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At least 235 records · Page 13Linked to original sources
PubMed1992

Metadoxine (pyrrolidone carboxylate of pyridoxine) antagonizes the locomotor-stimulatory effect of ethanol in mice.

The effects of metadoxine (pyrrolidone-carboxylic acid; PCA) and pyridoxine on the locomotor responses to ethanol in mice were compared. Metadoxine (200 and 400 mg/kg i.p.) and PCA (86 and 172 mg/kg) prevented, in a dose-related manner, the locomotor stimulant effect of a low dose of ethanol (1.5 g/kg i.p.), whereas pyridoxine (228 mg/kg i.p.) was completely ineffective. Neither compound modified the sedative effect of a high ethanol dose (2.5 g/kg i.p.). The results indicate that the antagonistic effect of metadoxine on ethanol stimulant response is due to the PCA component of the molecule.

Animals↗
PubMedDate not supplied

[Regulating effect of gamma-aminobutyric acid and pyrrolidone-2 on endogenous blood metalloproteins with anti- and pro-oxidant activity in hypoxia].

Various stages of hypokinesia are marked by specific changes in the level and activity of endogenous metalloproteins with anti- (MAA) and prooxidant action (MPA). In particular, the level of MPA [cytochromes b5 and b558 (III + IV) and suprol] decreases in all stages (except for the level of cytochrome b5 exceeding that in the free control on the 15th and 30th day of hypokinesia). The superoxide production activity of suprol always exceeds that in the control, while the activity of cytochrome b558 (III) exceeds that in the control only on the 30th day of experiment. The level and activity of MAA [ceruloplasmin, transferrin (TF), superoxide dismutase (SOD), and catalase] decrease with the duration of hypokinesia (except for 15th day, when the level of TF and the activity of SOD exceed the values in the free control group). The administration of GABA and pyrrolidone decreases the extent of oxidative stress, which is manifested by leveling of the MAA and MPA content and activity.

Animals↗
PubMed2005

Ternary amorphous composites of celecoxib, poly(vinyl pyrrolidone) and meglumine with enhanced solubility.

The present study highlights the development of ternary amorphous composites to enhance the solubility of a poorly soluble crystalline drug, celecoxib (CEL). These systems comprised of an 'amorphous drug,' and its 'stabilizer' and 'solubilizer.' The ternary amorphous system of CEL, poly(vinyl pyrrolidone) (PVP) and meglumine (MEG) (7:2:1 w/w) enhanced CEL solubility by approximately equal to 10.2-fold over that for the crystalline drug, and maintained the thermodynamic stability of the amorphous drug. However, MEG alone was unable to stabilize the amorphous CEL against thermally-induced crystallization, and so gave no solubility advantage. The PVP-MEG combination provided a 'synergistic' enhancement of CEL solubility, as compared to their use alone in the amorphous systems. Phase-solubility studies provided greater insight into molecular mechanisms underlying stability and solubility of these amorphous systems. MEG exhibited phase-specific interaction with CEL molecules, when stabilized by PVP in the amorphous state. The higher solubility of CEL from ternary amorphous systems was also thermodynamically favored, as analyzed by van't Hoff plots. A possible molecular level interaction of MEG with PVP-stabilized amorphous CEL seems to be responsible for the solubility advantage of the CEL-PVP-MEG ternary amorphous system.

Calorimetry, Differential Scanning↗
PubMed1990

[The value of magnesium pyrrolidone carboxylate in true cervix dystocia. A double blind versus placebo study].

The efficacy of spasmolytics in cervix dystocia during labor is very contested. For this reason the authors studied the action of pyrrolidone carboxylate of magnesium for this indication in a double-blind versus placebo study (48 patients divided in two groups). Strict inclusion criteria and homogeneity of the two groups of patients allowed them to find out that the use of this particular magnesium salt reduced significantly the length of labor. Consequently the authors assess that spasmolytics work not only through their placebo effect, which is thought by some authors.

