bluuebunny/crossref_metadata_2025_split huggingface dataset:
Identification and quantitative determination of some metabolites of methadone, isomethadone and normethadone
Authors: BECKETT A H , MITCHARD M , SHIHAB A A 
Published: April 2011

Abstract
Isomethadone and normethadone are metabolized by microsomal preparations of guinea-pig liver to yield 2-ethyl-1,4-dimethyl-3,3-diphenyl-1-pyrroline and 2-ethyl-1-methyl-3,3-diphenyl-1-pyrroline respectively. The structures of the pyrrolines were established (by comparison with the pyrroline derived from methadone) by thin-layer chromatography and by infrared and nuclear magnetic resonance spectral data. Methadone, isomethadone and normethadone are also metabolized to the corresponding N-oxides. A gas chromatographic procedure for the quantitative determination of unchanged drugs, cyclic metabolites and N-oxides of methadone, isomethadone and normethadone in microsomal homogenates is described. The N-oxides were reduced before analysis.
The distribution of methadone in man
Authors: ROBINSON ANN E , WILLIAMS FAITH M 
Published: April 2011

Abstract
The distribution of methadone and its metabolite, 1,5-dimethyl-3,3-diphenyl-2-ethylidene pyrrolidine, in man, postmortem, is presented. Quantitative data for methadone and the metabolite in blood, bile, urine, liver, kidney, spleen, lung and brain samples show that methadone blood concentrations range from 0·22–3·04 μg/ml and are less than in bile and urine. The metabolite is found particularly in bile and urine. The liver and kidney concentrations are approximately equivalent unless the survival time is reduced by the presence of another CNS-depressant drug. Lung tissue is the richest source of methadone and brain the poorest. Chromatographic data for three other methadone metabolites are included.
A note on the influence of diet in West Africa on urinary pH and excretion of amphetamine in man
Authors: WESLEY-HADZIJA B 
Published: April 2011

Abstract
The urinary excretion of amphetamine was examined after the oral administration of (+)-amphetamine sulphate to two groups of subjects whose urinary pH fluctuated about mean acidic or alkaline values due to their different diets. The group with a balanced protein diet giving acidic urine, excreted much more drug unchanged than the group with a low protein diet giving alkaline urine. A small increase in protein intake in the group with alkaline urine made their urine pH acidic in a few days and increased their excretion of amphetamine to the same level as the group with acid urine.
Decomposition of methoxamine in aqueous solution: Identification of the decomposition products
Authors: MILLARD B J , PRIAULX D J , SHOTTON E 
Published: April 2011

Abstract
Combined gas-liquid chromatography-mass spectrometry is used to study the decomposition of methoxamine. The major breakdown product in aqueous solution under air is shown to be 2,5-dimethoxy-benzaldehyde.
Structural differences in solutions derived from polymorphic modifications of aspirin
Authors: KILDSIG DANE O , DENBO RICHARD , PECK GARNET E 
Published: April 2011

Abstract
Differences in the structure of solutions derived from two polymorphic modifications of aspirin were demonstrated through differences in apparent pKa values. The apparent pKa's were determined in dimethylformamide using tetrabutyl-ammonium hydroxide as the titrant. The pKa differences were ascribed to differences in intra- and intermolecular hydrogen bonding of the solute.
Δ1-Tetrahydrocannabinolic acid, an important component in the evaluation of cannabis products
Authors: DE ZEEUW R A , MALINGRÉ TH M , MERKUS F W H M 
Published: April 2011

Abstract
The occurrence and some analytical properties of Δ1-etrahydrocannabinolic acid have been investigated, including its chromatographic behaviour in the presence of other cannabinoids. The acid is inactive but is converted on smoking into the active tetrahydrocannabinol. The acid is present in abundant amounts in various cannabis samples, marihuana in particular, and these will be more active on smoking than when administered by injection or orally. A method for the separate determination of tetrahydrocannabinol and its acid is also described.
The biliary excretion of tartrazine. Sex differences in the rat and species differences in the rat, guinea-pig and rabbit
Authors: GREGSON R H S , HIROM P C , MILLBURN P , SMITH R L , TURBERT H B , WILLIAMS R T 
Published: April 2011

