bluuebunny/crossref_metadata_2025_split huggingface dataset:
THE SIZE OF HYDROXYL GROUPS IN SOLUTION AND THE CHANGES IN SIZE ASSOCIATED WITH THE IONIZATION OF PHENOLIC, CARBOXYLIC AND AMINO GROUPS IN PHENOLIC QUATERNARY AMMONIUM SALTS, NICOTINE AND SOME AMINO ACIDS: POSSIBLE IMPLICATIONS FOR DRUG‐WATER AND DRUG‐RECEPTOR INTERACTIONS
Authors: BARLOW R.B. 
Published: May 2015

Size in solution can be expressed either as the apparent molal volume at infinite dilution (φv0) and the concentration parameter (j) or as the partial molal volume of the solute at infinite dilution () and the concentration parameter for the solute or solvent (qs or qw). Although calculated differently, these are derived from the same results and are equivalent.
From measurements with phenolic quaternary ammonium salts, including compounds with high nicotine‐like activity, the apparent size of the hydroxyl group in water is small and variable. Phenolic groups are slightly larger than alcoholic groups, which should be better hydrogen donors.
By measuring the volume change associated with ionisation it is possible to measure the size of charged groups such as phenate and carboxylate; these are much smaller than phenolic and carboxyl. Ammonium groups, however, are only slightly smaller than the corresponding amines.
The zwitterion forms of amino acids are associated with a minimum in volume but the volume changes increase with chain length from glycine to γ‐aminobutyric acid. Groups separated by less than this distance interact in their effects on water.
Decreases in volume or unexpectedly small increments in apparent molal volume represent decreases in entropy which must be taken into account in drug‐water‐receptor interactions. Although they may be offset by enthalpy changes, they should favour binding because there is more scope for an increase in entropy. This might explain the association of the small apparent size in water of the hydroxyl group in many compounds with its effects on their affinity for receptors.
STIMULATION OF THE ANTIGEN‐INDUCED CONTRACTION OF GUINEA‐PIG TRACHEA AND IMMUNOLOGICAL RELEASE OF HISTAMINE AND SRS‐A FROM SENSITIZED GUINEA‐PIG LUNG BY (2‐ISOPROPYL‐3‐INDOLYL)‐3 PYRIDYL KETONE (L8027) AND INDOMETHACIN
Authors: HITCHCOCK MARGARET 
Published: May 2015

(2‐Isopropyl‐3‐indolyl)‐3 pyridyl ketone (L8027) and indomethacin reduced basal tension and enhanced the antigen‐ and histamine‐induced contractions of tracheal spirals obtained from actively sensitized guinea‐pigs. The stimulating effect of L8027 required the presence of the drug, while that of indomethacin persisted after its removal from the organ bath.
L8027 and indomethacin stimulated the immunological release of histamine and slow reacting substance of anaphylaxis (SRS‐A) and inhibited the de novo synthesis and release of malondialdehyde from actively sensitized guinea‐pig lung fragments.
L8027 was 2,800 times more potent than indomethacin in both in vitro models of anaphylaxis.
A selective antagonist of SRS‐A (FPL 55712) inhibited contractions produced by antigen, but had no effect on contractions produced by histamine.
Prostaglandins E and F2α were continuously released into the organ bath fluid by the resting trachea. Contractions induced by antigen or histamine increased the rate of prostaglandin efflux.
L8027 had no effect on the efflux of prostaglandins E and F2α at rest and during contraction. Indomethacin inhibited prostaglandin efflux at rest and during contraction while present in the organ bath. Prostaglandin efflux was restored to 80% of control after removal of indomethacin.
The results suggest that prostaglandins E and F2α have no role in the stimulation by L8027 and indomethacin of the contractile responses of guinea‐pig trachea. The possible mechanism for the effects of these drugs is discussed.
THE EFFECT OF γ‐AMINOBUTYRIC ACID ON THE INPUT CONDUCTANCE AND MEMBRANE POTENTIAL OF ASCARIS MUSCLE
Authors: MARTIN R.J. 
Published: May 2015

