Novel 5-Hydroxytryptamine (5-HT3) Receptor Antagonists. I. Synthesis and Structure-Activity Relationships of Conformationally Restricted Fused Imidazole Derivatives.
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چکیده
منابع مشابه
Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT3 Receptor Ligands
The 5-HT₃ receptor, a pentameric ligand-gated ion channel (pLGIC), is an important therapeutic target. During a recent fragment screen, 6-chloro-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine (1) was identified as a 5-HT₃ hit fragment. Here we describe the synthesis and structure-activity relationships (SAR) of a series of (iso)quinoline and quinazoline compounds that were synthesize...
متن کاملThe 5-hydroxytryptamine type 3 (5-HT3) receptor reveals a novel determinant of single-channel conductance.
5-HT3 (5-hydroxytryptamine type 3) receptors are cation-selective ion channels of the Cys-loop transmitter-gated ion channel superfamily. Two 5-HT3 receptor subunits, 5-HT3A and 5-HT3B, have been characterized in detail, although additional putative 5-HT3 subunit genes (HTR3C, HTR3D and HTR3E) have recently been reported. 5-HT3 receptors function as homopentameric assemblies of the 5-HT3 subuni...
متن کاملToward Biophysical Probes for the 5-HT3 Receptor: Structure−Activity Relationship Study of Granisetron Derivatives
This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluo...
متن کامل5-HT3 receptor antagonists for the treatment of nausea/vomiting.
It is well appreciated that a number of things (e.g., various insults, chemotherapeutic agents, radiation) may lead to the release of serotonin from the enterochromaffin of the gastrointestinal tract. Released serotonin may then bind to certain 5-HT3 receptors and promote nausea/vomiting. 5-HT3 receptor antagonists may ameliorate nausea/vomiting in a number of circumstances and have been utiliz...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1996
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.44.991