Adult↗
PubMed1978

Responses to polyvinyl pyrrolidone and pneumococcal polysaccharide in protein-deficient mice.

Indirect haemagglutination titres induced by polyvinyl pyrrolidone (PVP) or pneumococcal polysaccharide Type III (S111) were determined in mice maintained on a 4% albumin diet from weaning and normally-fed littermates. Responses to PVP, given intravenously (i.v.) or intraperitoneally (i.p.), were elevated by protein-deficiency at low antigen doses and increasingly depressed at high doses. Increases in the duration of protein-deficiency generally improved these responses. The persistence of tolerance was reduced by protein-deficiency and priming was evident in both groups when tolerance was broken. The low protein diet depressed responses to moderate doses of S111 given i.p. to C57Bl mice, but such responses were normal in BALB/c mice and in C57Bl mice injected i.v. High doses of S111 (i.p., i.v.) elicited poor responses in deficient mice. These findings are discussed in relation to previous studies using other antigens, with a view to elucidating mechanisms responsible for the effects of protein-deficiency.

Animals↗
PubMed1989

Different modes of action of 3-amino-1-hydroxy-2-pyrrolidone (HA-966) and 7-chlorokynurenic acid in the modulation of N-methyl-D-aspartate-sensitive glutamate receptors.

The N-methyl-D-aspartate (NMDA)-sensitive glutamate receptors are known to be inhibited by 3-amino-1-hydroxy-2-pyrrolidone (HA-966) and 7-chlorokynurenic acid (Cl-KYN), which act at the glycine-regulated allosteric modulatory center. In this work we show that, in synaptic membranes prepared from rat brain, Cl-KYN and HA-966 inhibit the binding of [3H]glycine. Moreover, Cl-KYN can also completely inhibit the binding of [3H]glutamate to the primary transmitter recognition site for the NMDA receptor, whereas HA-966 only partially reduces this binding. Cl-KYN also abolishes the binding of the NMDA receptor antagonist [3H]3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP). In contrast, HA-966 increases [3H]CPP binding, affecting the affinity but not the maximal number of binding sites. This increase is inhibited by glycine and Cl-KYN. The binding of [3H] (+)-5-methyl-10,11-dihydro-5H-dibenzocyclohepten-5,10-imine maleate (MK-801), used as an index of NMDA receptor activation, is completely inhibited by Cl-KYN but only partially by HA-966. In addition, HA-966, but not Cl-KYN, increases the potency of CPP in inhibiting [3H]MK-801 binding. Our results demonstrate that Cl-KYN and HA-966 differ in their ability to modulate the NMDA receptor, perhaps acting at distinct but overlapping recognition sites. Furthermore, our results suggest that agonist and antagonist recognition sites of the NMDA receptor may be independently regulated by glycine and HA-966, which would result, respectively, in a positive and negative allosteric modulation of the NMDA receptor complex.

Animals↗
PubMed1989

Pyrrolidone carboxylic acid in acute and chronic alcoholism. Preclinical and clinical studies.

2-Pyrrolidone-5-carboxylic acid (PCA) is a cyclic derivative of glutamic acid, physiologically present in mammalian tissues. We herein report preclinical pharmacology experiments showing that PCA releases GABA from the cerebral cortex of freely-moving guinea-pigs and displays anti-anxiety effects in a simple approach-avoidance conflict situation in the rat. In clinical pharmacology experiments, PCA significantly shortens the plasma half-life of ethanol during acute intoxication. In chronic alcoholics a treatment with PCA (2g/day per 30 days) significantly hastens the recovery to physiological values of plasma gamma-glutamyl transferase activity and of the urinary excretion of glucaric acid, which are considered suitable markers of the trend of the alcoholic disease. The evidence emerging from preclinical and clinical studies strongly suggests that, by combining central anxiolytic actions with the peripheral recovery of the antioxidant defense system in the liver, PCA should be further investigated as an interesting endogenous molecule possibly helpful in the therapy of alcoholism.

