bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effect of enamine derivatives on the rectal absorption of insulin in dogs and rabbits
Authors: Kim Suni , Kamada Akira , Higuchi Takeru , Nishihata Toshiaki 
Published: April 2011

Abstract
Enamine derivatives resulting from the reaction between ethyl acetoacetate and amino acids were found to promote rectal absorption of insulin in normal rabbits, with the enamine of sodium DL-phenylalanate being the most effective adjuvant tested. Results of glucose tolerance tests in fasted alloxan diabetic rabbits showed that after oral administration of glucose, insulin suppositories containing enamines derived from either sodium phenylalanine or leucine were able to lower the serum glucose level to within the normal range for more than 2.5 h. The absorption-promoting effect of the sodium DL-phenylalanate enamine on rectal absorption of insulin in dogs was studied in two different formulations, gelatin microenema and suppository. The gelatin microenema containing the insulin solution caused a greater increase in the plasma insulin level than that obtained after administration of an insulin suppository.
Influence of prostacyclin and indomethacin on castor oil-induced gastrointestinal effects in rats
Authors: Vischer P , Casals-Stenzel J 
Published: April 2011

Abstract
The effects of castor oil, alone, as well as in combination with PGI2 and indomethacin on gastrointestinal functions have been examined in rats. Oral administration of the oil to fasted rats induced severe diarrhoea, with increased intestinal motility and fluid volume. Pretreatment with PGI2 (s.c.) inhibited the effect of the oil on intestinal fluid accumulation and decreased intestinal motility below control values, but only delayed the occurrence of mucoid diarrhoea. Indomethacin (i.p.) reduced the accumulation in intestinal fluid after castor oil administration to a much smaller extent (47%) than PGI2 and depressed the increased intestinal motility to control values. In contrast to PGI2, indomethacin inhibited the occurrence of diarrhoea after administration of castor oil. The present results do not definitely confirm the general opinion that the diarrhoeal action of laxative agents is due only to an altered intestinal electrolyte and water transport or an increase of intestinal motility.
Absorption of moisture by sodium cromoglycate and mixtures of sodium cromoglycate and lactose
Authors: Chan S Y , Pilpel N 
Published: April 2011

Abstract
The presence of up to about 15% w/w moisture has little effect on the tensile and shear properties of sodium cromoglycate and of 1:1 mixtures of sodium cromoglycate and lactose. Analysis of their adsorption and desorption isotherms using equations developed by Young and Nelson shows that this is because most of the moisture is absorbed into the interior of the sodium cromoglycate leaving little adsorbed moisture on the surfaces of the particles concerned.
Effect of anti-inflammatory drugs on partitioning characteristics of propranolol and oxprenolol
Authors: Parkin John E 
Published: April 2011

Abstract
The influence of a range of nine anti-inflammatory drugs on the octan-1-ol aqueous phosphate buffer pH 7·4 apparent partition coefficients of propranolol and oxprenolol has been examined. All produced a change in the apparent partition coefficient which can be explained in terms of partitioning of hydrophobic ion-pairs formed between the ionic anti-inflammatory compound and the protonated cationic drug.
Inhibition of cholinergic response by taurine in frog isolated skeletal muscle
Authors: Lehmann Anders , Hamberger Anders 
Published: April 2011

Abstract
Carbamylcholine-stimulated contractions of isolated frog gastrocnemius muscle were inhibited in a non-competitive fashion by 5–25 mm taurine. Taurine had no effect on the resting length of the muscle. Caffeine-induced contractures were unaffected by taurine which indicates that the sarcoplasmic reticulum is not an important site of action for taurine. A possible functional role for taurine in skeletal muscle is discussed.
The opioid κ-selective compound U−50,488H does not inhibit intestinal propulsion in rats
Authors: Tavani Alessandra , Gambino Maria Concetta , Petrillo Paola 
Published: April 2011

Abstract
The selective κ-compound U−50,488H, at doses producing strong central pharmacological effects (0·5–32 mg kg−1 i.p.) did not delay the intestinal transit of a charcoal meal and had little or no antagonist action against morphine-induced constipation. It appears that κ-opioid receptors are probably not involved in the mechanisms responsible for opioid-induced constipation.
Neuronal deamination of endogenous and exogenous noradrenaline in the mesenteric artery of the spontaneously hypertensive rat
Authors: Head R J , Cassis L A , Barone S , Stitzel R E , De La Lande I S 
Published: April 2011

