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 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.
Pauwels
P J
PJ
Laboratory of Cellular and Molecular Neurobiology, Centre de Recherche Pierre Fabre, Castres, France.
Colpaert
F C
FC
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000096:biosynthesis*; D006801:Humans; D009457:Neuroglia / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism; D018170:Sumatriptan / Q000378:metabolism* / Q000494:pharmacology; D014162:Transfection
D011985:Receptors, Serotonin; D005576:Colforsin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D018170:Sumatriptan; D000242:Cyclic AMP