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Amiloride delays the ischemia-induced rise in cytosolic free calcium.
Test data are consistent with the involvement of Na-Ca exchange in the rise in Cai during ischemia, and Nai in the untreated heart was threefold greater than control, whereas in the amiloride-treated heart, Nai was not significantly different from control.
Raising High-Density Lipoprotein in Humans Through Inhibition of Cholesteryl Ester Transfer Protein: An Initial Multidose Study of Torcetrapib
These effects of CETP inhibition resemble those observed in partial CETP deficiency, and serve as a prelude to further studies in subjects with low HDL, or combinations of dyslipidemia, in assessing the role of CETp in atherosclerosis.
Mechanism of preconditioning. Ionic alterations.
The hypothesis that preconditioning attenuates the increase in [Ca2+]i, [Na-i, and [H-i]i during ischemia is supported, most likely because of reduced stimulation of Na(+)-H+ and Na( +)- Ca2+ exchange.
Direct measurements of the dissociation-rate constant for inhibitor-enzyme complexes via the T1 rho and T2 (CPMG) methods.
The unimolecular dissociation rate constant, k-1, for the inhibitor-enzyme complex tubercidin-Escherichia coli purine nucleoside phosphorylase (PNPase) has been determined directly via two related 1H
Dissociation constants for dihydrofolic acid and dihydrobiopterin and implications for mechanistic models for dihydrofolate reductase.
The redetermined value for the pKa of N5 of H2folate has implications for mechanistic models for dihydrofolate reductase, and revised kinetic constants have been calculated for one model.
Development of a self-emulsifying formulation that reduces the food effect for torcetrapib.
Self-emulsifying drug delivery system (SEDDS) formulations have been developed to reduce the food effect observed in early clinical trials using medium chain triglyceride (MCT) softgels and to increase the dose per capsule.
Synthesis and binding characteristics of N-(1-naphthyl)-N'-(3-[(125)I]-iodophenyl)-N'-methylguanidine ([(125)I]-CNS 1261): a potential SPECT agent for imaging NMDA receptor activation.
Radiolabeled CNS 1261 appears to be a good candidate for further development as a single photon emission computed tomography tracer in the investigation of NMDA receptor activation in cerebral ischemia.
Relaxation-matrix analysis of the transferred nuclear Overhauser effect for finite exchange rates
Abstract A matrix formalism is developed for calculations of time-dependent nuclear Overhauser effects in systems undergoing chemical exchange, and the analysis is applied to the interpretation of
Pharmaceutical solid-state kinetic stability investigation by using moisture-modified Arrhenius equation and JMP statistical software.
An accelerated stress approach utilizing the moisture-modified Arrhenius equation and JMP statistical software was utilized to quantitatively assess the solid state stability of an investigational
Ionic Alterations
The mechanism by which preconditioning (brief intermittent periods of ischemia and reflow) improves recovery of function and reduces enzyme release after a subsequent 30-minute period of ischemia was