Mammalian cells require specific transport mechanisms for the cellular uptake and release of endogenous nucleosides such as adenosine, and nucleoside analogs used in chemotherapy. We have identified a novel splice variant of the mouse equilibrative nucleoside transporter, mENT1, that results from the exclusion of exon 11 during pre-RNA processing. This variant encodes a truncated protein (mENT1...

Background: Neurotransmitter release is an essential link in cell communication of the nervous system. Many investigations have focused on gamma amino butyric acid (GABA)-ergic neurotransmission, because it has been implicated in the pathophysiology of several central nervous system disorders. To bypass complications related to homo- and heterosynaptic modulation and to avoid indirect interpret...

Hexahydro-3-alkyl-3H-oxazolo[3,4-a]pyridines 4–15 for the quantitative analysis of various aldehydes were obtained in good yield via condensation reaction 2-hydroxymethylpiperidine (2-HMP) with under mild conditions. When acrolein was used, bicyclic 17 obtained. This novel compound has suitable physical characteristics an analytical standard. The hexahydro-3-vinyl-3H-oxazolo[3,4-a]pyridine 16 c...

The study investigated the corrosion-inhibitory properties of three synthetic triazole Mannich bases on C1018 carbon steel using various electrochemical techniques. inhibitors, namely 4-amino-2-[(4-methylpiperazin-1-yl)methyl]-5-(pyridin-4-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (4MPT), 4-amino-2-[(piperidin-1-yl)methyl]-5-(pyridin-4-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (PPT) and 4-ami...

Many naturally occurring and synthetic compounds containing dihydrocyanopyridine and cyanopyran moiety show pharmacological properties. The aim of this study is to investigate the larvicidal and antioxidant potential of dihydrophenanthroline-3-carbonitrile derivatives 4a-f. A novel series of 2-amino-10-chloro-4,12-diphenyl-1,4,5,6-tetrahydrobenzo[j][1,7]phenanthroline-3-carbonitrile derivatives...

eEF-2K is a potential target for treating cancer. However, potent specific inhibitors for this enzyme are lacking. Previously, we identified 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile (DFTD) as an inhibitor of eEF-2K. Here we describe its mechanism of action against eEF-2K, on the basis of kinetic, mutational, and docking studies, and use chemoinformatic approaches to identi...

In synaptosomal membranes from rat and monkey brain cortex, the addition of petroselenic (18:1, cis-delta 6) acid, oleic (18:1, cis-delta 9) acid, and vaccenic (18:1, cis-delta 11) acid or their corresponding methyl esters at 0.5 mumol/mg of membrane protein caused a similar 7-10% decrease in the microviscosity of the membrane core, whereas at the membrane surface the microviscosity was reduced...

Dopamine D2 receptor blockade is thought to be mandatory for antipsychotic action because most of the currently used antipsychotics have high affinity at these receptors. Here, we examined the in vivo binding characteristics of the D2-like receptor antagonist [3H]nemonapride in rat brain areas including the striatum, olfactory lobes and frontal cortex and its inhibition by a series of D2 antago...

We determined whether spatial distributions of substrate uptake are heterogeneous within the area at risk during reperfusion. Quantitative autoradiography with imaging plates and two long-lived radioisotopes was applied to 15 open-chest, anesthetized rats subjected to 30 min of coronary artery ligation and 30 min of reperfusion. Regions showing increased β-methyl-[1-14C]heptadecanoic acid ([14C...

A single reaction product was formed during the incubation of 1.5 microM (5S,12R)-dihydroxy-6,14-cis-8,10-trans-[3H]icosatetraenoic acid (leukotriene B4, LTB4) for 30 min at 37 degrees C in 10 mM potassium phosphate buffer (pH 7.5) with 100 microM NADPH and the 150,000 X g supernatant of sonicated human polymorphonuclear leukocytes (PMN). The reaction product exhibited the same mobility on reve...