125341-29-9Relevant academic research and scientific papers
Development of High-affinity 5-HT3 Receptor Antagonists. 2. Two Novel Tricyclic Benzamides
Youssefyeh, R. D.,Campbell, H. F.,Airey, J. E.,Klein, S.,Schnapper, M.,et al.
, p. 903 - 911 (2007/10/02)
Two new classes of potent 5-HT3 agents have been developed and examined as inhibitors of cytotoxic drug induced emesis in the ferret and dog.The absolute configuration of the most active molecules 10 and 18 have been determined by X-ray crystal
Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides
Youssefyeh,Campbell,Klein,Airey,Darkes,Powers,Schnapper,Neuenschwander,Fitzpatrick,Pendley,Martin
, p. 895 - 903 (2007/10/02)
This report describes the development of novel benzamides which are orally active, highly potent, specific antagonists of 5-HT3 receptors. Described in this first report are the structure-activity relationships that led to novel structures with improved potency and selectivity. From this series of compounds, (S)-28 was identified and selected for further evaluation as a 5- HT3 receptor antagonist. Compared with 5-HT3 antagonists such as GR 38032F, BRL 43694, and metoclopramide, (S)-28 was most active in (a) inhibiting binding to 5-HT3 receptor binding sites in rat entorhinal cortex with an K(i) value of 0.19 nM and (b) blocking cisplatin-induced emesis in the ferret with an ED50 value determined to be 9 μg/kg po.
