Tag: M.W:200-300

In an article, author is Anand, Devireddy, once mentioned the application of 4246-51-9, Product Details of 4246-51-9, Name is 3,3′-((Oxybis(ethane-2,1-diyl))bis(oxy))bis(propan-1-amine), molecular formula is C10H24N2O3, molecular weight is 220.3092, MDL number is MFCD00059850, category is Benzisoxazole. Now introduce a scientific discovery about this category.

Substrate Controlled Synthesis of Benzisoxazole and Benzisothiazole Derivatives via PhI(OAc)(2)-Mediated Oxidation Followed by Intramolecular Oxidative O-N/S-N Bond Formation

A phenyliodine(III) diacetate (PIDA)-mediated, highly efficient and tandem approach for the synthesis of aryldiazenylisoxazolo(isothiazolo)arenes from simple 2-amino-N’-arylbenzohydrazides has been developed. The reaction proceeds via formation of (E)-(2=aminoaryl)-(aryldiazenyl)methanone as the key intermediate, followed by intramolecular oxidative O-N/S=N bond formation in one pot at room temperature. The quiet different reactivity of the substrate is due to the formation of a diazo intermediate which encounters a nucleophilic attack by carbonyl oxygen on the electrophilic amine to produce isoxazole products, as compared to the previous reports(1a,b,4) in which an N-acylnitrenium ion intermediate is intramolecularly trapped by an amine group.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 629-25-4, Name is Sodium Laurate, molecular formula is C12H23NaO2. In an article, author is Brown-Proctor, C,once mentioned of 629-25-4, Product Details of 629-25-4.

Synthesis and evaluation of 6-[C-11]methoxy-3-[2-[l-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole as an in vivo radioligand for acetylcholinesterase

6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (K-i = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 +/- 20 GBq/mu mol at end of synthesis, by the alkylation of the desmethyl precursor with [C-11]methyl trifluoromethanesulfonate in N,N dimethylformamide at room temperature. In vivo studies in mice demonstrated good blood brain permeability but essentially uniform regional brain distribution. Thus, despite in vitro and in vivo activity as an AChE inhibitor, 6-[C-11]methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole does not appear to be a good candidate for in vivo imaging studies of AChE in the mammalian brain. NUCL MED BIOL 26;1: 99-103, 1999. (C) 1999 Elsevier Science Inc.

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Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 719-64-2, Name is 5-Chloro-3-phenylbenzo[c]isoxazole, molecular formula is , belongs to Benzisoxazole compound. In a document, author is Jadhav, VK, Application In Synthesis of 5-Chloro-3-phenylbenzo[c]isoxazole.

Sodium perborate: A facile synthesis of 1,2-benzisoxazole 2-oxides

An efficient and convenient methodology has been developed for the conversion of 2-hydroxy phenyl ketoxime to 1,2-benzisoxazole 2-oxide with sodium perborate (SPB) in glacial acetic acid under mild reaction conditions. Interestingly when the reaction was carried out under reflux condition deoximation was observed in quantitative yield.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 6106-21-4, Name is Sodium succinate hexahydrate. In a document, author is Schousboe, Arne, introducing its new discovery. SDS of cas: 6106-21-4.

GABA transport inhibitors and seizure protection: the past and future

Since it was first reported approximately 40 years ago that putative amino acid neurotransmitters, including GABA, would likely be inactivated by synaptic high-affinity transporters, there has been an exponential increase in interest in delineating the pharmacological characteristics of these transporters. During the 1980s and 1990s a large series of publications was devoted to a detailed characterization of neuronal and astroglial GABA transporters demonstrating important differences between these, a notion that turned out to be of relevance for the development of anticonvulsants targeting GABA transporters. The cloning era, leading to the identification of four proteins capable of transporting GABA across plasma membranes, has further boosted this research. Ultimately the clinically active antiepileptic drug, tiagabine, was developed and it was established that its mechanism of action involved inhibition of the GABA transporter-I (GATI). Current and future research is directed towards a better understanding of how extrasynaptic GABA receptors may be regulated via manipulation of extrasynaptic GABA levels, possibly involving extrasynaptic GABA transporters, most likely non-GATI transporters.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 68-04-2, Name is Sodium citrate, molecular formula is C6H5Na3O7, belongs to Benzisoxazole compound. In a document, author is GenreGrandpierre, A, introduce the new discover, SDS of cas: 68-04-2.

Catalysis of the Kemp elimination by antibodies elicited against a cationic hapten

Rather efficient catalysis of the decomposition of 5-nitro-benzisoxazole to the cyanophenol was observed with antibodies elicited against a cationic hapten structurally unrelated to the benzisoxazole substrate. The rate enhancement by the most active antibody is better than 10(4) and the reaction is catalyzed by a carboxylate group associated with a hydrophobic binding site. (C) 1997 Elsevier Science Ltd.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Related Products of 719-64-2, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 719-64-2, Name is 5-Chloro-3-phenylbenzo[c]isoxazole, SMILES is ClC1=CC2=C(C3=CC=CC=C3)ON=C2C=C1, belongs to Benzisoxazole compound. In a article, author is White, HS, introduce new discover of the category.

