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Start Over Author "HIGAKI, Masahide" Topic molecular mimicry

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1. Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.

Author

Hattori K, Tanaka A, Okitsu O, Tabuchi S, Taniguchi K, Nishio M, Koyama S, Higaki M, Seki J, and Sakane K

Subjects
Administration, Oral, Animals, Carbamates pharmacokinetics, Chlorocebus aethiops, Dogs, Humans, Proto-Oncogene Proteins c-met blood, Rats, Receptors, Epoprostenol, Recombinant Proteins agonists, Structure-Activity Relationship, Substrate Specificity, Carbamates chemistry, Carbamates pharmacology, Epoprostenol metabolism, Molecular Mimicry, Platelet Aggregation drug effects, Receptors, Prostaglandin agonists
Abstract

The new classes of diphenylcarbamate derivatives with a tetrahydronaphthalene skeleton as highly potent and selective IP agonists have been discovered. The optimized diphenylcarbamate type compound FK-788: (R)-4 exhibited potent antiaggregative potency with an IC50 of 18 nM and high binding affinity for the human recombinant IP receptor with K(i) values of 20 nM and selectivity for human IP over all other members of the human prostanoid receptor family. Compound (R)-4 was shown to exhibit good pharmacokinetic properties in rats and dogs, and also good bioavailability in healthy volunteers.

Published
2005
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