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Showing 1-30 of 124 results for "240931" within Papers

Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors.

Sumeyye Turkoglu et al.

Bioorganic & medicinal chemistry, 20(7), 2208-2213 (2012-03-06)

Site-directed mutagenesis has been used to change three amino acid residues involved in the binding of inhibitors (Asn67Ile; Gln92Val and Leu204Ser) within the active site of human carbonic anhydrase (CA, EC 4.2.1.1) II (hCA II). Residues 67, 92 and 204

Vagus nerve stimulation has antidepressant effects in the kainic acid model for temporal lobe epilepsy.

Annelies Grimonprez et al.

Brain stimulation, 8(1), 13-20 (2014-12-03)

Depression is the most common psychiatric comorbidity in epilepsy patients. The lack of success with current pharmacological interventions for this patient population, highlights the importance of optimizing non-pharmacological neuromodulatory treatments such as vagus nerve stimulation (VNS). Studies on the antidepressant

An efficient, regioselective amination of 3,5-disubstituted pyridine N-oxides using saccharin as an ammonium surrogate.

Robert P Farrell et al.

Organic letters, 15(1), 168-171 (2012-12-14)

A process for the regioselective amination of unsymmetrical 3,5-substituted pyridine N-oxides has been developed utilizing cheap, readily available saccharin as an ammonium surrogate. High conversions of the corresponding saccharin adducts have been achieved under mild reaction conditions. In situ deprotection

Artificial sweeteners stimulate adipogenesis and suppress lipolysis independently of sweet taste receptors.

Becky R Simon et al.

The Journal of biological chemistry, 288(45), 32475-32489 (2013-09-27)

G protein-coupled receptors mediate responses to a myriad of ligands, some of which regulate adipocyte differentiation and metabolism. The sweet taste receptors T1R2 and T1R3 are G protein-coupled receptors that function as carbohydrate sensors in taste buds, gut, and pancreas.

Expression of Quinone Reductase-2 in the Cortex Is a Muscarinic Acetylcholine Receptor-Dependent Memory Consolidation Constraint.

Akiva N Rappaport et al.

The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(47), 15568-15581 (2015-11-27)

Learning of novel information, including novel taste, requires activation of neuromodulatory transmission mediated, for example, by the muscarinic acetylcholine receptors (mAChRs) in relevant brain structures. In addition, drugs enhancing the function of mAChRs are used to treat memory impairment and

Melatonin administration alters nicotine preference consumption via signaling through high-affinity melatonin receptors.

William J Horton et al.

Psychopharmacology, 232(14), 2519-2530 (2015-02-24)

While it is known that tobacco use varies across the 24-h day, the time-of-day effects are poorly understood. Findings from several previous studies indicate a potential role for melatonin in these time-of-day effects; however, the specific underlying mechanisms have not

Saccharin: a toxicological and historical perspective.

D L Arnold et al.

Toxicology, 27(3-4), 179-256 (1983-07-01)

Saccharin, first synthesized in 1879, eventually became popular as an inexpensive substitute for sugar, particularly as a non-caloric sweetner. The dispute concerning the safety of saccharin for human consumption is almost as old as saccharin itself. In this article, the

Effect of chronic exposure to rimonabant and phytocannabinoids on anxiety-like behavior and saccharin palatability.

Lesley D O'Brien et al.

Pharmacology, biochemistry, and behavior, 103(3), 597-602 (2012-10-30)

The acute effects of cannabinoid compounds have been investigated in animal models of anxiety-like behavior and palatability processing. However, the chronic effects of cannabinoids in such models are poorly understood. Experiment 1 compared the effects of both acute and chronic

Sweet success, bitter defeat: a taste phenotype predicts social status in selectively bred rats.

John M Eaton et al.

PloS one, 7(10), e46606-e46606 (2012-10-12)

For social omnivores such as rats and humans, taste is far more than a chemical sense activated by food. By virtue of evolutionary and epigenetic elaboration, taste is associated with negative affect, stress vulnerability, responses to psychoactive substances, pain, and

Role of nitrification in the biodegradation of selected artificial sweetening agents in biological wastewater treatment process.

