YM-09151-2(cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide) is a new benzamide which has been reported to be an antagonist of dopamine (DA) at D1-type DA receptors. In the present study, we have examined the extent of the interaction of YM-09151-2 with D2-type ...
In anesthetized dogs, YM-09538, a new sulfonamide-substituted phenylethylamine, competitively antagonised the phenylephrine-induced vasopressor response with a DR10 of 0.50 mg/kg i.v. and the isoproterenol-induced positive chronotropic response with a DR10 of 0.66 mg/kg, i.v., indicating that YM...
We compute the β-function of a YM theory, broken to U(1), by evaluating the coupling constant renormalization in the broken phase. We perform the calculation in the unitary gauge where only physical particles appear and the theory looks like a version of QED containing massive charged spin-1 pa...
The cerebral protective actions of a new thyrotropin releasing hormone (TRH) analogue, YM-14673, (Nα-[[(S)-4-oxo-2-azetidyl-carbonyl]-l- histidyl-L-prolinamide]dihydrate), were compared with those of CDP-choline (cerebral metabolic enhancer) and naloxone in rats rats subjected to unilateral car...
The present study was designed to determine whether the 1-form of YM-12617, which was developed recently as an α1-adrenoceptor blocker, is capable of protecting the myocardium from hypoxia-induced disturbances of cardiac function and metabolism. Isolated rabbit hearts were perfused for 25 min u...
1.1. Homogenates of bovine retinas were used to study the capacities of two new dopamine (DA) receptor agonists, e.g. YM 435 and A 77636, to interact with D1 receptors.2.2. Adenylate cyclase experiments. YM 435 and A 77636 enhanced cAMP accumulation, with EC50 values of 1.97 μM and 22.9 nM, res...
We studied the antischistosomal activity of betulin, betulinic acid and its 9 triphenylphosphonium derivatives characterized by a covalently linkage of the hydrophobic fragment of triterpenoid at C(2)- or C(30)-position with the triphenylphosphonium moiety via a hydrocarbon bridge. The triphenyl...
Under moderate conditions in the presence of a demethylating reagent, such as iodide, methyl 2,2,-difluoro-2-(fluorosulfonyl)acetate (MDFA) releases difluorocarbene, which in the presence of triphenylphosphine forms difluoromethylene triphenylphosphonium ylide. When the process is carried out al...
The acylphosphoranes 5 formed in a highly selective and sequential manner from the reaction of N-substituted anthranilic acids 1 and N-phenyl(triphenylphosphoranylidene)ethenimine 2 undergo intramolecular Wittig cyclization on the imide carbonyl to afford the pyrrolo- and pyrido[1,2-a]quinolones...
3-Chloropentane-2,4-dione exists, in solution, almost exclusively as enol tautomer, which undergoes a complex reaction with dialkyl acetylenedicarboxylates and triphenylphosphine to produce alkyl 5,5-diacetyl-2-oxo-3-(triphenylphosphoranylidene)tetrahydrofuran-4-carboxylates in moderate to fairl...
Alkyl 2-chloroacetoacetates undergo a complex reaction with dialkyl acetylenedicarboxylates in the presence of triphenylphosphine to produce a nearly 1:1 mixture of the cis/trans isomers of dialkyl 5-acetyl-2-oxo-3-(triphenylphosphoranylidene)tetrahydrofuran- 4,5-dicarboxylates in excellent yields.
Dynamic 1H NMR (500 MHz) investigation of aryl-N-(arylsulfonyl)-N-(triphenylphosphoranylidene)imidocarbamates in CDCl3, CD3COCD3, and CD3OD at the temperature range of 183–298 K is reported. The observed free energy barriers (almost 12 kcal mol−1) are attributed to conformational isomerization ...
In th presence of zinc and a catalytic amount of cuprous chloride, ethyl 4-bromo-4,4-difluoro-3-oxo-2-(triphenylphosphoranylidene)butanoate 1 reacted with carbonyl compounds to give the gem-difluoromethylenated 2-(triphenylphosphoranylidene)-δ-lactones 4 in moderate to high yields.
BackgroundDynamic contrast enhanced (DCE) breast MRI is highly sensitive for breast cancer and requires gadolinium-based contrast agents (GBCA)s, which have potential safety concerns.
Three-dimensional T1-weighted MRI of mouse brain in vivo (9.4 T, 80 μm isotropic resolution) identified assemblies of nerve cell bodies in the habenula, hippocampal formation, locus coeruleus, dorsal motor nucleus of vagus, and nucleus ambiguus as high signal intensities, while suppressing the ...
Three fatty acid glycosides, designated pescaprosides A, B, and E, have been isolated from Ipomoea pescaprae (family Convolvulaceae). Chemical studies on pescaproside E, the major product, led to its characterisation as a pentaglycoside of 11-hydroxyhexadecanoic acid. Its sugar chain was esterif...
The widespread use of immobilized metal-affinity chromatography (IMAC) for fast and efficient purification of recombinant proteins has brought potentially toxic transition elements into common laboratory usage. However, there are few studies on the leaching of metal from the affinity resin, such...
In the present investigation a glycerol based carbon was synthesized by partial carbonization of glycerol using concentrated H2SO4 in the molar ratio 1:4. The carbonized material was further treated at 120 °C and 350 °C to obtain the carbons GBC-120 and GBC-350 respectively. The samples were c...
A dye being reluctant to degradation due to their structural complexity requires a cost-effective and an eco-friendly technique of degradation. Present study, Bacillus fermus isolated from Annona reticulata, gram positive bacteria was employed for the degradation of Acid Blue-9 dye. Minimal salt...
To avoid multidrug resistance and tumour recurrence, photodynamic therapy (PDT) was emerging as an alternative therapy and its efficiency was related to photosensitizer (PS) efficiency, oxygen concentration and light characteristic. Methylene blue (MB) molecules as PSs were loaded in silica (sil...
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