Abstract
The excretion of tartrazine in the bile and urine has been studied in biliary cannulated rats, rabbits and guinea-pigs. This dye is excreted unchanged by these species. In the rat a sex difference in the relative amounts of tartrazine excreted in bile and urine has been found. Male rats excrete in 3 h about 17 % of an intravenous dose (50 μmol/kg) in the bile and about 70% in the urine, whereas females excrete about 40 and 45 % respectively. The biliary excretion of tartrazine in the rat appears to be influenced by dose level, for at the lower level of 4.5 μmol/kg male rats excrete about 9 % of an intravenous dose in the bile and 64% in the urine in 3 h, the corresponding values for female rats being 30% and 50%. There is also a species difference in the extent of biliary excretion of tartrazine (50 μmol/kg intravenously). The female rat and female guinea-pig excrete in 3 h about 40 % of the dose in the bile and a similar amount in the urine whereas the female rabbit excretes only 6% in the bile and nearly 70% in the urine. Previous work in this laboratory has shown that molecular weight is an important factor in the biliary excretion of foreign compounds and the present results fit in with this view.
A possible relation between pKa1 and lipid solubility and the amounts excreted in urine of some tobacco alkaloids given to man
Authors: BECKETT A H , GORROD J W , JENNER P 
Published: April 2011

Abstract
The amount of unchanged (—)-nicotine, (—)-nornicotine, (—)-methylanabasine and (—)-anabasine excreted in the urine after oral administration to man was dependent on urinary pH while that of (—)-cotinine depended on urinary pH and on urine flow rate. No unchanged β-nicotyrine, β-nornicotyrine or myosmine was detected in urine. More nornicotine and anabasine than their corresponding tertiary amines nicotine and methylanabasine were excreted unchanged in the urine. Correlations of pKa1 and lipid solubility and the urinary excretion of these compounds were made.
The effect of sugars on the temperature dependence of the critical micelle concentrations of cationic surfactants
Authors: ADDERSON J E , BUTLER C G 
Published: April 2011

Abstract
The temperature dependence of the critical micelle concentrations (cmc) of decyl, dodecyl and tetradecyl trimethylammonium and dodecyl benzyl dimethylammonium bromides in the presence of glucose or sucrose is reported. Thermodynamic parameters have been calculated using the uncharged phase-change model. An interpretation of the changes in cmc values, relative to those in simple aqueous solutions, is offered in terms of the resultant of two effects, namely modifications in water-structure and reduction of dielectric constant.
The absorption from the gut of quinine and chlorpheniramine given with various anionic agents
Authors: SUZUKI E , TSUKIGI M , MURANISHI S , SEZAKI H , KAKEMI K 
Published: April 2011

Abstract
The absorption of quinine and chlorpheniramine with anionic agents was examined in the rat rectum, small intestine and stomach. The enhancement of absorption was related to partition behaviour, to the organic solvent, and surface activity of ion-pair complexes, but it seems that with results from these properties alone it is not possible to explain the apparent increase in the in situ absorption of amines. In the presence of anionic agents, the absorption of amines was enhanced at all sites examined and kinetically the uptake to the mucosal membrane was increased in the rectum and small intestine. The effect of anionic agents on the uptake of amines was greater in the rectum than in the small intestine and this may be related to differences in the nature of the gut wall.
The preservation of ophthalmic solutions with antibacterial combinations
Authors: RICHARDS R M E , MCBRIDE R J 
Published: April 2011

Abstract
Solutions of pilocarpine, atropine and physostigmine preserved with benzalkonium, chlorhexidine, phenylmercuric nitrate (PMN), chlorocresol and chlorbutol in simple solution and in combination with either phenylethanol or disodium edetate (EDTA), were contaminated on two separate occasions with high inocula of P. aeruginosa. Phenylethanol-antibacterial combinations were consistently effective in killing the inoculum within 15 min except for one formulation with chlorhexidine and physostigmine salicylate and formulations with PMN for which sterilization times ranged from 30 to 90 min.
Effect of neuroleptic drugs on central catecholamine turnover assessed using tyrosineand dopamine-β-hydroxylase inhibitors
Authors: ANDÉN NILS-ERIK , CORRODI HANS , FUXE KJELL 
Published: April 2011

