Lobelane analogues as novel ligands for the vesicular monoamine transporter-2.
A series of lobelane analogues has been synthesized and their structure-activity relationships at the vesicular monoamine transporter-2 (VMAT2) have been evaluated. The most potent analogues in this series were the cis-2,6-piperidino analogues, 25b, 27b, 28b, and 30b, with K(i) values ranging from 430 to 580 nM.
Zheng
Guangrong
G
College of Pharmacy, University of Kentucky, Rose Street, Lexington, KY 40536-0082, USA.
Dwoskin
Linda P
LP
Deaciuc
Agripina G
AG
Zhu
Jun
J
Jones
Marlon D
MD
Crooks
Peter A
PA
D000818:Animals; D001923:Brain Chemistry; D005731:Ganglionic Stimulants / Q000138:chemical synthesis*; D008024:Ligands; D008120:Lobeline / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D008562:Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors*; D008694:Methamphetamine; D018733:Nicotinic Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects; D013329:Structure-Activity Relationship; D019966:Substance-Related Disorders / Q000188:drug therapy; D013570:Synaptic Membranes / Q000737:chemistry; D050492:Vesicular Biogenic Amine Transport Proteins; D050493:Vesicular Monoamine Transport Proteins
D005731:Ganglionic Stimulants; D008024:Ligands; D008562:Membrane Glycoproteins; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D018733:Nicotinic Antagonists; D011978:Receptors, Nicotinic; C493454:Slc18a2 protein, rat; D050492:Vesicular Biogenic Amine Transport Proteins; D050493:Vesicular Monoamine Transport Proteins; D008694:Methamphetamine; D008120:Lobeline