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BMS-204352: a potassium channel opener developed for the treatment of stroke.

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During ischemic stroke, a fatal biochemical cascade that results in neuronal hyperexcitability is initiated when neurons at risk are exposed to excessive excitatory amino acids and pathologically high levels of intracellular calcium (Ca(2+)). Therefore, neuroprotectants including NMDA-antagonists

Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels.

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During ischemic stroke, neurons at risk are exposed to pathologically high levels of intracellular calcium (Ca++), initiating a fatal biochemical cascade. To protect these neurons, we have developed openers of large-conductance, Ca++-activated (maxi-K or BK) potassium channels, thereby augmenting an

BMS-204352 (Bristol Myers Squibb).

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BMS-204352 is a fluoro-oxindole potassium channel opener being developed by Bristol-Myers Squibb as a potential neuroprotectant for the treatment of acute ischemic stroke. Phase I trials were underway in Japan in 1998 [288541]. By July 1999, it was in phase II trials in the US [331682] and by

Acid-base catalysis of chiral Pd complexes: development of novel catalytic asymmetric reactions and their application to synthesis of drug candidates.

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Using the unique character of the chiral Pd complexes 1 and 2, highly efficient catalytic asymmetric reactions have been developed. In contrast to conventional Pd(0)-catalyzed reactions, these complexes function as an acid-base catalyst. Thus active methine and methylene compounds were activated to

Pharmacokinetic study of isocorynoxeine metabolites mediated by cytochrome P450 enzymes in rat and human liver microsomes.

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Isocorynoxeine (ICN) is one of the major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla (Miq.) Jacks. that is widely used for the treatment of hypertension, vascular dementia, and stroke. The present study was undertaken to assess the plasma pharmacokinetic characteristics

Rhynchophylline Protects Against the Amyloid β-Induced Increase of Spontaneous Discharges in the Hippocampal CA1 Region of Rats.

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Accumulated soluble amyloid β (Aβ)-induced aberrant neuronal network activity has been recognized as a key causative factor leading to cognitive deficits which are the most outstanding characteristic of Alzheimer's disease (AD). As an important structure associated with learning and memory, the

Effects of mobile phase composition and temperature on the supercritical fluid chromatography enantioseparation of chiral fluoro-oxoindole-type compounds with chlorinated polysaccharide stationary phases.

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The indole ring is present in many pharmaceutically active compounds, as in MaxiPost™ (or BMS-204352), an active pharmaceutical ingredient for post-stroke neuroprotection. Two different fluoro-oxindole-type chiral solutes derived from MaxiPost were prepared. The structural modification was placed on

Role of Plant Derived Alkaloids and Their Mechanism in Neurodegenerative Disorders.

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Neurodegenerative diseases are conventionally demarcated as disorders with selective loss of neurons. Conventional as well as newer molecules have been tested but they offer just symptomatic advantages along with abundant side effects. The discovery of more compelling molecules that can halt the

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