Abstract
The effects of some neuroleptic drugs on the noradrenaline turnover in the rat brain and spinal cord were studied biochemically and histochemically with the help of a new inhibitor of the enzyme dopamine-β-hydroxylase, bis(4-methyl-1-homopiperazinyl-thiocarbonyl) disulphide; (FLA-63). Haloperidol (1 mg/kg, i.p.), chlorpromazine (5–10 mg/kg, i.p.), pimozide (1–5 mg/kg, i.p.) and fluspirilene (1–5 mg/kg, i.p.) produced an acceleration of the noradrenaline disappearance induced by FLA-63. Clothiapine (1 mg/kg, i.p.) was ineffective. The lowering of brain dopamine after treatment with α-methyltyrosine methylester (H44/68) was markedly enhanced by haloperidol (5 mg/kg, i.p.) and slightly so by chlorpromazine (5 mg/kg, i.p.), whereas both drugs simultaneously caused a significant increase in the noradrenaline loss. Thus, the same results were obtained with dopamine-β-hydroxylase and tyrosine-hydroxylase inhibition on the influence of neuroleptic drugs on the noradrenaline turnover. The acceleration seen after haloperidol and chlorpromazine, but not after pimozide and fluspirilene, could be due to a compensatory activation of noradrenaline neurons produced by a noradrenaline receptor blockade.
The influence of replacement of the N-ethyl group by the cyanoethyl group on the absorption, distribution and metabolism of (±)-ethylamphetamine in man
Authors: BECKETT A H , SHENOY E V B , SALMON J A 
Published: April 2011

Abstract
N-2-Cyanoethylamphetamine in man was metabolized rapidly and extensively, as indicated by the analysis of the drug and its metabolite in urine, under acidic and normal conditions. A comparison with the excretion and metabolism of ethylamphetamine under comparable conditions was made. The results were assessed using an analogue computer; a simple one compartmental model sufficed to describe the excretion and metabolism of ethylamphetamine and amphetamine but the additional programming of free amphetamine was necessary for cyanoethylamphetamine because of its very rapid metabolism to amphetamine.
The properties of tablets manufactured on an automatically-controlled rotary machine
Authors: RIDGWAY K , LAZAROU C , THORPE E E 
Published: April 2011

Abstract
Four direct-compression bases: Celutab in the hydrous and the anhydrous form, Emcompress Special, and spray-dried lactose, have been compared with a traditional lactose granulation with respect to initial physical properties of the powder, tabletting performance and the characteristics of the tablets produced. The tablets were made on an instrumented rotary machine with feedback weight control operating to minimize time-dependent change within a batch, compression force being continuously monitored. Tensile strength by diametral crushing, porosity, disintegration time and surface indentation hardness were assessed and correlated with changes in compaction force, machine speed and tablet thickness. All materials gave wellformed tablets with no evidence of capping between 90 and 350 MN m−2, and weight variation was small except for Emcompress Special at the highest machine speed, when die filling became erratic.
Comparative investigation of inhibitors of extracerebral dopa decarboxylase in man and rats
Authors: KURUMA I , BARTHOLINI G , TISSOT R , PLETSCHER A 
Published: April 2011

Abstract
The decarboxylase inhibitor Ro 4–4602 [N1-(dl-seryl)-N2-(2,3,4-trihydroxybenzyl)hydrazine] in doses of 3.4–34.0 μmol/kg (1–10mg/kg) progressively enhances the increase of dopa and 3-O-methyldopa and diminishes the rise of phenolcarboxylic acids in human plasma induced by administration of l-dopa. A dose of 3.4 μmol/kg Ro 4–4602 is approximately equipotent to 17.0 μmol/kg MK 485 [β-(3,4-dihydroxyphenyl)-α-hydrazino-α-methyl-dl-propionie acid]. Ro 4–4602, combined with 2 mg/kg l-dopa, causes a higher increase of catecholamines than 20 mg/kg l-dopa alone in the striatum and probably in the hypothalamus of rat brain, whereas in the other brain areas the amine rise is equal after both treatments. MK 485 in doses equimolar to Ro 4–4602 has a less marked effect in all brain areas. Either inhibitor (10–2 μmol/kg) combined with 2 mg/kg l-dopa causes markedly less increase of catecholamines than 20 mg/kg l-dopa alone in the rat heart. Ro 4–4602, in small single doses, used at present in the treatment of Parkinson's syndrome, markedly inhibits the extracerebral decarboxylation of l-dopa in man and rats and is more potent than MK 485.
Desoxyisoprenaline: an adrenoceptor stimulating and blocking agent
Authors: MAENGWYN-DAVIES GERTRUDE D , FLEISCH JEROME H , PRUSS T P 
Published: April 2011

