentage of encapsulated material in comparison with other recovery techniques.
Interactions of narcotic antagonists and antagonist-analgesics
Authors: Blane G F , Dugdall D 
Published: April 2011

Abstract
In the rat the potent narcotic antagonist N-cyclopropylmethyl-6,14-endoethano-7α- (1-hydroxy-1-methylethyl)-tetrahydronororipavine (M5050, Reckitt), which itself lacks analgesic activity, resembled naloxone in its capacity to reverse the antinociceptive effects of morphine antagonist-analgesics. The nociceptive stimulus employed was bradykinin administered by an intra-arterial route. ED50 values were established for the reversal by M5050 of the analgesic effect of nalorphine, levallorphan, pentazocine and some newer compounds. When antagonist-analgesics were given concomitantly with morphine the response varied from antagonism of the analgesic effect of the morphine to synergism, depending on the dose combination.
The effect of antirheumatic drugs on the extractable collagen in lathyric chick embryos
Authors: Trnavský K , Trnavskñ Z 
Published: April 2011

Abstract
The lathyrogenic effect of 2·5 mg of β-aminopropionitrile in the chick embryo has been measured by the increase in the extractability of collagen from bones using M saline. Sodium salicylate (3 mg/embryo) and hydrocortisone (1·5 mg/embryo) applied 24 hr after the injection of β-aminopropionitrile decreased the elevated amount of soluble collagen. Phenylbutazone, chloroquine diphosphate and sodium aurothiosulphate were ineffective in this experimental system.
Subcellular distribution of [3H]amphetamine and [3H]guanethidine and their interaction with adrenergic neurons
Authors: Obianwu H O , Stitzel R , Lundborg P 
Published: April 2011

Abstract
The subcellular distribution of [3H]amphetamine and [3H]guanethidine and their interaction with each other and with noradrenaline binding sites have been examined. The ratio p/(p + s) × 100, an indication of affinity for noradrenaline storage particles, for [3H]amphetamine and [3H]guanethidine was 12% and 57% respectively. Protriptyline, a substance which inhibits amine transport mechanism at the level of the cell membrane, i.e. the membrane pump, and reserpine, an agent which impairs incorporation of amines into the storage particles in the adrenergic nerve fibre, inhibited the uptake and storage respectively, of [3H]guanethidine more than that of [3H]amphetamine. Retention of [3H]guanethidine by rat salivary glands was markedly decreased by sympathetic denervation of the glands while that of [3H]amphetamine was not. The results suggest that guanethidine possesses a much higher affinity for noradrenaline binding sites than amphetamine.
Activity of centrally acting drugs on amphetamine metabolism
Authors: Valzelli L , DOLFINI E , Tansella M , Garattini S 
Published: April 2011

Abstract
Amitriptyline, nortriptyline and dibenzepine prolong the increase in temperature produced by amphetamine in rats and also increase the level of brain amphetamine above that effected by amphetamine alone. After chlorpromazine and propericiazine, brain amphetamine levels are also higher but the rise of body temperature elicited by amphetamine is inhibited. Phenelzine prolongs and α-methyl-p-tyrosine inhibits the rise in body temperature without modifying the accumulation of brain amphetamine. In reserpinized rats amphetamine causes a temperature increase several degrees greater than in control animals although its level in the brain is lower.
The effects of diethyldithiocarbamate and L-dopa on body temperature in mice
Authors: Barnett A , Taber R I 
Published: April 2011

Abstract
Diethyldithiocarbamate (ddtc) raises body temperature in reserpinized mice, an effect that is unlikely to be an intrinsic action of the compound since ddtc lowers temperature in normal mice. ddtc has no effect on body temperature of reserpinized rats. The effects of ddtc on body temperature in normal and reserpinized mice are mimicked qualitatively by l-dopa indicating that the effects may reflect increased dopamine levels. Pargyline pretreatment does not influence the hypothermia produced by ddtc.
The role of the tissues and gut micro-organisms in the metabolism of [14C]protocatechuic acid in the rat. Aromatic dehydroxylation
Authors: Dacre J C , Williams R T 
Published: April 2011

Abstract
The fate of oral doses (0·1 g/kg) of [carboxy-14C]3, 4-dihydroxybenzoic (protocatechuic) acid in normal and neomycin-treated rats has been studied. In normal rats about 72% of the dose of 14C is excreted in 7 days (about 64% in urine and 8% in faeces) whereas in neomycin-treated rats 99% is excreted (87% in urine and 12% in faeces). In normal rats, the radioactive metabolites found in the urine excreted in 24 hr after dosing were protocatechuic acid (36%), vanillic acid (21%), m-hydroxybenzoic acid (2·1%), p-hydroxybenzoic acid (1·2%) and m-methoxybenzoic acid (2%). After neomycin-treatment protocatechuic acid (55%) and vanillic acid (22%) were found, but the other three were virtually absent. Incubation of [14C]protocatechuic acid with rat intestinal contents yielded 14CO2 and small amounts of m- and p-hydroxybenzoic acid. When [14C]protocatechuic acid was injected intraperitoneally into biliary cannulated rats about 13% appeared in the bile mainly as the 4-O-glucuronide of vanillic acid. It is concluded that, whilst the conjugation and methylation of protocatechuic acid occurs in the tissues of the rat, the dehydroxylation and decarboxylation of the acid is carried out by the gut micro-organisms.
The role of the tissues and gut flora in the metabolism of [14C]homoprotocatechuic acid in the rat and rabbit
Authors: Dacre J C , Scheline R R , Williams R T 
Published: April 2011