Abstract
The noradrenaline (NA) content of the mesenteric arteries from spontaneously-hypertensive rats (SHR) are greater than those in arteries from normotensive Kyoto Wistar rats (WKY). The possibility that impaired neuronal monoamine oxidase (MAO) activity in mesenteric arteries from SHR rats was responsible for the differences in NA content was explored. The in-vitro formation of dihydroxyphenylethylene glycol (DOPEG) by intact segments of mesenteric arteries was used as an index of neuronal MAO activity. There were no differences in the production of DOPEG from endogenous NA by arteries from normotensive and hypertensive rats. Moreover, the formation of DOPEG from exogenous NA was similar in arteries from SHR and WKY rats. The neuronal uptake of NA was indistinguishable between mesenteric arteries from SHR and WKY rats. The results argue against an impairment of neuronal MAO in contributing to the enhanced content of NA in the mesenteric artery of the SHR rat.
The effects of binder film characteristics on granule and tablet properties
Authors: Reading Susan J , Spring M S 
Published: April 2011

Abstract
The physical properties of cast films of four polymers, which are used as binders in tableting, have been determined. Films were equilibrated at different relative humidities and tested both in tension, at three rates of strain, and by the use of indentation to determine creep compliance and hardness of the film under load. Granules and compacts have also been made using the four polymers as binders and the properties of these have been measured. One of the polymers, starch, formed a paste that was difficult to mix adequately. With the other three polymers a positive correlation was found between compact crushing strength and the creep compliance, the ultimate tensile strength and the elongation at fracture of the cast films. A negative correlation was found between the compact crushing strength and the Brinell Hardness of the films.
Effect of omeprazole and polyethylene glycol−400 on antipyrine elimination by the isolated perfused rat liver
Authors: Webster Lorraine K , Jones D Brian , Mihaly George W , Smallwood Richard A 
Published: April 2011

Abstract
The effect of the substituted benzimidazole, omeprazole, a potent inhibitor of gastric acid secretion, on the hepatic elimination of antipyrine was studied in the rat isolated perfused liver. Bolus dosage (10 mg in 100 ml perfusate) and infusions (1 μg ml−1 perfusate concentrations) of omeprazole in its solvent, polyethylene glycol−400 (PEG−400), reduced antipyrine clearance by approximately one third (P &lt; 0·05). PEG−400 alone caused a 15% decrease in antipyrine clearance (P &gt; 0·10), indicating that the effect seen with omeprazole was at least partly due to the vehicle of dissolution. A significant but mild choleresis was noted in all preparations (P &lt; 0·01) exposed to PEG−400. We conclude that the effect of omeprazole on hepatic drug elimination in patients warrants further study.
‘Superactivation’ of alkaline phosphatase activity by cycloheximide in rat hepatoma cell cultures
Authors: Sorimachi Kenji , Mizuno Hideaki , Yasumura Yosihiro 
Published: April 2011

Abstract
We have found that rat hepatoma cells (R-Y121B) retain alkaline phosphatase activity, and that this enzyme activity is increased by cycloheximide. Actinomycin D also increased the enzyme activity. This increase due to actinomycin D was partially inhibited by cycloheximide. The characteristics of alkaline phosphatase of the cells treated or untreated with cycloheximide or actinomycin D were similar to each other; they were heat labile and the enzyme reaction was strongly inhibited by l−homoarginine, but weakly by l−phenylalanine. The increase in alkaline phosphatase activity with cycloheximide has been termed a ‘superactivation’ of alkaline phosphatase.
Physiological disposition of oral piracetam in Sprague-Dawley rats
Authors: Tacconi Maria T , Wurtman Richard J 
Published: April 2011

Abstract
The distribution and fate of piracetam (2-oxo-1-pyrrolidine acetamide, Nootropil), the prototype ‘nootropic drug’, was examined in rats given 100–1000 mg kg−1 by gavage, with or without [3H]piracetam as a tracer. Peak serum concentrations were attained after 60 min. Its half-life of disappearance from serum was about 2 h during the initial 8 h after administration and then about 6·4 h for the next 16 h. Brain piracetam concentrations equilibrated with those of serum at about 4 h, after which they fell exponentially but remained about twice those of serum; piracetam concentrations in the brainstem were lower (by 30–40%) than those in the cortex, olfactory bulb, and colliculi. No evidence could be obtained for significant piracetam metabolism, either in-vivo or when incubated with liver homogenates. No specific binding of [3H]piracetam to any of various subcellular fractions was observed after its administration along with unlabelled carrier. Repeated daily doses of piracetam (7 days, 100 mg kg−1) failed to elevate serum or brain concentrations beyond those observed after a single dose.
Inhibition by diethylcarbamazine of acetylcholine-induced endothelium-dependent relaxation of rabbit aorta: are leukotrienes involved?
Authors: Förstermann Ulrich , Neufang Brigitte 
Published: April 2011

