On the selectivity of 7-nitroindazole as an inhibitor of neuronal nitric oxide synthase

Article Abstract:

The ability of nitric oxide synthase (NOS) to inhibit various isoforms of NOS was examined. Assays classified biologic actions as neuronal NOS (nNOS)-mediated or endothelial NOS (eNOS)-dependent. On the basis of these assays, it was asserted that 7-nitroindazole (7-NI) does not exhibit eNOS-mediated cardiovascular effects in vivo. However, recent clinical studies have validated the active role of 7-NI in blood pressure regulation in rats. Further studies should be made to straighten out the in vivo selectivity of 7-NI for nNOS and eNOS.

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FLAP: a novel drug target for inhibiting the synthesis of leukotrienes

Article Abstract:

MK0886 is a potent drug derived from indole-3-alkanoic acid that suppresses the synthesis of leukotrienes. The drug exhibits strong affinity to 5-lipoxygenase-activating proteins (FLAP) which upon binding results in the inhibition of 5-lipoxygenase activation. This inhibition involves the translocation of 5-lipoxygenase to the cell membrane which disrupts the progress of cellular leukotriene synthesis.

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Phosphodiesterases: the journey towards therapeutics

Article Abstract:

Researchers discussed the therapeutic use of phosphodiesterase inhibitors at a conference in France in December, 1999. Most research focuses on the use of PDE4 inhibitors as anti-inflammatory agents and PDE5 inhibitors as a treatment for impotence. PDE4 inhibitors may also be beneficial in treating chronic obstructive lung disease.

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