Stereoselectivity of 8-OH-DPAT enantiomers at cloned human 5-HT1D receptor sites

The cAMP responses of (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and its enantiomers were measured at cloned human 5-HT1D alpha and 5-HT1D beta receptors in transfected C6-glial cells. R(+)-8-OH-DPAT demonstrated potent intrinsic activity (EC50 value: 30 nM) at 5-HT1D alpha receptor si...

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Bibliographic Details
Published in:European journal of pharmacology 1996-04, Vol.300 (1-2), p.137-140
Main Authors: PAUWELS, P. J, COLPAERT, F. C
Format: Article
Language:English
Subjects:
8-Hydroxy-2-(di-n-propylamino)tetralin - chemistry
8-Hydroxy-2-(di-n-propylamino)tetralin - metabolism
8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology
Animals
Biological and medical sciences
Cell Line
Colforsin - pharmacology
Cyclic AMP - biosynthesis
Humans
Medical sciences
Neuroglia - drug effects
Neuroglia - metabolism
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Rats
Receptors, Serotonin - drug effects
Receptors, Serotonin - metabolism
Serotoninergic system
Stereoisomerism
Sumatriptan - metabolism
Sumatriptan - pharmacology
Transfection
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Summary:The cAMP responses of (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and its enantiomers were measured at cloned human 5-HT1D alpha and 5-HT1D beta receptors in transfected C6-glial cells. R(+)-8-OH-DPAT demonstrated potent intrinsic activity (EC50 value: 30 nM) at 5-HT1D alpha receptor sites, its maximal effect being comparable to that of sumatriptan. Racemic 8-OH-DPAT and S(-)-8-OH-DPAT showed similar agonist efficacy but were respectively 2 and 75 times less potent than R(+)-8-)OH-DPAT. This differs from the lack of stereoselectivity of the 8-OH-DPAT enantiomers for 5-HT1A receptors.
ISSN:0014-2999
1879-0712
DOI:10.1016/0014-2999(95)00876-4