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Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels
TLDR
The novel fluoro-oxindoles BMS-204352 and racemic compound 1 are potent, effective and uniquely Ca++-sensitive openers of maxi-K channels, thereby augmenting an endogenous mechanism for regulating Ca++ entry and membrane potential.
Pharmacokinetics and pharmacodynamics of labetalol in the pregnant sheep.
TLDR
Whereas there were no significant maternal or fetal cardiovascular effects, some very significant metabolic effects were observed, including fetal and maternal lactic acidosis and hyperglycemia, and the exact mechanism by which labetalol causes these metabolic effects is not clear.
Involvement of cytochrome P‐450 isozymes in melatonin metabolism and clinical implications
TLDR
Melatonin was incubated with 0-lymphoblastoid cell lines that have been engineered to stably express cDNAs for specific CYP P450 isozymes to gain a preliminary understanding of the specific human cytochrome P-450 iszymes responsible for metabolism of melatonin, evaluate the inhibitory potential ofmelatonin, and predict possible drug interactions.
Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist.
TLDR
In vitro metabolism of BMS-214778 was mostly by hydroxylation and dehydrogenation, with CYP1A1, 1A2, 2D6, and 2C9 being the most likely isoforms to be involved in its metabolism in humans.
Selective Inhibition of Eosinophil Influx into the Lung by Small Molecule CC Chemokine Receptor 3 Antagonists in Mouse Models of Allergic Inflammation
TLDR
It is concluded that small molecule CCR3 antagonists reduce pulmonary eosinophilic inflammation elicited by chemokine or allergenic challenge.
THE CHIMPANZEE (PAN TROGLODYTES) AS A PHARMACOKINETIC MODEL FOR SELECTION OF DRUG CANDIDATES: MODEL CHARACTERIZATION AND APPLICATION
TLDR
The chimpanzee serves as a valuable surrogate model for human pharmacokinetics, especially when species differences in P450 enzyme activity are considered, as well as an acceptable range for biological variability.
Disposition, metabolism, and pharmacodynamics of labetalol in adult sheep.
TLDR
The contribution of skeletal muscles in the development of metabolic acidosis induced by labetalol is investigated and the involvement of active metabolite(s) using conscious, chronically instrumented adult nonpregnant ewes is exploredUsing GC-mass selective detection, the presence of 3-amino-1-phenylbutane, a close congener of amphetamine, in urine and bile samples was established.
Pharmacokinetics and oral bioavailability of exogenous melatonin in preclinical animal models and clinical implications
TLDR
Pharmacokinetics and oral bioavailability of exogenous melatonin in preclinical animal models andclinical implications and clinical implications are studied.
The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.
3-Aryl-3-fluorooxindoles can be efficiently synthesized in two steps by the addition of an aryl Grignard to an isatin, followed by treatment with DAST. Oxindole 1 (BMS-204352; MaxiPost) can be
Sensitive microbore high-performance liquid chromatographic assay for labetatol in the fluids of pregnant sheep
A rapid and sensitive microbore high-performance liquid chromatographic (HPLC) assay is reported for the quantitation of labetalol, an anti-hypertensive agent, in small volumes (250 microliters) of
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