Involvement of the first transmembrane segment of human alpha(2)-adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine



: Laurila JMM, Wissel G, Xhaard H, Ruuskanen JO, Johnson MS, Scheinin M

Publisher: WILEY-BLACKWELL

: 2011

: British Journal of Pharmacology

: BRITISH JOURNAL OF PHARMACOLOGY

: BRIT J PHARMACOL

: 5

: 164

: 5

: 1558

: 1572

: 15

: 0007-1188

DOI: https://doi.org/10.1111/j.1476-5381.2011.01520.x


TM1 is involved in determining the low affinity of some antagonist ligands at the human alpha(2A)-adrenoceptor. The exact mechanism is not known, but the position of TM1 at a large distance from the binding pocket indicates that TM1 does not participate in specific side-chain interactions with amino acids within the binding pocket of the receptor or with ligands bound therein. Instead, molecular models suggest that TM1 has indirect conformational effects related to the charge distribution or overall shape of the binding pocket.



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