Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.
A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at alpha4beta2* and alpha7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.
Zheng
Guangrong
G
College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.
Dwoskin
Linda P
LP
Deaciuc
Agripina G
AG
Crooks
Peter A
PA
D000818:Animals; D008024:Ligands; D011485:Protein Binding; D051381:Rats; D011978:Receptors, Nicotinic / Q000378:metabolism; D013329:Structure-Activity Relationship; D014326:Tropanes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
D008024:Ligands; D011978:Receptors, Nicotinic; D014326:Tropanes