Abstract
The fate of orally administered [carboxy-14C]3, 4-dihydroxyphenylacetic (homoprotocatechuic) acid has been studied in normal and neomycin-treated rats and rabbits. In normal rats about 93% of the dose (0·1 g/kg) is excreted in 13 days after dosing, although 80% is excreted in the urine within 2 days. In neomycin-treated rats 100% of the 14C is excreted in 13 days, 95% being in the urine within 2 days. The urinary metabolites in 44 hr in normal rats were unchanged homoprotocatechuic acid (55% of the dose), homovanillic acid (19%), m-hydroxyphenylacetic acid (6·5%) and p-hydroxyphenylacetic acid (1·4%). In neomycin-treated rats, homoprotocatechuic acid (70%) and homovanillic acid (22%) were found but the other two metabolites were virtually absent. In normal and neomycin-treated rabbits, the 14C was excreted in the urine almost quantitatively in 9 days. The same metabolites as in rats were excreted, but there was more m-hydroxybenzoic acid (14%) and less homovanillic acid (6%). In neomycin-treated rabbits the excretion of m- and p-hydroxyphenylacetic acids was suppressed. In the rat, the metabolism of homoprotocatechuic acid, as far as methylation, dehydroxylation and decarboxylation (Scheline, 1967) is concerned, is qualitatively similar to that of protocatechuic acid (Dacre & Williams, 1968). In the rabbit, however, there is little, if any, decarboxylation. Whilst methylation is a reaction of the tissues, dehydroxylation and decarboxylation appear to be carried out by gut micro-organisms.
Effect of crystal form, cortisone alcohol and agitation on crystal growth of cortisone acetate in aqueous suspensions
Authors: Carless J E , Moustafa M A , Rapson H D C 
Published: April 2011

Abstract
Particle size distribution in aqueous suspensions of stable and unstable crystal forms of cortisone acetate under conditions of agitation and different degrees of saturation with cortisone alcohol is described. Agitation accelerated the diffusion-controlled processes of dissolution and crystallization, leading to the formation of a high proportion of large particles. Cortisone alcohol inhibited the polymorphic transformation necessary for the crystal growth and formation of the water-stable form. The mechanism of action is discussed.
The constituents of the seeds of Asphodelus microcarpus Viviani and A. fistulosus L.
Authors: Fell K R , Hammouda F M , Rizk A M 
Published: April 2011

Abstract
Evidence is presented that β-sitosterol and β-amyrin can be separated from the fixed oil of seeds of A. microcarpus Viviani and A. fistulosus L. by thin-layer, column and gas-liquid chromatography, together with other minor sterols (campesterol and stigmasterol). Myristic, palmitic, stearic, oleic and linoleic acids were identified in the oil of both species by thin-layer and gas-liquid chromatography. Sucrose, raffinose and stachyose were indicated in seeds of both species, also melibiose in seeds of A. microcarpus. Colchicine was not found in either species.
The uptake and retention of [3H]noradrenaline in rat sciatic nerves after ligation
Authors: Dahlström Annica , Waldeck Bertil 
Published: April 2011

Abstract
The uptake and retention of [3H]noradrenaline (3H-NA) was examined in sciatic nerves of albino rats. In the 1 cm part of nerve proximal to a 12 hr ligation the uptake and retention of exogenous noradrenaline was about 4 times the uptake in 1 cm of normal unligated nerves. Treatment with reserpine 10 hr before killing caused a marked decrease in the estimated amount of 3H-NA, while injection of nialamide 15 min before 3H-NA administration in ligated, reserpine-treated animals caused a somewhat larger uptake and retention of 3H-NA in the nerve part above the ligation. Protriptyline, a blocker of the “membrane pump”, was approximately 3 times less effective in 12 hr-ligated nerves than in unligated nerves, indicating a reduced efficiency of the “membrane pump” in the distended axons above a ligation.
Peptic inhibition by macroanions
Authors: Anderson W , Baillie A J , Harthill J E 
Published: April 2011

Abstract
Heparin, dextran sulphate, dextran phosphate, chondroitin sulphate and degraded Λ-carrageenan inhibit peptic activity by substrate occlusion or depletion. This holds for various substrates and enzyme preparations, but the amount of inhibition observed varies with method and inhibitor used. The most active inhibitors of the series are disulphated on at least alternate sugar residues and in addition to disulphation high molecular weight confers, in certain conditions, greatest activity. High and low molecular weight macroanions have different inhibition characteristics and it is concluded that activity may depend upon the structure of the substrate-inhibitor complexes formed. Inhibition is not observed when substrate-inhibitor interaction does not occur, as when pepsin or N-acetyl-L-phenylalanine-L-diiodotyrosine (APDT) are used as substrate.
The bactericidal effect of silver ions on Pseudomonas aeruginosa
Authors: Brown M R W , Anderson R A 
Published: April 2011

Abstract
THERE are frequent reports of Pseudomonas aeruginosa infections in hospitals, with contamination of hospital equipment and pharmaceutical preparations (Editorial, 1967). Cason, Jackson & others (1966) report a high incidence of this organism in burn patients and found silver nitrate compresses to be an effective prophylactic measure.
Little information is available on the action of silver ions on Ps. aeruginosa, and the present communication reports the initial stages of such a study. Using cultures whose growth was eventually limited by the magnesium concentration in the culture medium, Brown & Melling (1968) found that Ps. aeruginosa resistance to EDTA was related to the degree of magnesium-limitation. We have examined the effect of magnesium-limitation on sensitivity to silver.