Minimal structural requirements of alkyl γ-lactones capable of antagonizing the cocaine-induced motility decrease in planarians.
Submitted by Oné R Pagán on
Title | Minimal structural requirements of alkyl γ-lactones capable of antagonizing the cocaine-induced motility decrease in planarians. |
Publication Type | Journal Article |
Year of Publication | 2011 |
Authors | Baker, D, Deats, S, Boor, P, Pruitt, J, Pagán, OR |
Journal | Pharmacol Biochem Behav |
Volume | 100 |
Issue | 1 |
Pagination | 174-9 |
Date Published | 2011 Nov |
ISSN | 1873-5177 |
Keywords | Animals, Cocaine, Lactones, Motor Activity, Planarians, Structure-Activity Relationship |
Abstract | We recently reported that the natural cyclic lactone, parthenolide, and related analogs prevent the expression of behavioral effects induced by cocaine in planarians and that parthenolide's γ-lactone ring is required for this effect. In the present work, we tested a series of alkyl γ-lactones with varying chain length (1-8 carbons) to determine their ability to antagonize the planarian motility decrease induced by 200 μM cocaine. Alkyl lactones with up to a 4-carbon alkyl chain did not affect planarian motility or antagonized the cocaine-induced motility decrease; only the compound γ-nonalactone (a γ-lactone with a 5-carbon chain) was able to prevent the cocaine-induced behavioral patterns, while alkyl lactones with longer carbon chains failed to prevent the cocaine-induced effects. Thus, we conclude that the optimal structural features of this family of compounds to antagonize cocaine's effect in this experimental system is a γ-lactone ring with at a 5-carbon long functional group. |
DOI | 10.1016/j.pbb.2011.08.013 |
Alternate Journal | Pharmacol. Biochem. Behav. |
PubMed ID | 21878350 |
PubMed Central ID | PMC3183103 |
Grant List | R03 DA026518-01 / DA / NIDA NIH HHS / United States R03DA026518 / DA / NIDA NIH HHS / United States |