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Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands |
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| Authors: | Banister Samuel D Moussa Iman A Beinat Corinne Reynolds Aaron J Schiavini Paolo Jorgensen William T Kassiou Michael |
| Institution: | a School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia b Brain and Mind Research Institute, Sydney, NSW 2050, Australia c Discipline of Medical Radiation Sciences, The University of Sydney, Sydney, NSW 2006, Australia |
| Abstract: | In our continued exploration of trishomocubane derivatives with central nervous system (CNS) activity, N-arylalkyl-8-aminopentacyclo5.4.0.02,6.03,10.05,9]undecanes (10-13) displaying affinity for the sigma (σ) receptor were also found, in several cases, to interact with the dopamine transporter (DAT). Compound 12 was identified as the first trishomocubane-derived high affinity DAT ligand (Ki = 1.2 nM), with greater than 8300-fold selectivity over the monoamine transporters NET and SERT, and only low to moderate affinity for σ1 and σ2 receptors. |
| Keywords: | Trishomocubanes Monoamine transporters Sigma receptors CNS Structure-activity relationships |
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