Twin intracellular recordings were made from the bag region of Ascaris muscle in order to make conductance measurements. The preparation was bathed in a cool (22°C) Ringer solution to abolish the large spontaneous depolarizing potentials and to improve stability for recording.
The resting membrane potential was − 31 ± 1 mV, mean ± s.e. mean (n = 17). The current‐voltage plots were linear in the hyperpolarizing direction but showed evidence of delayed rectification during the application of depolarizing currents. The input conductance of the bag was measured from the slope of these plots during the application of hyperpolarizing current. The resting conductance of the bags was 2.4 ± 0.2 μS, mean ± s.e. mean (n = 12).
When the preparation was perfused with γ‐aminobutyric acid (GABA) in concentrations greater than 3 μm, a dose‐dependent increase in conductance associated with a hyperpolarizing potential was recorded. The log dose‐response relationship obtained from 6 preparations was sigmoidal and had an ED50 of 3 μm.
When Cl− in the Ringer was replaced by SO2‐4, the GABA‐induced conductance changes decreased and were associated with depolarizing potentials.
Voltage responses were recorded in the bag region during the iontophoretic application of GABA to different regions of the muscle cell. The largest responses were recorded when GABA was applied to the bag region. Smaller responses were recorded when GABA was applied to the arms and syncytial regions. The responses of the bags were dose‐dependent and were antagonized by bath‐applied picrotoxin.
An extrapolation method using 10−5 m GABA suggested that the GABA reversal potential was about 30 mV more negative than the resting membrane potential. This was confirmed by means of a two microelectrode voltage clamp technique. The reversal potential was thus estimated as − 61.2 + 2.2 mV mean ± s.e. mean (n = 27).
EFFECTS OF METOCLOPRAMIDE AND ISOPRENALINE IN THE RAT VAS DEFERENS; INTERACTIONS WITH α‐ADRENOCEPTORS
Authors: SPEDDING M. 
Published: May 2015

Metoclopramide (2.8 to 280 μm) augmented contractions of rat vas deferens preparations induced by field stimulation (6 Hz for Is). This effect was antagonized by phentolamine (0.1 μm). Metoclopramide (2.8 to 280 μm) did not affect phenylephrine‐induced contractions.
Metoclopramide (2.8 to 280 μm) antagonized the inhibitory effects of clonidine on the contractions induced by field stimulation, but not the inhibitory effects of purine nucleosides.
From these results it is concluded that metoclopramide (2.8 to 280 μm) is a presynaptic α‐adrenoceptor antagonist in the rat vas deferens.
Following β‐adrenoceptor blockade with (±)‐propranolol (3.3 μm), (‐)‐isoprenaline (0.47 to 14 μm) inhibited responses to field stimulation but not to phenylephrine. These propranolol‐resistant effects of isoprenaline were antagonized by metoclopramide (2.8 to 280 μm) and by phentolamine (0.1 to 10 μm), indicating that isoprenaline may stimulate presynaptic α‐adrenoceptors in this preparation.
ABSENCE OF CHANGES IN DRUG DISPOSITION AND CATECHOLAMINE SENSITIVITY IN THE HYPERTHYROID DOG
Authors: ISHIZAKI TAKASHI , TAWARA KAZUJI 
Published: May 2015

