(R)- and (S)-8-acetyl-2-(dipropylamino)tetralin (LY-41): two novel 5-HT1A receptor agonists |
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| Affiliation: | 1. Health and Biomedical Innovation, Clinical and Health Sciences, University of South Australia, Adelaide, SA, Australia;1. Department of Economics, University of Foggia, Largo Papa Giovanni Paolo II, 1, 71121 Foggia, Italy;2. Department of Quality and Operations Management, Faculty of Engineering and the Built Environment, University of Johannesburg, APB Campus, P. O. Box 524, Auckland Park 2006 Johannesburg, South Africa;3. Department of Agricultural and Environmental Sciences, Production, Landscape, Agroenergy, University of Milan, Via G. Celoria 2, 20133 Milan, Italy;4. University of Campinas, Faculty of Food Engineering, Department of Food Science, Campinas, São Paulo, Brazil;5. Department of Industrial Engineering, University of Catania, Viale A. Doria 6, 95125 Catania, Italy |
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| Abstract: | Interactions between central 5-HT1A receptors and the enantiomers of LY-41, a 2-aminotetralin derivative related to 8-OH-DPAT (8-hydroxy-2-(dipropylamino)tetralin), were studied. Both enantiomers of LY-41 behaved as potent 5-HT1A receptor agonists in rats, inducing the 5-HT behavioural syndrome, decreasing body temperature and inhibiting the cage-leaving response. The behavioural syndrome and the hypothermia were antagonized by the 5-HT1A receptor antagonist, (S)-UH-301. The LY-41 enantiomers also reduced brain 5-HTP accumulation in rats treated with a decarboxylase inhibitor. The pharmacology of the enantiomers of LY-41 appeared similar to that of 8-OH-DPAT. However, it is noteworthy that the stereoselective interaction of 5-HT1A receptors with LY-41 was opposite to that of 8-OH-DPAT. Thus, (R)-8-OH-DPAT was more potent than (S)-8-OH-DPAT, whereas (S)-LY-41 appeared to be more potent than (R)-LY-41. |
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