Abstract
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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Brain Chemistry
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Ganglionic Stimulants / chemical synthesis*
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Ligands
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Lobeline / analogs & derivatives*
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Lobeline / chemical synthesis
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Membrane Glycoproteins / antagonists & inhibitors*
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Membrane Transport Modulators*
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Membrane Transport Proteins / antagonists & inhibitors*
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Methamphetamine
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Nicotinic Antagonists / chemical synthesis
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Nicotinic Antagonists / pharmacology
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Rats
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Receptors, Nicotinic / drug effects
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Structure-Activity Relationship
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Substance-Related Disorders / drug therapy
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Synaptic Membranes / chemistry
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Vesicular Biogenic Amine Transport Proteins
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Vesicular Monoamine Transport Proteins
Substances
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Ganglionic Stimulants
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Ligands
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Membrane Glycoproteins
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Membrane Transport Modulators
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Membrane Transport Proteins
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Nicotinic Antagonists
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Receptors, Nicotinic
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Slc18a2 protein, rat
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Vesicular Biogenic Amine Transport Proteins
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Vesicular Monoamine Transport Proteins
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Methamphetamine
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Lobeline