In order to study the relative contribution of hepatic drug metabolizing enzymes and hepatic blood flow to the clearance of drugs in the hyperthyroid state, the disposition kinetics of two model compounds (antipyrine and propranolol) were examined in thyroid‐fed dogs as compared to euthyroid and phenobarbitone‐pretreated animals.
In hyperthyroid dogs, the possibility of catecholamine hypersensitivity was evaluated by assessing the chronotropic response to isoprenaline and by constructing a drug concentration‐effect (β‐blockade) relationship.
The plasma propranolol half‐life (0.97 ± 0.12 h) of the hyperthyroid animals did not differ significantly from either the euthyroid group or the phenobarbitone‐pretreated group. This was observed with no significant change in the apparent volume of distribution among the three experimental groups.
Phenobarbitone pretreatment accelerated significantly the elimination of antipyrine (half‐life, 1.09 ± 0.15 h, P < 0.01) as compared to the euthyroid (2.84 ± 0.35 h) and the hyperthyroid groups (2.58 ± 0.13 h), respectively, without any changes in the apparent volume of distribution in any group.
Neither the chronotropic responses to exogenously administered catecholamine, nor the antagonist concentration‐effect relationships support the concept that the hyperthyroid state potentiates sensitivity of the receptor‐effect system of the heart.
The data obtained from the present study fit best with the view that thyroid hormone excess alters neither the disposition of the model compounds used nor the catecholamine‐sensitivity examined.
ANTAGONISM OF PROSTANOID‐INDUCED CONTRACTIONS OF RAT GASTRIC FUNDUS MUSCLE BY SC‐19220, SODIUM MECLOFENAMATE, INDOMETHACIN OR TRIMETHOQUINOL
Authors: BENNETT A. , JAROSIK C. , SANGER G.J. , WILSON D.E. 
Published: May 2015

The effects of SC‐19220, sodium meclofenamate, indomethacin or trimethoquinol were studied on contractions of the rat stomach longitudinal muscle to prostaglandin D2 (PGD2), PGE2, PGF2α, PGH2, epoxymethano PGH2 analogues, PGI2, 6‐keto‐PGF1α, 6,15‐diketo‐PGF1α and thromboxane B2. All the drugs reduced contractions to all the prostanoids, but the degree of reduction differed widely. Selectivity of blockade was assessed by comparison with acetylcholine (ACh).
With SC‐19220 5 μg/ml the effect on thromboxane B2, PGD2 or PGH2 and its epoxymethano analogues was not significantly different from the small effect on ACh, but the other prostanoids were blocked to greater extents.
The effect of the cyclo‐oxygenase inhibitor sodium meclofenamate, 1 or 2 μg/ml, on 6,15‐diketo‐PGF1α or thromboxane B2 was similar to the small antagonism of ACh, whereas the other prostanoids were blocked to greater extents. Indomethacin, 1 μg/ml, also reduced contractions to the prostanoids, but antagonism of the PGH2 epoxymethano analogues was considerably less than with meclofenamate.
The β‐adrenoceptor stimulant trimethoquinol, 50 ng/ml, was the most potent prostanoid antagonist tested; all the prostanoids except PGE2 were antagonized more than ACh.
EVIDENCE FOR SPECIFIC ADENOSINE RECEPTORS AT CHOLINERGIC NERVE ENDINGS
Authors: SILINSKY E.M. 
Published: May 2015

An electrophysiological study was made to determine if adenosine and adenine nucleotides affect cholinergic nerve endings to frog skeletal muscle through relatively non‐specific nucleotide receptors or through specific adenosine receptors.
Non‐hydrolysable derivatives of adenosine triphosphate failed to alter the mean number of acetylcholine (ACh) quanta released by a nerve impulse (m̄) or the miniature endplate potential frequency (m.e.p.p.f) but N6‐methyladenosine and 2‐chloroadenosine, two adenosine analogues with an unsubstituted ribose moiety (R‐site agonists), produced marked reductions in m̄ and m.e.p.p.f.
In contrast, 2′‐deoxyadenosine, a derivative with an unsubstituted purine ring (P‐site agonist), generally produced increases in m̄ and m.e.p.p.f, which further increased after removing the drug. Other P‐site agonists such as 5′‐deoxyadenosine (in the presence of theophylline) and 9‐β‐d‐arabinofuranosyl adenine also increased m̄ and m.e.p.p.f.
The results suggest that two types of adenosine receptors may be present at cholinergic nerve endings, one type (R‐site) mediating depression and the other type (P‐site) producing enhancement of ACh release.
INHIBITORY ACTIONS OF METHIONINE‐ENKEPHALIN AND MORPHINE ON THE CAT CAROTID CHEMORECEPTORS
Authors: McQUEEN D.S. , RIBEIRO J.A. 
Published: May 2015