N H Tran et al.

Bioresource technology, 161, 40-46 (2014-04-01)

The biodegradation of the six artificial sweetening agents including acesulfame (ACE), aspartame (ASP), cyclamate (CYC), neohesperidindihydrochalcone (NHDC), saccharin (SAC), and sucralose (SUC) by nitrifying activated sludge was first examined. Experimental results showed that ASP and NHDC were the most easily

Dynamic behavior of binary component ion-exchange displacement chromatography of proteins visualized by confocal laser scanning microscopy.

Qing-Hong Shi et al.

Journal of chromatography. A, 1257, 48-57 (2012-08-21)

Confocal laser scanning microscopy (CLSM) was introduced to visualize particle-scale binary component protein displacement behavior in Q Sepharose HP column. To this end, displacement chromatography of two intrinsic fluorescent proteins, enhanced green fluorescent protein (eGFP) and red fluorescent protein (RFP)

Assessment of the Effects of 6 Standard Rodent Diets on Binge-Like and Voluntary Ethanol Consumption in Male C57BL/6J Mice.

Simon Alex Marshall et al.

Alcoholism, clinical and experimental research, 39(8), 1406-1416 (2015-06-26)

In recent years, much attention has been given to the lack of reproducibility in biomedical research, particularly in preclinical animal studies. This is a problem that also plagues the alcohol research field, particularly in consistent consumption in animal models of

Saccharin and its salts.

IARC monographs on the evaluation of carcinogenic risks to humans, 73, 517-624 (2000-05-11)

Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamate.

Tomoko Minakuchi et al.

Journal of medicinal chemistry, 52(8), 2226-2232 (2009-03-26)

The beta-carbonic anhydrase (CA, EC 4.2.1.1) encoded by the gene Rv1284 (mtCA 1) of Mycobacterium tuberculosis shows appreciable catalytic activity for CO(2) hydration, with a k(cat) of 3.9 x 10(5) s(-1) and a k(cat)/K(m) of 3.7 x 10(7) M(-1) s(-1).

High locomotor reactivity to novelty is associated with an increased propensity to choose saccharin over cocaine: new insights into the vulnerability to addiction.

Nathalie Vanhille et al.

Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 40(3), 577-589 (2014-08-15)

Drug addiction is associated with a relative devaluation of natural or socially-valued reinforcers that are unable to divert addicts from seeking and consuming the drug. Before protracted drug exposure, most rats prefer natural rewards, such as saccharin, over cocaine. However

The disposition of saccharin in animals and man--a review.

A G Renwick

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 23(4-5), 429-435 (1985-04-01)

Recent studies on saccharin in animals and man have allowed a detailed understanding of its fate in the body. Saccharin is slowly absorbed from the gut but rapidly eliminated in the urine, largely by renal tubular secretion. Saccharin does not

Cloning, characterization and sulfonamide inhibition studies of an α-carbonic anhydrase from the living fossil sponge Astrosclera willeyana.

Anna Ohradanova et al.

Bioorganic & medicinal chemistry, 20(4), 1403-1410 (2012-01-31)

The α-carbonic anhydrase (CA, EC 4.2.1.1) Astrosclerin-3 previously isolated from the living fossil sponge Astrosclera willeyana (Jackson et al., Science 2007, 316, 1893), was cloned, kinetically characterized and investigated for its inhibition properties with sulfonamides and sulfamates. Astrosclerin-3 has a

pH-dependent solubility of indomethacin-saccharin and carbamazepine-saccharin cocrystals in aqueous media.

Amjad Alhalaweh et al.

Molecular pharmaceutics, 9(9), 2605-2612 (2012-08-08)

Cocrystals constitute an important class of pharmaceutical solids for their remarkable ability to modulate solubility and pH dependence of water insoluble drugs. Here we show how cocrystals of indomethacin-saccharin (IND-SAC) and carbamazepine-saccharin (CBZ-SAC) enhance solubility and impart a pH-sensitivity different

Effect of selective inhibition of monoacylglycerol lipase (MAGL) on acute nausea, anticipatory nausea, and vomiting in rats and Suncus murinus.