Abstract
Acetylcholine caused relaxations of preconstricted rabbit aortic strips if the endothelium was intact. These relaxations were reversed in a concentration-dependent manner by diethylcarbamazine, an inhibitor of slow-reacting substance and leukotriene formation. However, when exogenous leukotrienes (LTA4, LTB4, LTC4 and LTD4) were added to the precontracted arterial strips none of them caused relaxation, showing that they are unlikely to be involved as mediators in the acetylcholine-induced relaxation of rabbit aorta.
Correlation between gastric irritancy and anti-inflammatory activity of non-steroidal anti-inflammatory drugs
Authors: Dearden J C , Nicholson R M 
Published: April 2011

Abstract
Gastric irritancies and anti-inflammatory potencies of 25 commercially available non-steroidal anti-inflammatory drugs (NSAIDs) have been measured in the rat. When irritancy is measured as the dose required to produce a specified level of gastric mucosal damage, it is found that irritancy increases with anti-inflammatory potency. However, when irritancy is measured as the level of gastric mucosal damage at the anti-inflammatory ED50 (which is a clinically realistic measure) then irritancy decreases as anti-inflammatory potency increases. Hence it should be possible to design high-potency, low-irritancy NSAIDs.
The effect of protein on the dissolution of phenytoin
Authors: Rosen A , Macheras P 
Published: April 2011

Abstract
Ultrafiltration of a continuous flow system was used to follow the dissolution of phenytoin powder in buffered solutions of pH 1, 4 and 7·4. The presence of either human serum albumin (HSA) or casein caused changes in both the absolute solubility and the dissolution rate. Normal protein binding cannot be responsible for the effects noted. It would seem likely that within the diffusion layer a higher degree of protein binding occurs than is possible in the bulk aqueous solution. The drug solubilized in this way is then released in solution in a form that is at least metastable with respect to phenytoin in normal solution. The effect of protein on phenytoin dissolution may well affect the bioavailability of the drug.
The in-vivo evaluation of an osmotic device (Osmet) using gamma scintigraphy
Authors: Davis S S , Hardy J G , Taylor M J , Stockwell A , Whalley D R , Wilson C G 
Published: April 2011

Abstract
The release of a radiolabelled marker from an orally administered osmotic pump device (Osmet) has been evaluated in-vivo in a group of 6 subjects, using the technique of gamma scintigraphy. The duration of residence of the pump in the stomach was greatly influenced by food intake. However, the release of the marker from the device was independent of food and position within the gastrointestinal tract. Furthermore, the material released from the osmotic pump was well distributed in the gastrointestinal tract. Good agreement between in-vitro and in-vivo release rates was obtained.
Biotransformation of the topical glucocorticoids budesonide and beclomethasone 17α,21-dipropionate in human liver and lung homogenate
Authors: Andersson P , Ryrfeldt Å , Draco AB 
Published: April 2011

Abstract
Tritiated budesonide and beclomethasone 17α,21-dipropionate (BDP) were incubated with the 9000g supernatant of human liver homogenate. BDP was immediately hydrolysed to beclomethasone 17α-propionate (BMP). BMP was then further biotransformed to polar metabolites. Budesonide was rapidly biotransformed (2–4 times more rapidly than BMP) to metabolites of low glucocorticoid potency. The compounds were also incubated with the 1000g supernatant of human lung homogenate. BDP was rapidly hydrolysed to BMP and then more slowly to beclomethasone. Budesonide was not biotransformed in the lung.
Influence of mecamylamine and atropine on tolerance development to nicotine hypothermia in rats
Authors: Horstmann Michael 
Published: April 2011

Abstract
Nicotine hypothermia is known as a central effect of nicotine waning after repeated administration due to the development of tolerance. In the present experiments using female rats, this tolerance was attenuated by the concomitant administration of mecamylamine. Atropine was without effect. It is concluded that tolerance to this effect of nicotine implies its contact with specific sites within the cns.
α-Adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle
Authors: Ohizumi Yasushi , Kajiwara Akiko , Nakamura Hideshi , Kobayashi Jun’ichi 
Published: April 2011