The effects of intracarotid injections of methionine‐enkephalin (Met‐enkephalin) and morphine on chemoreceptor activity recorded from the peripheral end of a sectioned carotid sinus nerve have been studied in cats anaesthetized with pentobarbitone.
Met‐enkephalin caused a rapid, powerful, inhibition of spontaneous chemoreceptor discharge, the intensity and duration of which was dose‐dependent.
Morphine was a less potent inhibitor of spontaneous chemoreceptor discharge, and the inhibition it evoked was rather variable and tended to be biphasic. Low doses of morphine caused a slight increase in discharge.
Naloxone (0.2 mg i.c.) slightly increased spontaneous discharge, greatly reduced the chemo‐inhibition caused by morphine, and reduced the inhibitory effect of Met‐enkephalin. A higher dose of naloxone (0.8 mg) caused a substantial reduction of the Met‐enkephalin effect.
Chemo‐excitation evoked by intracarotid injections of acetylcholine, CO2‐saturated Locke solution, and sodium cyanide were only slightly and somewhat variably reduced following injections of Met‐enkephalin, whereas the inhibitory effect of dopamine was potentiated. Following morphine administration, responses to acetylcholine and sodium cyanide were reduced slightly, whereas those to CO2 and dopamine were potentiated.
Responses to acetylcholine and CO2 were slightly potentiated during infusion of Met‐enkephalin (50 μg/min, i.c.) and the response to sodium cyanide was slightly reduced.
It is concluded that naloxone‐sensitive opiate receptors are present in the cat carotid body; when activated they cause inhibition of spontaneous chemoreceptor discharge. The physiological role of these receptors and the identity of any endogenous ligand remains to be established.
VASORELAXANT ACTION OF CAROVERINE FUMARATE (A QUINOXALINE DERIVATIVE), A CALCIUM‐BLOCKING AGENT
Authors: ISHIDA YUKISATO , OZAKI HIROSHI , SHIBATA SHOJI 
Published: May 2015

Caroverine fumarate, 1‐(2‐diethylaminoethyl)‐3‐(p‐methoxy‐benzyl)‐1,2‐dihydro‐2‐quinoxalinone fumarate, caused a greater inhibition of the pressor response to KCl (8 × 10−2 m) than that to noradrenaline (10−6 m) in the rat hindquarter preparation.
In the isolated aorta of the rat, caroverine (up to 10−6 m) markedly suppressed the contraction caused by KCl (4 × 10−2 m) (high‐K) but had little effect on the contractile response to noradrenaline (10−6 m) whether added before the spasmogen or in its presence.
In the high‐K‐treated aorta, caroverine shifted the concentration‐response curve for external calcium to the right, competitively. The negative logarithm of the affinity (pA2) of caroverine was calculated to be approx. 7.
Increased 45Ca uptake of the high‐K‐treated aorta measured by a modified lanthanum method was inhibited by either caroverine (3 × 10−6 m) or verapamil (10−6 m).
Concentrations of caroverine and verapamil reducing high‐K‐induced aortic contraction to 50% of its maximum were 2.4 × 10−7 and 6.6 × 10−8 m respectively.
Following washout the caroverine‐induced inhibition of high‐K‐induced aortic contraction was more rapidly restored than the verapamil‐induced inhibition.
These results suggest that caroverine fumarate is a specific and readily reversible calcium influx inhibitor in the rat vascular smooth muscle.
Low‐density lipoprotein‐cholesterol (LDL‐C) greater than 100 mg/dL as a quality indicator: locating risk in person, place and time
Authors: Rohrer James E. , Doganer Yusuf C. , Merry Stephen P. , Angstman Kurt B. , Erickson Jacob L. , Furst Joseph W. 
Published: May 2015

