Regular paperDelineation of rat kidney α2A- and α2B-adrenoeeptors with [3H]RX821002 radiollgand binding: computer modelling reveals that guanfacine is an α2A-selective compound
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2011, Pharmacology Biochemistry and BehaviorStructural determinants of the alpha2 adrenoceptor subtype selectivity
2011, Journal of Molecular Graphics and ModellingCitation Excerpt :However, because of the common mechanisms for the signal transduction and the very high degree of sequence homology (more than 80%) exhibited by α2-ARs, information regarding subtype-selective compounds is still limited. At the time of this manuscript preparation, only a few compounds have been reported to be α2-ARs subtype-selective: the agonists guanfacine for α2a-AR and R-(+)-m-nitrobiphenylinde oxalate for α2c-AR and the antagonists BRL-44408 for α2a-AR, JP-1302 and OPC28326 for α2c-AR [13–19]. As a follow-up of our previous works [20,21], this paper combines structural bioinformatics approaches like homology modeling and docking to identify the main molecular characteristics which regulate the selectivity within the α2-ARs subtypes.