Article
The second extracellular loop of alpha2A-adrenoceptors contributes to the binding of yohimbine analogues.
British journal of pharmacology - 1 Aug 2007
Laurila J M M, Xhaard H, Ruuskanen J O, Rantanen M J M, Karlsson H K, Johnson M S, Scheinin M
Abstract excerpt
BACKGROUND AND PURPOSE: Rodent alpha(2A)-adrenoceptors bind the classical alpha(2)-antagonists yohimbine and rauwolscine with lower affinity than the human alpha(2A)-adrenoceptor. A serine-cysteine difference in the fifth transmembrane helix (TM; position 5.43) partially explains this, but all determinants of the interspecies binding selectivity are not known. Molecular models of alpha(2A)-adrenoceptors suggest...
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