AbstractRationale, aims and objectivesAchieving control over elevated lipid parameters, particularly low‐density lipoprotein (LDL)‐cholesterol, is an acknowledged quality indicator in primary care. The Centers for Disease Control and Prevention (CDC)'s model for investigation of outbreaks (person–place–time) can be applied to the analysis of quality indicators.MethodsA sample of 322 family medicine patients for whom lipid levels were ordered was extracted. LDL > 100 mg/dL was cross‐tabulated by personal characteristics [age group, gender, body mass index (BMI), diagnoses], month (time) and ordering department (place).ResultsAge (except one age category), gender, time and location were not related to LDL > 100 mg/dL after adjustment for covariates. All levels of BMI above normal elevated the risk of LDL > 100 mg/dL [BMI 25–29.9: odds ratio (OR) = 3.41, confidence interval (CI) = 1.61–7.23, P = 0.0014; BMI 30–34.9: OR = 2.93, CI = 1.28–6.70, P = 0.0109; BMI ≥ 35: OR = 2.75, CI = 1.19–6.37, P = 0.0181]. Patients with coronary artery disease (CAD) and diabetes mellitus (DM) were at reduced risk for LDL > 100 mg/dL (CAD: OR = 0.47, CI = 0.24–0.91, P = 0.0254; DM: OR = 0.28, CI = 0.14–0.55, P = 0.0002).ConclusionAn outbreak investigation model is useful for analysing variations in this quality indicator. Patients with higher BMI and those not diagnosed with CAD or DM type I/II may be considered for intensified lipid lowering using quality improvement efforts. These might include counselling for lifestyle changes or medication therapy depending upon their calculated cardiac risk.
Do all the patients with vitamin B12 deficiency have pernicious anemia?
Authors: Sun Andy , Chang Julia Y.‐F. , Wang Yi‐Ping , Cheng Shih‐Jung , Chen Hsin‐Ming , Chiang Chun‐Pin 
Published: May 2015

BackgroundVitamin B12 deficiency may result in pernicious anemia (PA). This study evaluated whether all the patients with vitamin B12 deficiency had PA.MethodsThe blood hemoglobin (Hb), iron, vitamin B12, folic acid, and homocysteine concentrations and mean corpuscular volume (MCV) in 90 vitamin B12‐deficient patients were measured and compared with the corresponding data in 180 age‐ and sex‐matched healthy control subjects. PA was defined by World Health Organization (WHO) as having an Hb concentration <13 g/dl for men and <12 g/dl for women, an MCV ≧ 100 fl, a serum vitamin B12 level <200 pg/ml, and serum gastric parietal cell antibody (GPCA) positivity.ResultsWe found that 35 (38.9%) and 20 (22.2%) patients with vitamin B12 deficiency had deficiencies of Hb (men <13 g/dl, women <12 g/dl) and iron (<60 μg/dl), respectively. Moreover, 65 (72.2%) and 37 (41.1%) patients with vitamin B12 deficiency had abnormally high blood homocysteine level (>12.7 μM) and high MCV (≧100 fl), respectively. In addition, 43 (47.8%) vitamin B12‐deficient patients with had GPCA positivity. Patients with vitamin B12 deficiency had a significantly higher frequency of Hb or iron deficiency, of abnormally elevated blood homocysteine level or high MCV, and of GPCA positivity than healthy control subjects (all P‐values < 0.001). However, only 17 (18.9%) of 90 vitamin B12‐deficient patients were diagnosed as having PA by the WHO definition.ConclusionOnly 18.9% of patients with vitamin B12 deficiency are discovered to have PA by the WHO definition.
Dietary supplementation with glutamine and γ‐aminobutyric acid improves growth performance and serum parameters in 22‐ to 35‐day‐old broilers exposed to hot environment
Authors: Hu H. , Bai X. , Shah A. A. , Wen A. Y. , Hua J. L. , Che C. Y. , He S. J. , Jiang J. P. , Cai Z. H. , Dai S. F. 
Published: May 2015