Correlation between anticonvulsant activity and inhibitory action on glial gamma-aminobutyric acid uptake of the highly selective mouse gamma-aminobutyric acid transporter 1 inhibitor 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and its N-alkylated analogs

The inhibitory effect of 3-hydroxy-4-amino-4,5,6,7-tetrahydro1,2-benzisoxazole (exo-THPO) and its N-methylated (N-methylexo-THPO) and N-ethylated (N-ethyl-exo-THPO) analogs, derived from gamma-aminobutyric acid (GABA) and 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (THPO) on GABA transport was investigated using cultured neocortical neurons (GABAergic) and astrocytes and cloned mouse GABA transporters GAT1-4 expressed in human embryonic kidney (HEK) 293 cells. Anticonvulsant activity was assessed after i.c.v. administration to Frings audiogenic seizure-susceptible mice. Anticonvulsant activity of the O-pivaloyloxymethyl prodrug of N-methyl-exo-THPO was assessed after i.p. administration. Results from these studies were compared with those obtained from similar studies with the novel anticonvulsant drug tiagabine, which acts via inhibition of GABA transport. exo-THPO and its N-alkyl analogs inhibited neuronal, astrocytic, and GAT1-mediated GABA transport but not GABA uptake mediated by GAT2-4. N-Methyl-exo-THPO was 8-fold more potent as an inhibitor of astrocytic versus neuronal GABA uptake. The IC50 value for inhibition of GABA uptake by GAT1 closely reflected its IC50 value for inhibition of neuronal uptake. Tiagabine was approximately 1000-fold more potent than exoTHPO and its alkyl derivatives as an inhibitor of GABA uptake in cultured neural cells and GAT1-expressing HEK 293 cells. exoTHPO, its alkylated analogs, and tiagabine displayed a time- and dose-dependent inhibition of audiogenic seizures after i.c.v. administration. N-Methyl-exo-THPO was the most potent anticonvulsant among the exo-THPO compounds tested and only slightly less potent than tiagabine. The findings suggest a correlation between anticonvulsant efficacy and selective inhibition of astroglial GABA uptake. Furthermore, results obtained with the N-methyl-exo-THPO prodrug demonstrate the feasibility of developing a glial-selective GABA uptake inhibitor with systemic bioavailability.

Related Products of 719-64-2, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 719-64-2.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Application of 35963-20-3, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, SMILES is O=S(C[C@]1(C2(C)C)C(C[C@]2([H])CC1)=O)(O)=O, belongs to Benzisoxazole compound. In a article, author is Bhana, N, introduce new discover of the category.

Risperidone – A review of its use in the management of the behavioural and psychological symptoms of dementia

Risperidone is a benzisoxazole derivative which has proven efficacy against the positive and negative symptoms of schizophrenia It has mon recently been investigated and shown efficacy as a treatment for the behavioural and psychological symptoms associated with dementia in the elderly. Risperidone has pharmacological properties resembling those of the atypical antipsychotic clozapine and an improved tolerability profile compared with the conventional antipsychotic haloperidol. Risperidone has antagonistic activity primarily at serotonin 5-HT2A and dopamine D-2 receptors. In the first 2 large, well controlled trials of an antipsychotic agent used in the treatment of elderly patients with Alzheimer’s dementia, vascular dementia or mixed demential risperidone 1 mg/day was at least as effective as haloperidol and superior to placebo. as assessed by the rating scales for global behaviour, aggression and psychosis. In extension phases of the 2 trials, clinical benefits were maintained for treatment periods of up to 1 year, with an incidence rate of tardive dyskinesia (2.6%) one-tenth of that seen with conventional antipsychotics. Risperidone, administered at a low dosage of 1 mg/day was associated with fewer extrapyramidal symptoms compared with haloperidol in elderly patients, Risperidone was well tolerated with no clinically relevant abnormalities in laboratory tests. vital signs or electrocardiogram results. Conclusion: The efficacy of risperidone has been demonstrated in the treatment of the behavioural and psychological symptoms associated with dementia in the elderly. Preliminary results from 1-year extension studies confirm the favourable efficacy and tolerability profile of risperidone 1 mg/day, Although head to head studies with other atypical antipsychotic agents are required and the long term use of the drug requires clarification, risperidone represents a generally well tolerated and effective treatment in the management of dementia-associated behavioural and psychological symptoms in the elderly.

Application of 35963-20-3, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 35963-20-3 is helpful to your research.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 4246-51-9, Name is 3,3′-((Oxybis(ethane-2,1-diyl))bis(oxy))bis(propan-1-amine), molecular formula is , belongs to Benzisoxazole compound. In a document, author is Liu, XC, SDS of cas: 4246-51-9.

