Details

Autor(en) / Beteiligte

• Sarker, Subhodeep
• Weissensteiner, René
• Steiner, Ilka
• Sitte, Harald H
• Ecker, Gerhard F
• Freissmuth, Michael
• Sucic, Sonja

Titel

The high-affinity binding site for tricyclic antidepressants resides in the outer vestibule of the serotonin transporter

Ist Teil von

• BMC pharmacology, 2010-11, Vol.10 (S1), p.A21-A21, Article A21

Ort / Verlag

London: BioMed Central

Erscheinungsjahr

2010

Quelle

EZB Free E-Journals

Beschreibungen/Notizen

• Conclusions These observations are consistent with a model, where (i) the tricyclic ring is docked into the outer vestibule and the dimethyl-aminopropyl side chain points to the substrate binding site, (ii) binding of amphetamines creates a structural change in the inner and outer vestibule that precludes docking of the tricyclic ring, (iii) simultaneous binding of ibogaine (which binds to the inward-facing conformation) and of carbamazepine is indicative of a second binding site in the inner vestibule, consistent with the pseudo-symmetric fold of monoamine transporters.