SummaryThis study was designed using 360 21‐day‐old chicks to determine the influences of diet supplementation with glutamine (5 g/kg), γ‐aminobutyric acid (GABA, 100 mg/kg) or their combinations on performance and serum parameters exposed to cycling high temperatures. From 22 to 35 days, the experimental groups (2 × 2) were subjected to circular heat stress by exposing them to 30–34 °C cycling, while the positive control group was exposed to 23 °C constant. The blood of broilers was collected to detect serum parameters on days 28 and 35. Compared with the positive control group, the cycling high temperature decreased (p < 0.05) the feed consumption, weight gain and serum total protein (TP), glucose, thyroxine (T4), insulin, alkaline phosphatase (ALP), glutamine, GABA and glutamate levels, while increased (p < 0.05) the serum triglyceride (TG), corticosterone (CS), glucagon (GN), creatine kinase (CK), glutamic oxaloacetic transaminase (GOT), nitric oxide synthase (NOS), glutamate pyruvate transaminase (GPT) and lactate dehydrogenase (LDH) levels during 22–35 days. However, dietary glutamine (5 g/kg) increased (p < 0.05) the feed consumption, weight gain and serum levels of glutamine, TP, insulin and ALP, but decreased (p < 0.05) the serum TG, CK, GOT, NOS and GPT levels. Diet supplemented with GABA also increased (p < 0.05) weight gain and the serum levels of TP, T4, ALP, GABA and glutamine. In addition, the significant interactions (p < 0.05) between glutamine and GABA were found in the feed consumption, weight gain and the serum ALP, CK, LDH, GABA, T3 and T4 levels of heat‐stressed chickens. This research indicated that dietary glutamine and GABA improved the antistress ability in performance and serum parameters of broilers under hot environment.
Impact of Physical Resistance Training on the Sexual Function of Women with Polycystic Ovary Syndrome
Authors: Lara Lúcia Alves Silva , Ramos Fabiene Karine Piccki , Kogure Gislaine Satiko , Costa Rafael Silva , Silva de Sá Marcos Felipe , Ferriani Rui Alberto , dos Reis Rosana Maria 
Published: May 2015

ABSTRACT

Introduction
There is a need for specific measures to address overall care in women with polycystic ovary syndrome (PCOS). Physical resistance training (PRT) has been shown to improve certain body parameters. However, the effect of PRT on the sexual function of PCOS women has not been evaluated.

Aim
The study aimed to assess sexual function and emotional status of PCOS women after 16 weeks of PRT.

Methods
This case-control study involved 43 women with PCOS and 51 control ovulatory women, aged 18–37 years. All women were subjected to a supervised PRT protocol for 16 weeks and evaluated at the end of the program. Sexual function was assessed at baseline and after PRT protocol.

Main Outcome Measures
The main outcome measure used was the Female Sexual Function Index (FSFI).

Results
Of the 43 women with PCOS, 30 (69.70%) had a basal total FSFI score ≤ 26.55 and 24 of them (58.54%) had a score ≤ 26.55 after PRT (P = 0.08). Of the 51 control women, 32 (62.7%) and 27 (52.9%) had FSFI scores &lt; 26.55 at baseline and after PRT, respectively (P = 0.06). Control women experienced a significant improvement in pain domain score after PRT (P &lt; 0.03). PCOS women experienced significant increases in total score and in the desire, excitement and lubrication domains after PRT (P &lt; 0.01 each). After PRT, there was a significant difference between the PCOS and control groups in the sexual desire domain (4.09 ± 1.29 vs. 3.75 ± 1.42, P = 0.04). Significantly fewer women in the PCOS group were at risk of depression (P &lt; 0.01) and anxiety (P &lt; 0.02) after than before PRT, whereas the differences in the control group were not significant. Mean depression and anxiety scores were reduced significantly in both the PCOS (P &lt; 0.01 each) and control (P &lt; 0.01) groups.

Conclusions
PRT significantly enhanced total score and the desire, excitement, and lubrication domains of the FSFI in PCOS women. PRT reduced pain, and total depression and anxiety scores in both groups.