Abstract
In the rabbit isolated aorta and renal artery, aaptamine (3 times 10−5 m), a novel heteroaromatic substance isolated from a sea sponge Aaptos aaptos produced a parallel, rightward shift of the dose-response curve for noradrenaline, whereas that for histamine or KCl was not affected. But, the derivatives of aaptamine, demethylaaptamine, demethyloxyaaptamine, dihydroaaptamine and dihy-drodemethylaaptamine at concentrations of 10−5 to 10−4 m had no effect on the dose-response curve for noradrenaline. These results suggest that aaptamine is a competitive antagonist of α-adrenoceptors in vascular smooth muscles.
Is vasoactive intestinal peptide an inhibitory transmitter in the circular but not the longitudinal muscle of guinea-pig colon?
Authors: Bennett A , Bloom S R , Ch’ng J , Christofides N D , Peacock L E , Rennie J A 
Published: April 2011

Abstract
Circular muscle strips of guinea-pig isolated colon relaxed with vasoactive intestinal peptide or peptide histidine methionine, whereas the longitudinal muscle contracted. The non-adrenergic-non-cholinergic inhibitory nerves may therefore be different in these two muscle layers.
Pro- and anti-convulsant drug effects in combination with the convulsant benzodiazepine Ro 5–4864
Authors: Pellow Sharon , File Sandra E 
Published: April 2011

Abstract
The effects of several compounds believed to act at the GABA-benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol (leptazol, pentylenetetrazole) were investigated in combination with the convulsant benzodiazepine Ro 5–4864. Tracazolate (25–100 mg kg−1) failed to affect convulsions induced by Ro 5–4864; however, they were prevented by treatment with CL 218, 872 (20 mg kg−1). Compounds having proconvulsant activity in combination with a subthreshold dose of Ro 5–4864 were: CL 218,872 (5 mg kg−1), and CGS 8216 (20 mg kg−1) and FG 7142 (40 mg kg−1), two compounds characterized as ‘inverse agonists’; at benzodiazepine receptors. The phenylquinolines PK 8165 and PK 9084, originally believed to have anxiolytic properties, had no significant effect in combination with Ro 5–4864 (25–100 mg kg−1). The convulsant profile of Ro 5–4864 is compared with that of picrotoxin and pentetrazol.
Muscarinic receptor agonist-antagonist interaction in the rat rectum: are there ways of activating the same receptors?
Authors: Akah P A , Oriowo M A 
Published: April 2011

Abstract
The interaction between the muscarinic receptor agonists, carbachol, acetylcholine (ACh) and methacholine, and antagonists, atropine, gallamine, 4-DAMP and pirenzepine, was studied on the rat isolated rectum preparation. ACh (1.93 times 10−8-1.95 times 10−6M), methacholine (8.7 times 10−8-1.1 times 10−6 M) and carbachol (1.1 times 10−7-3.5 times 10−6 M) induced contractions that were reversibly antagonized by atropine (1.9 times 10−9-4.8 times 10−8 M), 4-DAMP (1.5 times 10−8-2.86 times 10−7 M) gallamine (1.12 times 10−6-1.12 times 10−4 M) and pirenzepine (2.8 times 10−7-7.0 times 10−6 M). The pA2 values were atropine: 8.99 ± 0.28, 9.29 ± 0.14 and 8.86 ± 0.05; 4-DAMP: 8.39 ± 0.10, 8.66 ± 0.15 and 8.26 ± 0.30, gallamine: 5.85 ± 0.23, 5.73 ± 0.25 and 5.96 ± 0.10 and pirenzepine: 6.85 ± 0.44, 7.17 ± 0.13 and 7.21 ± 0.03 against ACh, methacholine and carbachol, respectively. The experimental dose-ratio (atropine + gallamine) was greater than the expected dose-ratio (as predicted by the Paton & Rang rule) for ACh and methacholine while the experimental dose-ratio closely approximates the expected dose-ratio for carbachol. It is suggested that atropine, 4-DAMP pirenzepine and gallamine act on the same receptors but gallamine allosterically altered the binding of the agonists and antagonists to varying extents.
Characterization of α2-adrenoceptor binding properties of imidazoline-like drugs, azoloazepine derivatives and β-phenethylamine-like drugs in human platelet membranes
Authors: Vago Tarcisio , Meroni Rachele , Dagani Regina , Baldi Gabriella , Pagani Marco , Bevilacqua Maurizio , Norbiato Guido 
Published: April 2011

