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Abstract A new HPLC method was developed using a chiral column to efficiently separate four 1′′-hydroxybufuralol (1′′-OH-BF) diastereomers that are major metabolites of bufuralol (BF). Employing this method, we examined diastereomer selectivity in the formation of 1′′-OH-BF from BF...
Abstract Schild regressions for the selective AT 1 and AT 2 receptor antagonists, losartan and PD123319 ( S -+-1-(4-dimethylamino-3-methylphenyl)methyl-5-diphenylacetyl-4,5,6,7-tetrahydro-1 H -imidazol4,5- c pyridine-6-carboxilic acid), respectively, were calculated to analyze the heterogeneity...
Abstract Agonist efficacy may influence the magnitude of neuroadaptation in response to chronic drug exposure. Chronic administration of either Δ 9 -tetrahydrocannabinol (THC), a partial agonist, or R -(+)-2,3-dihydro-5-methyl-3-(morpholinyl)methylpyrrolo-1,2,3- de...
Abstract Previous studies have shown that 6-methoxy-8-hydroxylaminoquinoline (MAQ-NOH), an N -hydroxy metabolite of the antimalarial drug, primaquine, is a direct-acting hemolytic agent in rats. To investigate the mechanism underlying this hemolytic activity, the effects of hemotoxic...
Abstract During myocardial ischemia and reperfusion, nitric oxide ( ⋅ NO) was shown to exert either beneficial or detrimental effects. Uncoupled ⋅ NO synthases (NOS) can generate superoxide anion under suboptimal concentrations of substrate and cofactors. The aim of our study was to...
Abstract Non-Hodgkin lymphomas usually become resistant to chemotherapy and relapse due to the their intense antiapoptotic robustness. Furthermore, the slow growth of these malignancies limits the effectiveness of drugs aimed mainly at the proliferative pathways. Because protein tyrosine kinases...
Abstract Assessing the inducibility of CYP3A4 by various xenobiotics can predict potential drug interactions. In the present investigation, human hepatoma cells were stably integrated with either the CYP3A4 enhancer region and a luciferase reporter gene or the CYP3A4-luciferase construct and the...
Abstract ATP-sensitive potassium (K ATP ) channel openers (KCOs) have been shown to inhibit spontaneous myogenic contractile activity of the urinary bladder, a mechanism hypothesized to underlie detrusor instability and symptoms of overactive bladder. However, the therapeutic utility of KCOs has...
Abstract We have identified a new benzopyran derivative, 3-(4-methoxy) phenyl-4-4-2-(1-piperidinyl)ethoxyphenylmethyl-2 H -1-benzopyran-7-ol hydrochloride (CHF 4227), with improved in vivo estrogen agonist/antagonist effects. CHF 4227 binds with high affinity to the human estrogen receptor-α and...
Abstract Nootropic drug nefiracetam and related compounds are used in diseases with learning and memory deficits. Recent studies have implicated relationships between learning, memory, and chronic pain. Thus, in the present report, we have studied the effects of nootropic drug nefiracetam on the...
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