Catalysis of benzisoxazole isomerization by molecularly imprinted polymers

A tailor-made catalytically active polymer catalyzing the benzisoxazole isomerization is described. Kinetic studies carried out in water/ethanol (3:1, v/v) at room temperature, showed a rate acceleration (k(MIP)/k(control)) of 7.2-fold compared to the control polymer. The imprinted polymer exhibits Michaelis-Menten kinetics with a K-m of 0.484 mM and a k(cat) of 0.205 min(-1). Compared with the uncatalyzed reaction, a rate enhancement ((k(cat)/K-m)/k(uncat)) of 4 x 10(4) fold was obtained. Substrate selectivity, accessible binding site analysis, dissociation constant determination, and inhibition study were also performed.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 4246-51-9, in my other articles. SDS of cas: 4246-51-9.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 629-25-4, Name is Sodium Laurate, SMILES is CCCCCCCCCCCC([O-])=O.[Na+], in an article , author is VANBEIJSTERVELDT, LEC, once mentioned of 629-25-4, COA of Formula: C12H23NaO2.

REGIONAL BRAIN DISTRIBUTION OF RISPERIDONE AND ITS ACTIVE METABOLITE 9-HYDROXY-RISPERIDONE IN THE RAT

Risperidone is a new benzisoxazole antipsychotic. 9-Hydroxy-risperidone is the major plasma metabolite of risperidone. The pharmacological properties of 9-hydroxy-risperidone were studied and appeared to be comparable to those of risperidone itself, both in respect of the profile of interactions with various neurotransmitters and its potency, activity, and onset and duration of action. The absorption, plasma levels and regional brain distribution of risperidone, metabolically formed 9-hydroxy-risperidone and total radioactivity were studied in the male Wistar rat after single subcutaneous administration of radiolabelled risperidone at 0.02 mg/kg. Concentrations were determined by HPLC separation, and off-line determination of the radioactivity with liquid scintillation counting. Risperidone was well absorbed. Maximum plasma concentrations were reached at 0.5-1 h after subcutaneous administration. Plasma concentrations of 9-hydroxy-risperidone were higher than those of risperidone from 2 h after dosing. In plasma, the apparent elimination half-life of risperidone was 1.0 h, and mean residence times were 1.5 h for risperidone and 2.5 h for its 9-hydroxy metabolite. Plasma levels of the radioactivity increased dose proportionally between 0.02 and 1.3 mg/kg. Risperidone was rapidly distributed to brain tissues. The elimination of the radioactivity from the frontal cortex and striatum-brain regions with high concentrations of 5-HT2 or dopamine-D-2 receptors-became more gradual with decreasing dose levels. After a subcutaneous dose of 0.02 mg/kg, the ED(50) for central 5-HT2 antagonism in male rats, half-lives in frontal cortex and striatum were 3-4 h for risperidone, whereas mean residence times were 4-6 h for risperidone and about 12 h for 9-hydroxy-risperidone. These half-lives and mean residence times were 3-5 times longer than in plasma and in cerebellum, a region with very low concentrations of 5-HT2 and D-2 receptors. Frontal cortex and striatum to plasma concentration ratios increased during the experiment. The distribution of 9-hydroxy-risperidone to the different brain regions, including frontal cortex and striatum, was more limited than that of risperidone itself. This indicated that 9-hydroxy-risperidone contributes to the in vivo activity of risperidone, but to a smaller extent than would be predicted from plasma levels. AUCs of both active compounds in frontal cortex and striatum were 10-18 times higher than those in cerebellum. No retention of metabolites other than 9-hydroxy-risperidone was observed in any of the brain regions investigated.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 68-04-2, Name is Sodium citrate, molecular formula is C6H5Na3O7, belongs to Benzisoxazole compound. In a document, author is Kociolek, Martin, introduce the new discover, Computed Properties of C6H5Na3O7.

Electrochemical reduction of 3-phenyl-1, 2-benzisoxazole 2-oxide on boron-doped diamond

The bioreduction of N-oxide compounds is the basis for the mode of action of a number of biologically active molecules. These compounds are thought to act by forming a reactive oxygen species through an intracellular reduction and subsequent redox cycling process within the organism. With these results in mind, the preliminary investigation into the electrochemical reduction of the benzisoxazole 2-oxide ring system was undertaken, with the thought that this class of compounds would reduce in a similar fashion to other N-oxide heterocycles. The electrochemical reduction of 3-phenyl-1,2-benzisoxazole 2-oxide on boron-doped diamond was studied using cyclic and square wave voltammetry as well as controlled potential electrolysis and HPLC for qualitative identification of the reaction products. It was found that the reduction proceeded with an initial quasi-reversible one-electron reduction followed by the very fast cleavage of either the endocyclic or exocyclic N-O bond. Subsequent electron transfer and protonation resulted in an overall two-electron reduction and formation of the 2-hydroxyaryl oxime and benzisoxazole. These results are analogous to those observed in the electrochemical reduction of other heterocyclic N-oxides albeit the reduction of the benzisoxazole N-oxides takes place at a more negative potential. However, these encouraging results warrant further investigation into the reduction potential of substituted benzisoxazole N-oxides as well as to elucidate and characterize the nature of the intermediate species involved. Copyright (c) 2014 John Wiley & Sons, Ltd.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 68-04-2. Computed Properties of C6H5Na3O7.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics