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Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Oct 01; Vol. 16 (19), pp. 5018-21. Date of Electronic Publication: 2006 Aug 14. - Publication Year :
- 2006
-
Abstract
- A series of des-keto lobeline analogs has been synthesized and evaluated for their ability to inhibit the dopamine transporter (DAT) and serotonin transporter (SERT) function and for their affinity for the synaptic vesicle monoamine transporter (VMAT2), as well as for alpha4beta2( *) and alpha7( *) neuronal nicotinic acetylcholine receptors (nAChRs). The enantiomers 8R-hydroxylobel-9-ene (3a) and 10S-hydroxylobel-7-ene (3c) exhibited high potency and selectivity at SERT and DAT, respectively.
- Subjects :
- Humans
Lobeline chemical synthesis
Lobeline pharmacology
Protein Binding
Receptors, Nicotinic metabolism
Serotonin Antagonists chemistry
Serotonin Antagonists pharmacology
Stereoisomerism
Structure-Activity Relationship
Vesicular Monoamine Transport Proteins metabolism
alpha7 Nicotinic Acetylcholine Receptor
Dopamine Plasma Membrane Transport Proteins antagonists & inhibitors
Lobeline analogs & derivatives
Serotonin Antagonists chemical synthesis
Serotonin Plasma Membrane Transport Proteins drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16905316
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.07.070