Linda A Parker et al.

Psychopharmacology, 232(3), 583-593 (2014-08-03)

To determine the role of the endocannabinoid, 2-arachodonyl glycerol (2-AG), in the regulation of nausea and vomiting. We evaluated the effectiveness of the potent selective monoacylglycerol lipase (MAGL) inhibitor, MJN110, which selectively elevates the endocannabinoid 2-AG, to suppress acute nausea

Taste reactivity alterations after streptozotocin microinjection into the mediodorsal prefrontal cortex.

Bernadett Nagy et al.

Behavioural brain research, 234(2), 228-232 (2012-07-07)

The mediodorsal prefrontal cortex (mdPFC), as an integrant part of the forebrain glucose-monitoring neural network, plays important roles in neural control of feeding. Previous studies suggested that streptozotocin (STZ) causes selective destruction of forebrain glucose-monitoring (GM) neurons leading to development

Cocaine decreases saccharin preference without altering sweet taste sensitivity.

Jennifer K Roebber et al.

Pharmacology, biochemistry, and behavior, 133, 18-24 (2015-03-31)

In rodents, saccharin consumption is suppressed when the sweet taste stimulus is paired with moderate doses of cocaine. Several hypotheses have been used to explain the seemingly contradictory effect of decreased consumption of a normally preferred substance following a highly

Distinct ethanol drinking microstructures in two replicate lines of mice selected for drinking to intoxication.

A M Barkley-Levenson et al.

Genes, brain, and behavior, 14(5), 398-410 (2015-05-20)

The High Drinking in the Dark (HDID) mice have been selectively bred for reaching high blood ethanol concentrations (BECs) following the limited access Drinking in the Dark (DID) test. We have shown previously that mice from the first HDID replicate

Selective breeding for differential saccharin intake as an animal model of drug abuse.

Marilyn E Carroll et al.

Behavioural pharmacology, 19(5-6), 435-460 (2008-08-12)

A positive relationship between the consumption of sweetened dietary substances (e.g. saccharin and sucrose) and drug abuse has been reported in both the human and other animal literature. The proposed genetic contribution to this relationship has been based on evidence

Status report on saccharin in humans.

G R Newell et al.

Journal of the National Cancer Institute, 61(2), 275-276 (1978-08-01)

Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii.

Alessandra Cincinelli et al.

Bioorganic & medicinal chemistry, 19(6), 1847-1851 (2011-03-08)

A high activity α-carbonic anhydrase (CA, EC 4.2.1.1) has been purified from various tissues of the Antarctic seal Leptonychotes weddellii. The new enzyme, denominated lwCA, has a catalytic activity for the physiologic CO(2) hydration to bicarbonate reaction, similar to that

Schedule of passive ethanol exposure affects subsequent intragastric ethanol self-infusion.

Tara L Fidler et al.

Alcoholism, clinical and experimental research, 33(11), 1909-1923 (2009-08-14)

Many studies have shown that chronic ethanol exposure can enhance later self-administration of ethanol, but only a few studies have identified critical parameters for such exposure. The present studies examined temporal and other parameters of chronic ethanol exposure on subsequent

Organ-specific modifying effects of phenobarbital, saccharin and antioxidants on 2-stage chemical carcinogenesis.

N Ito

Developments in toxicology and environmental science, 12, 359-369 (1986-01-01)

Functional characterization of the heterodimeric sweet taste receptor T1R2 and T1R3 from a New World monkey species (squirrel monkey) and its response to sweet-tasting proteins.

Bo Liu et al.

Biochemical and biophysical research communications, 427(2), 431-437 (2012-09-25)

The family C G protein-coupled receptor (GPCR) T1R2 and T1R3 heterodimer functions as a broadly acting sweet taste receptor. Perception of sweet taste is a species-dependent physiological process. It has been widely reported that New World monkeys and rodents are

Saccharin consumption increases food consumption in rats.

Nutrition reviews, 48(3), 163-165 (1990-03-01)

Neural computational prediction of oral drug absorption based on CODES 2D descriptors.

A Guerra et al.

European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)

A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising

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