Abstract
To characterize the agonist profile of α2-adrenoceptor agonists (imidazoline-like drugs, azoloazepine derivatives, β-phenethylamines-like drugs) on human platelets, the characteristics of α2-adrenoceptors (KD, Bmax) have been evaluated and the affinity constants measured by displacement technique and computer-assisted analysis of the curves. Furthermore, since α2-adrenoceptor agonists interact with the post-synaptic receptors in a calcium-operated channel, whether the effect of calcium-entry inhibitors (verapamil, nifedipine, diltiazem) is related to a competition with α2-receptors has also been examined. By Scatchard analysis, it was calculated that in human platelets α2-adrenoceptors have KD = 3.45 nM and Bmax = 247 fmol (mg protein)−1. As far as the potency is concerned, imidazoline-like drugs were the most potent agonists in human platelet α2-adrenoceptors (guanabenz IC50 = 8.6 ± 0.8 times 10−8, B-HT 920 IC50 = 2.9 ± 0.3 times 10−7, (-)-adrenaline IC50 = 3.4 ± 0.5 times 10−7). Among the calcium-entry inhibitors only verapamil antagonized [3H]rauwolscine binding: the effect was stereospecific, (-)-D 600 being more potent than (+)-D 600. Nifedipine and diltiazem did not affect α2-receptor binding. It is concluded that human platelets α2-receptors share the agonist potency profile of other tissues containing α2-receptors (brain, pre-synaptic junction), and that among calcium-entry blockers only verapamil can antagonize α2-agonists. Nifedipine and diltiazem do not appear to interact stereospecifically with α2-adrenoceptors.
Influence of the granulation technique and starting material properties on the lubricating effect of granular magnesium stearate
Authors: Johansson Mats E 
Published: April 2011

Abstract
Magnesium stearate has been granulated in four ways to produce lubricant granulations with different properties. The lubricating properties, as well as the tablet properties with the granulated lubricant, were evaluated on tablets prepared from a mixture of dicalcium phosphate, corn starch and microcrystalline cellulose. The lubricating effect of the magnesium stearate granulations showed a similar pattern regardless of the granulation technique used except for a granulation with providone. Increasing the particle size of the magnesium stearate granulation increased the amount of lubricant required to obtain lubrication similar to powdered magnesium stearate. Variations in the specific surface area of the starting materials could be masked by using them in granular form.
The characterization of wet powder masses suitable for extrusion/spheronization
Authors: Harrison P J , Newton J M , Rowe R C 
Published: April 2011

Abstract
The characterization of the flow of wet powder masses has been achieved using a ram extruder. Force/displacement curves obtained when material is forced through dies of varying length were found to exhibit three stages: (1) compression (2) steady state flow and (3) forced flow. To provide high quality extrudate it was found preferable to ensure that the compression stage was as short as possible and that steady state flow predominated. To produce these conditions, an optimum composition, die length and ram speed were required. The implications of these findings in relation to the provision of suitable formulations and production conditions for the preparation of spherical granules are discussed.
Isolation of a new aloe-emodin dianthrone diglucoside from senna and its potentiating effect on the purgative activity of sennoside A in mice
Authors: Nakajima Née Sasakl Kazuko , Yamauchi Kazuko , Kuwano Shigeaki 
Published: April 2011

Abstract
Two aloe-emodin dianthrone diglucosides (I and II) were isolated from the leaves of Cassia angustifolia Vahl by successive column chromatography with Amberlite XAD-2, silica gel, Polyamide C-200 and Sephadex LH-20. The stereostructures of I and II were elucidated as trans and meso isomers at 10-10′, respectively, from the patterns of the ultraviolet absorption spectra and circular dichroism curves. This is the first report of isolation of diglucoside I from senna. Despite the lack of purgative activity, diglucoside I exerts a potentiating effect of about 1. 3 times on the purgative activity of sennoside A in mice when even 15% is included in the mixture. The difference between I and a third active glycoside based on aloe-emodin is also discussed.
Facilitated transport of sodium salicylate across an artificial lipid membrane by Azone
Authors: Hadgraft Jonathan , Walters Kenneth A , Wotton Paul K 
Published: April 2011

Abstract
The ability of Azone (1-dodecylazacylcoheptan-2-one), a recently developed penetration enhancer, to facilitate the transport of sodium salicylate across an artificial lipid membrane has been investigated using the rotating diffusion cell, a well defined model for percutaneous absorption. Azone was found to be capable of enhancing the transport of the salicylate anion across an isopropyl myristate membrane, by using a pH gradient as the chemical driving force. The results indicate that Azone may be capable of forming ion pairs with anionic drugs.
Kinetics of D-α-tocopherol in a water soluble base in man
Authors: Bateman N E , Uccellini D A 
Published: April 2011

Abstract
The kinetics of D-α-tocopherol (vitamin E) were investigated in 10 healthy, adult volunteers following a single dose of 500 iu D-α-tocopherol. Plasma concentration/time curves fitted using a one compartment open model, showed a rise to 12 ± 1.9 μmol litre−1 above endogenous values over 8-9 h and then a tailing away to 7 ± 1.1 μmol litre−1 after 24 h.