Abstract
Zoniporide (CP-597,396) is a potent and selective inhibitor of NHE-1, which exhibits high aqueous solubility and acceptable pharmacokinetics for intravenous administration. The discovery, synthesis, activities, and rat and dog pharmacokinetics of this compound are presented. The potency and selectivity of zoniporide may be due to the conformation that the molecule adopts due to the presence of a cyclopropyl and a 5-quinolinyl substituent on the central pyrazole ring of the molecule.
MeSH terms
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Animals
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Dogs
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Guanidines / chemistry
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Guanidines / pharmacokinetics
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Guanidines / pharmacology*
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Injections, Intravenous
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Molecular Conformation
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Protective Agents / pharmacokinetics
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Protective Agents / pharmacology
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Pyrazoles / chemistry
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Pyrazoles / pharmacokinetics
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Pyrazoles / pharmacology*
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Rats
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Sodium-Hydrogen Exchangers / antagonists & inhibitors*
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Sodium-Hydrogen Exchangers / metabolism
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Solubility
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Water / chemistry
Substances
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Guanidines
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Protective Agents
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Pyrazoles
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Slc9a2 protein, rat
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Sodium-Hydrogen Exchangers
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growth factor-activatable Na-H exchanger NHE-1
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Water
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zoniporide