Ligand interaction with the purified serotonin transporter in solution and at the air/water interface

FEBS Letters

Launay, J.M.⁴  Morimoto, H.³  Airaksinen, M.M.⁵  Manivet, P.⁴  Baszkin, A.¹  Rosilio, V.¹  Faivre, V.¹  Callaway, J.C.² 

[1] Laboratoire de Physico-Chimie des Surfaces, UMR CNRS 8612, 5 rue J-B. Clément, 92296 Châtenay-Malabry, France;Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 6, 70211 Kuopio, Finland;National Tritium Labelling Facility (NTLF), University of California, 1 Cyclotron Road, Berkeley, CA 94720, USA;C.R.C. Bernard ‘Pathologie Expérimentale et Communications Cellulaires’, Service de Biochimie, IFR 6, Hôpital Lariboisière AP-HP, 2 rue Ambroise Paré, 75010 Paris, France;Department of Pharmacology and Toxicology, University of Kuopio, P.O. Box 6, 70211 Kuopio, Finland

关键词: Serotonin;    Transporter;    Surface pressure;    Protein monolayer;    Serotonin transporter–drug interaction;    5-HT;    5-hydroxytryptamine (serotonin);    SERT;    serotonin transporter;    RTI (cocaine congener);    3β-(4-iodophenylpropene-2β-carboxylic acid methyl ester);    MDMA;    3;    4-methylene dioxymethamphetamine (ecstasy);   

DOI  :  10.1016/S0014-5793(00)01362-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The purified serotonin transporter (SERT) was spread at the air/water interface and the effects both of its surface density and of the temperature on its interfacial behavior were studied. The recorded isotherms evidenced the existence of a stable monolayer undergoing a lengthy rearrangement. SERT/ligand interactions appeared to be dependent on the nature of the studied molecules. Whereas an unrelated drug (chlorcyclizine) did not bind to the spread SERT, it interacted with its specific ligands. Compared to heterocyclic drugs, for which binding appeared to be concentration-dependent, a ‘two-site’ mechanism was evidenced for pinoline and imipramine.

【 授权许可】

Unknown