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Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444.
Biotransformation of Prasugrel, a Novel Thienopyridine Antiplatelet Agent, to the Pharmacologically Active Metabolite
One possible mechanism for the ultimate formation of R-138727 in vitro can be through formation of a sulfenic acid mediated by P450s followed possibly by a glutathione conjugation to a mixed disulfide and reduction of the disulfides to the active metabolite R- 138727.
Discovery of DS79182026: A potent orally active hepcidin production inhibitor.
[2-(omega-phenylalkyl)phenoxy]alkylamines.II: Synthesis and selective serotonin-2 receptor binding.
(S)-2-[2- [2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]-1-methylpyrrolidine, (S)-27, exhibited the most potent and selective affinity for 5-HT2 receptors and was effective in inhibiting 5- HT2-induced vasoconstriction in vitro and platelet aggregation both in vivo and ex vivo.
Discovery of DS42450411 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4-aminopyrimidine derivatives.
Cinnamylindoline derivatives: synthesis and factor Xa (FXa) inhibitory activities.
- Tetsuji Noguchi, N. Tanaka, K. Fujimoto
- Chemistry, BiologyChemical & pharmaceutical bulletin
- 1 October 2007
Some novel derivatives of cinnamylindoline derivatives showed potent FXa inhibitory activities and good selectivity over trypsin and exhibited potent anticoagulant activities in vitro.
Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives.
Effects of R-102444, an orally active 5-HT2A receptor antagonist, in rat models of peripheral vascular disease.
Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: Additional evidence for possible involvement of 5-HT2A…
[2-(O-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding (2).
A series of 12-(2-phenylethyl)phenoxy]ethylpyrrolidine derivatives were synthesized, and their affinity for serotonin-2 (5-HT2) and dopamine-2 (D2) receptors was examined. Among them, compound 17,…