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Bioorg Med Chem Lett ; 22(7): 2560-4, 2012 Apr 01.
Article in English | MEDLINE | ID: mdl-22381048

ABSTRACT

A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT(2C) receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.


Subject(s)
Appetite Depressants/chemical synthesis , Piperidines/chemical synthesis , Pyridines/chemical synthesis , Receptor, Serotonin, 5-HT2C/metabolism , Serotonin 5-HT2 Receptor Agonists/chemical synthesis , Animals , Appetite Depressants/pharmacology , Calcium/metabolism , Ergolines/pharmacology , Humans , Kinetics , Piperidines/pharmacology , Protein Binding , Pyridines/pharmacology , Radioligand Assay , Receptor, Serotonin, 5-HT2C/chemistry , Serotonin 5-HT2 Receptor Agonists/pharmacology , Serotonin Antagonists/pharmacology , Stereoisomerism , Structure-Activity Relationship
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