Abstract
Desoxyisoprenaline (N-isopropyldopamine, DOI), an optically inactive analogue of isoprenaline, which lacks the alcoholic -OH group, was shown to stimulate β-adrenoceptors in cat papillary muscle, rat aorta and rat trachea, in addition to causing a hypotensive effect in anaesthetized cats. DOI was also shown to stimulate α-adrenoceptors in rat aorta. Furthermore, DOI blocked both α- and β-adrenoceptors in rabbit aortic strips and β-adrenoceptors in rat trachea. These different actions indicate that DOI has both adrenoceptor stimulating and blocking properties.
Responses of blood vessels to various amines applied by microiontophoresis
Authors: STONE T W 
Published: April 2011

Abstract
Various amines have been applied to arterioles of the rat intestine and mesentery by microiontophoresis. Noradrenaline produced a profound constriction with a long latency and time course. This effect was prevented by phentolamine but not by propranolol. Histamine caused a partial relaxation of noradrenaline-constricted vessels, but had no apparent action on “normal” vessels. Acetylcholine and methacholine had no apparent effect on the vessels. The results are discussed in relation to previous findings. It is suggested that the effects of microiontophoretically applied amines on blood vessels may be of importance in studies of the actions of these substances in the central nervous system using this technique.
Application of orthogonal functions to the determination of naphazoline
Authors: ABDINE H , WAHBI A M , KORANY M A 
Published: April 2011

Abstract
A rapid method for the determination of naphazoline in antazoline- naphazoline drops is discussed. The method depends upon precipitating antazoline by a solution of sodium carbonate. Naphazoline is determined in the filtrate using (i) the modified Vierordt method and (ii) Glenn's method of orthogonal functions to correct for the unprecipitated fraction of antazoline.
The fate of [14C]disodium cromoglycate in man
Authors: WALKER S R , EVANS MARION E , RICHARDS A J , PATERSON J W 
Published: April 2011

Abstract
The fate of [14C]disodium cromoglycate (DSCG) has been examined in 12 asthmatic patients. Maximum plasma concentrations (mean 9.2 ng/ml) were obtained within 15 min of inhaling DSCG (20 mg) and the average plasma half-life was 81 min. Although absorption from the lung is rapid, most of the inhaled dose is swallowed. Only 2.0% of the dose was excreted in the urine, and 84% was recovered from the faeces. DSCG is poorly absorbed from the gastrointestinal tract, only 0.4 % of an oral dose (20 mg) appeared in the 24 h urine and 83 % was recovered from the faeces. Intravenous administration of DSCG resulted in approximately equal amounts (30–50% of dose) being excreted via the urine and faeces. No metabolites of DSCG were detected chromatographically.
The pharmacokinetics of inulin and urea: a comparison of the dose eliminated from a compartmental model and that eliminated in urine
Authors: BOURNE G R , BARBER H E 
Published: April 2011

Abstract
The distribution kinetics of inulin and urea were studied in the male rat to test the validity of a proposed compartmental model. The plasma curves could be adequately described by a biexponential function. For inulin, analysis of the results gave valid parameters in terms of an open two compartment model. These parameters did not necessarily predict the amount eliminated from the central compartment but did so under constant clearance conditions after allowance for a time lag between filtration and appearance of the drug in the collecting vessel. A triexponential fit interpreted in terms of a three compartmental model described the urea data.
Cholinesterase activity in the plasma and acid- secretory gastric mucosa of normal, castrated, and castrated oestrogen-treated male rats
Authors: OMOLE A A 
Published: April 2011

Abstract
Cholinesterase activity in plasma and fundic mucosa of male, normal, castrated, and castrated and oestrogen-treated rats has been measured. Castration significantly elevated cholinesterase activity in both plasma (0.02&lt;P&lt;0.05) and fundic mucosa (P&lt;0.001). Castrated rats given 17β-oestradiol (120 μg, s.c. daily for 10 days) had enzyme activity in plasma and fundus not significantly different from that in normal rats.
Serum and brain concentrations of pentazocine in relation to analgesic activity in mice
Authors: PAALZOW LENNART , ARBIN ASTRID 
Published: April 2011

