Studies of NMDA receptor function and stoichiometry with truncated and tandem subunits [PDF]
The subunits that compose eukaryotic glutamate ion channel receptors have three transmembrane domains (TMs) and terminate with intracellular tails that are important for controlling channel expression and localization.
Colquhoun, D., Schorge, S.
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ISOXAZOLE – A POTENT PHARMACOPHORE
Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group & found in many β-lactamase resistant antibiotics, such as cloxacillin ...
S. Raja, Krishna Veni Chikkula
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Hippocampal‐Specific Insulin Resistance Elicits Synaptic Effects on Glutamate Neurotransmission
In animals with hippocampal‐specific insulin resistance, reduced vGluT2 and synaptophysin expression resulted in lowered synaptic glutamate concentrations. These animals also exhibited reduced serine phosphorylation of GluA1 (green postsynaptic receptor) and reduced expression of GluN2B (purple postsynaptic receptor).
Jennifer M. Erichsen+5 more
wiley +1 more source
Benzo-fused Lactams from a Diversity-oriented Synthesis (DOS) Library as Inhibitors of Scavenger Receptor BI (SR-BI)-mediated Lipid Uptake [PDF]
We report a new series of 8-membered benzo-fused lactams that inhibit cellular lipid uptake from HDL particles mediated by Scavenger Receptor, Class B, Type I (SR-BI).
Bennion, Melissa+13 more
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A trace amine beta‐phenylethylamine is anxiolytic and reduces brain acetylcholine at 12 μg/L, but elevates anxiety and cortisol levels at 1000 μg/L. Acute tryptamine at 7 mg/L is anxiogenic, reduces shoaling and social interaction, but elevates brain acetylcholine and cortisol levels. Acute tyramine at 15 μg/L, and octopamine at 125, 500, and 1500 μg/L,
Thalia M. Quintanilha+10 more
wiley +1 more source
Chalcones as versatile synthons for the synthesis of 5- and 6-membered nitrogen heterocylces [PDF]
Chalcones belong to the flavonoid family which constitutes one of the major classes of naturally occurring oxygen heterocyclic compounds. The alpha,beta-unsaturated carbonyl system of chalcones possesses two electrophilic reactive centers allowing them ...
Albuquerque, Hélio+3 more
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Synthetic isoxazole as antiplatelet agent
Abstract Nine synthetic isoxazoles were evaluated as antiplatelet agents and studied the possible mechanism of more active compound. The initial screening was evaluating all compounds against platelet aggregation assays. The most active compound was isoxazole 8 showing an inhibition of platelet aggregation around 70%. In subsequent experiments, ADP and
Gutierrez, Margarita+4 more
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Substituent effects in isoxazoles: identification of 4-substituted isoxazoles as Michael acceptors
Crystallographic and theoretical studies have been used to investigate substituent effects, which are manifest in electrochemical and yeast-catalysed reactions of 4- and 5-acyl-, alkoxycarbonyl-, cyano- and phenyl-substituted isoxazoles. The results show that isoxazoles substituted at the 4-position with π-electron-withdrawing substituents have ...
Lee, Connie+6 more
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CXX.—Action of alkalis on the nitro-compounds of the paraffin series. Part II. Reactions and constitution of methazonic acid and the mode of formation of isoxazoles [PDF]
Wyndham R. Dunstan, Ernest Goulding
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Discrimination of Potent Inhibitors of Toxoplasma gondii Enoyl-Acyl Carrier Protein Reductase by a Thermal Shift Assay [PDF]
Many microbial pathogens rely on a type II fatty acid synthesis (FASII) pathway that is distinct from the type I pathway found in humans. Enoyl-acyl carrier protein reductase (ENR) is an essential FASII pathway enzyme and the target of a number of ...
Afanador, G.A.+18 more
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