Alcoholic Intoxication↗
PubMedDate not supplied

[Characteristics of the effect of 2-pyrrolidone acetamide (piracetam) on energy coupling in rat skeletal muscle mitochondria during cold stress].

Effects of 2-pyrrolidone acetamide (piracetam) on energetic state of mitochondria were studied in skeletal muscles of intact and ovaryectomized rats under conditions of drastic cooling (4 min swimming at 10 degrees). Readministration of piracetam was shown to cause uncoupling of oxidation and phosphorylation in mitochondrial respiratory chain (a decrease in respiratory control by Chance), as well as the drug increased the rate of O2 consumption in presence of oligomycin and decreased the uncoupler stimulating action on respiration in the group of intact animals. The alterations observed were most distinct in rats with cold stress, which was followed by piracetam administration, except of the rate of respiration stimulation, distinctly increased in presence of uncoupler. Piracetam did not exhibit any noticeable effects on the patterns of respiration studied in skeletal muscles of ovaryectomized rats. Protective properties of piracetam in cooling are discussed.

Animals↗
PubMed1988

[Effect of 2-pyrrolidone and gamma-butyrolactone on the rate of 14C-leucine incorporation into the proteins of different brain structures and of their arterial tissues].

The ability of cyclic GABA and GHBA derivatives--2-pyrrolidone and gamma-butyrolactone--to increase markedly the inclusion of 14C-leucine in the proteins of hypothalamus and cerebral arteries both normally and in condition of cerebral blood supply disturbances produced by unilateral 20 min ligation of a common carotid artery has been demonstrated.

4-Butyrolactone↗
PubMed1979

[Peritoneal irrigation and lavage using iodinated polyvinyl-pyrrolidone in acute generalized peritonitis (70 cases treated in an intensive care unit)].

The authors report 70 cases of severe acute generalise peritonitis treated during the immediate postoperative periode by peritoneal irrigation-lavage using iodinated polyvinyl-pyrrolidone for 16 days. All of the patients were hospitalised in an intensive care unit because of septicaemia, respiratory distress, acute renal failure, etc. After an aetiological study of these cases of peritonitis, the technique of installation and surveillance and the complications of peritoneal irrigation-lavage are analysed. The results in this series confirm the efficacy of the technique as long as it is used from the outset, immediately following the onset of peritonitis.

Acute Disease↗
PubMedDate not supplied

[Action of 2-pyrrolidone acetamide (piracctam) on the electron transfer respiratory chain in rat liver mitochondria].

Repeated administration of 2-pyrrolidone acetamide (pyracetam; a structural analogue of GABA) at a dose of 100 mg/kg led to considerable alteration in systems of oxidative phosphorylation in liver mitochondria of intact rats. These alterations consisted in a decrease in the value of respiratory control when glutamate and malate were used as substrates, an increase in the rate of exogenous NADH oxidation in the amytal-antimycin A resistenant pathway and reduction in concentrations of cytochromes c, c1 and a. These effects were not observed in castrated rats. The effect of pyracetam on respiratory chain of liver mitochondria appears to be realized via regulation of sexual glands functions.

Animals↗
PubMed1984

Effect of polyvinyl pyrrolidone derivative compound on production of interleukin-1 by monocytes.

We studied the effect of 1-acetamide, 2-pyrrolidone (PVP-A), a B-cell mitogen derivative, on interleukin-1 (IL-1) production by peripheral blood monocytes. The compound was capable of inducing monocytes to produce IL-1 to an extent significantly lower than that induced by lipopolysaccharide (LPS). However, addition of PVP-A in conjunction with LPS resulted in IL-1 superinduction. Furthermore, PVP-A addition to monocytes of patients with Alzheimer's disease (AD) restored diminished IL-1 production by these cells to levels comparable with monocytes from age-matched healthy individuals. We also examined the effect of PVP-A on immunoglobulin (Ig) synthesis in vitro. PVP-A increased the production of both IgM and IgG by peripheral blood lymphocytes (PBL) in response to pokeweed mitogen (PWM). We conclude, since Ig synthesis of B-cells requires monocytes, that perhaps PVP-A activated monocytes can boost B-cells resulting in augmented Ig production.

Adult↗
PubMed1995

Effect of pyrrolidone carboxylate (PCA) and pyridoxine on liver metabolism during chronic ethanol intake in rats.

Rats subjected to chronic ethanol intake for a period of 28 days showed significant elevation in blood ethanol levels, a marked decrease in hepatic reduced glutathione (GSH) content and a decrease in liver tryptophan pyrrolase (TPO) activity. A daily intraperitoneal injection of a combined solution of pyrrolidone carboxylate (PCA) and vitamin B6 (pyridoxine hydrochloride) (0.3 mmoles/kg) into ethanol-treated rats resulted in the blood ethanol levels becoming significantly reduced, while the hepatic GSH content and TPO activity were markedly elevated. Our results support the view that PCA and pyridoxine operate to restore the redox imbalance of the hepatocytes caused by chronic alcohol intake.

Alcoholism↗
PubMedDate not supplied

Effects of nefiracetam (DM-9384), a pyrrolidone derivative, on brain monoamine systems.

The pyrrolidone cyclic gamma-aminobutyric acid (GABA) derivative nefiracetam [DM-9384; N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide] has been shown to enhance acquisition and ameliorate amnesia in different learning tasks in rodents. In the present study, the effects of nefiracetam on the brain monoamine systems were studied. Male, adult Sprague-Dawley rats were treated with nefiracetam in single doses (0, 1, 3, 10, 30 or 100 mg/kg, p.o.) and analyzed after 1 and 4 hr, or treated by daily doses (0, 1, 3, 10 or 30 mg/kg, p.o.) for 2 weeks. In general, no or only weak effects were observed on tissue monoamine levels, either following acute or 14 days treatment with nefiracetam. Acute administration of intermediate doses of nefiracetam induced minor increases in dopamine (DA) and homovanillic acid (HVA) tissue levels in the striatum, while hypothalamic 3,4-dihydroxyphenylacetic acid (DOPAC) decreased at 1 hr. Noradrenaline (NA) and serotonin (5-HT) levels increased in some regions after higher doses of nefiracetam. Increases in 5-hydroxyindoleacetic acid (5-HIAA) were also seen at 4 hr, but only after the 3 mg/kg dose. Minor decreases of HVA and DOPAC levels were seen in some regions after treatment with various doses of nefiracetam for 14 days, while an increase in 5-HT levels was observed occasionally. Using in vivo microdialysis in freely moving animals, no significant effects on extracellular levels of HVA, DOPAC and 5-HIAA in the striatum or of HVA, DOPAC and NA levels in the dorsal hippocampus were seen after acute administration of nefiracetam. On the other hand, extracellular hippocampal 5-HIAA levels decreased by 20% after the 1 and 3 mg/kg doses. Nefiracetam, in a concentration range of 1 nM to 10 microM, did not affect the in vitro synaptosomal uptake of [3H]NA and [3H]5-HT in the cortex or of [3H]DA in the striatum. Taken together, nefiracetam appears to exert minor, regionally restricted and not dose-dependent effects on the monoamine systems following either acute or repeated administrations in normal rats. A direct or indirect, possible GABA-mediated, influence of nefiracetam may underlie the modest changes seen on monoamines. The cognitive-enhancing action of nefiracetam does not seem to be related to effects on presynaptic monoamine functions.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1995

Direct or indirect skin lipid-ordering effect of pyrrolidone carboxylate sodium after topical treatment with penetration enhancers.

The structural changes in the lipid of the excised skin of nude mice and the porcine stratum corneum was investigated by in vitro treatment with vitamin C, oleic acid, or DMSO. The CH2 stretching vibrational peaks of lipid near 2920 cm-1 (asymmetric) and 2850 cm-1 (symmetric) shifted to higher wavenumber due to the lipid-disorder after in vitro treatment with above enhancers. The spectral shift of the asymmetric CH2 band was more sensitive than that of the symmetric CH2 band. The higher wavenumber of CH2 stretching bands decreased gradually to the lower region after co-treatment or posttreatment with pyrrolidone carboxylate sodium (PCA Na). Such a decrease was dependent on the PCA Na concentration and the time of treatment. The higher the concentration of PCA Na used, the lower value of the permeability coefficient of vitamin C through the excised skin and the downward spectral shift of asymmetric CH2 band were obtained. When PCA Na coexisted with vitamin C in the cell donor compartment, a competitive effect between PCA Na and vitamin C was found. The oleic acid was supposed to directly insert it into the lipid structure to form a rigid structure, leading to larger spectral shift of both stretching bands but lesser restoring ability after PCA Na treatment. However, DMSO only displaces water from the lipid head groups and protein domain of skin to indirectly loosen the lipid structure, resulting in lesser spectral shift of the CH2 stretching bands to higher region, which was easier and better restoration after PCA Na application. The PCA Na enabled to restore the disordered lipid structure to order state might be attributed to PCA Na previously penetrated into skin and then absorbed water to directly or indirectly rearrange the disordered lipid bilayer structure.

Absorption↗
PubMedDate not supplied

The acute toxicity and in vivo antitumour activity against L1210 leukemia of triphenyltin 3,5-diisopropylsalicylate, bis (di-n-butyl-(s)-2-pyrrolidone-5-carboxylato)tin oxide and di-n-butyltin bis(3-amino-4-methylbenzoate).

Triphenyltin 3,5-di-isopropylsalicylate, compound 1, is characterized by a maximum tolerated dose (MTD) of 20 mg/kg. Bis[di-n-butyl(2-pyrrolidone-5-carboxylato)tin] oxide, compound 2, and (di-n-butyltin bis(3-amino-4-methyl-benzoate), compound 3, exhibit similar acute toxicities (MTD = 8 mg/kg) despite their lower in vitro activity, as compared to compound 1, against the two human tumor cell lines MCF-7 and WiDr. All three are inactive in vivo against L1210 leukemia in mice.

Aminobenzoates↗
PubMed1993

Audiogenic seizures in magnesium-deficient mice: effects of magnesium pyrrolidone-2-carboxylate, magnesium acetyltaurinate, magnesium chloride and vitamin B-6.

Magnesium deficiency in mice causes and increases audiogenic seizures. This effect was reversed by oral administration of magnesium acetyltaurinate (ATaMg), magnesium pyrrolidone-2-carboxylate (PCMH), MgCl2. When treatment was discontinued, audiogenic seizures recurred only in the groups treated with PCMH or MgCl2. Following intraperitoneal administration of AtaMg, the mice were protected against audiogenic seizures after 4 h and this protection persisted for up to 72 h after the treatment. With the other magnesium salts (PCMH and MgCl2) maximum protection occurred by 6 h after the injection, but after that time the number of seizures increased sharply. Intraperitoneal taurine alone only reduced the severity of the audiogenic seizures. The length of treatment needed to inhibit audiogenic seizures was reduced by treatment with a combination of vitamin B-6 (a magnesium fixing agent) and PCMH or MgCl2. However this combination of vitamin B-6 and magnesium salts did not prevent the recurrence of audiogenic seizures, which was only achieved by ATaMg. The results suggest that audiogenic seizures in magnesium-deficient mice form a model of magnesium depletion. This depletion is completely inhibited by the combination of an inhibitory neurotransmitter (taurine) and magnesium, in the form of magnesium acetyltaurinate.

Acoustic Stimulation↗