| Literature DB >> 16821786 |
Thomas H McLean1, James J Chambers, Jason C Parrish, Michael R Braden, Danuta Marona-Lewicka, Deborah Kurrasch-Orbaugh, David E Nichols.
Abstract
A conformationally restricted analogue of mescaline, C-(4,5,6-trimethoxyindan-1-yl)-methanamine, was designed using a 5-HT(2A) receptor homology model. The compound possessed 3-fold higher affinity and potency than and efficacy equal to that of mescaline at the 5-HT(2A) receptor. The new analogue substituted fully for LSD in drug discrimination studies and was 5-fold more potent than mescaline. Resolution of this analogue into its enantiomers corroborated the docking experiments, showing the R-(+) isomer to have higher affinity and potency and to have efficacy similar to that of mescaline at the 5-HT(2A) receptor.Entities:
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Year: 2006 PMID： 16821786 DOI： 10.1021/jm060272y
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446