A1 Refereed original research article in a scientific journal
Involvement of the first transmembrane segment of human alpha(2)-adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine
Authors: Laurila JMM, Wissel G, Xhaard H, Ruuskanen JO, Johnson MS, Scheinin M
Publisher: WILEY-BLACKWELL
Publication year: 2011
Journal: British Journal of Pharmacology
Journal name in source: BRITISH JOURNAL OF PHARMACOLOGY
Journal acronym: BRIT J PHARMACOL
Number in series: 5
Volume: 164
Issue: 5
First page : 1558
Last page: 1572
Number of pages: 15
ISSN: 0007-1188
DOI: https://doi.org/10.1111/j.1476-5381.2011.01520.x
Abstract
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.
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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