Abstract
Serum and brain concentrations of pentazocine and its metabolite, the trans-alcohol, have been studied in mice and related to analgesic activity. The concentrations were determined fluorometrically after extraction and isolation of the compounds by partition chromatography as ion pairs. The acute intravenous toxicity (LD50) of the drug was also determined. The analgesic activity was found to reside in the unchanged pentazocine since, after the initial distribution phase, the drug elicits a higher degree of analgesia in animals showing higher brain concentrations of pentazocine. Furthermore, animals which did not show an analgesic response had higher serum concentrations of the trans-alcohol in comparison with animals showing analgesic activity, indicating a relation between analgesia and the degree of metabolism. However, the relation between the analgesic response and the brain concentration during the first 20 min after intravenous injection of the drug was poor.
Effects of a bicyclic thymoleptic drug (LU 3–010) on neuroerfector function in rat isolated portal veins
Authors: HÄGGENDAL J , JOHANSSON B , JONASON J , LJUNG B 
Published: April 2011

Abstract
The effects of the thymoleptic drug, LU 3–010, on adrenergic transmitter release and reuptake and on effector cell function in rat isolated portal veins have been investigated. The contractile response to exogenous noradrenaline was potentiated by LU 3–010 and its concentration-effect curves after LU 3–010 10−7 g/ml were displaced to the left to a similar extent as had been found in chronically denervated preparations, indicating efficient blockade of the membrane pump mechanism. LU 3–010 10−7g/ml slightly potentiated the neurogenic response to electrical field stimulation, whereas 10−6 g/ml or more reduced the neural effector response in a concentration- dependent manner. The output of radioactive material per nerve impulse after incubation with 3H-NA was also studied. At 10−7 and 3 × 10−7 g/ml of LU 3–010 no significant change in transmitter overflow was observed. At 10−6 g/ml there was a decrease in the “fractional release”, suggesting that LU 3–010 concentrations of 10−6 g/ml or higher reduce transmitter release. Evidence is also given for a direct inhibitory effect of LU 3–010 on the smooth muscle.
Synergistic action of pyrazole on ethanol incoordination: differential metabolic and central nervous system effects
Authors: GOLDBERG L , HOLLSTEDT C , NERI A , RYDBERG U 
Published: April 2011

Abstract
The influence of pyrazole on ethanol-induced incoordination was measured by a modified tilting-plane technique. Pyrazole (1–77 mmol/kg; 120 mg/kg) and/or ethanol (32.6 mmol/kg; 1.5 g/kg) was given intraperitoneally to rats. Impairment of coordination was related to blood ethanol concentrations. The mean maximal impairment was significant in all conditions. For ethanol alone the maximal impairment was 8.7%, for pyrazole alone 4.8% and for ethanol + pyrazole 16.5 %. Ethanol alone induced a total impairment, assessed planimetrically, of 530 units. Pyrazole alone induced an impairment gradually increasing with time (totally 1070 units). When pyrazole was combined with ethanol, the rate of ethanol elimination was reduced by 81%, and the time it remained in the blood was prolonged from 196 ± 11 to 850 ± 16 min. The rate of disappearance was reduced from 8.05 to 1.57 μg/ml per min. The total impairment increased to 5600 units, indicating a synergistic interaction between ethanol and pyrazole, which is contrary to the normalizing effects of pyrazole on ethanol-induced metabolic changes. A “post-drug” impairment was observed one week after pyrazole, while no such effects were found after repeated administration of saline or ethanol alone in control animals. Thus, pyrazole showed acute and long-term toxic eifects.
Mouse caecum as a selective β-adrenoceptor tissue
Authors: KAUL PUSHKAR N , WHITTLE SHEILA J 
Published: April 2011

Abstract
The mouse isolated caecum has been found to contain β-adrenoceptors and 5-hydroxytryptamine receptors. Conditions for optimum function of the tissue in an isolated environment are described. The preparation is sturdy, lasting, economic and dependable for the screening of potential drugs, possessing agonistic or antagonistic activity on the extra-cardiac β-adrenoceptors.
Some factors affecting the absorption of paracetamol
Authors: MCGILVERAY I J , MATTOK G L 
Published: April 2011

Abstract
Blood concentration and urinary excretion data demonstrated that subjects who had ingested 1 g of paracetamol after fasting overnight absorbed the drug up to 5 times more rapidly but to the same extent as when they ingested the drug after a substantial high carbohydrate breakfast. Subjects who had ingested 1 g of paracetamol immediately before sleep at night excreted up to 36% less than when they took the drug at 8.30 a.m.