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Neuropharmacology v.32 no.3, 1993년, pp.205 - 208  

Stereoselective actions of the isomers of metitepine at 5-HT1D receptors in the guinea pig brain

Wilkinson, L.O. ; Hawkins, L.M. ; Beer, M.S. ; Hibert, M.F. ; Middlemiss, D.N. ;
  • 초록  

    The present studies examined the relative antagonist potencies of the optical isomers of the 5-HT receptor antagonist metitepine at the 5-HT 1D binding site labelled by the novel radioligand serotonin-O-carboxymethylglycyl [ 125 ]iodotyrosinamide ([ 125 I]GTI), and at the terminal 5-HT autoreceptor in guinea pig frontal cortex, a proposed model of 5-HT 1D receptor activation.The pharmacological specificity of the [ 125 I]GTI binding site in guinea pig frontal cortex was similar to previously published studies in the bovine cortical 5-HT 1D recognition site labelled with [ 3 H]5-HT. The (+) isomer of metitepine displaced [ 125 I]GTI binding with a lower affinity (64 nM) than did the (-) isomer (18 nM), which was equiactive with the racemic mixture. The (-) isomer of metitepine was more effective than the (+) isomer at attenuating the inhibitory effects of 5-HT and sumatriptan at the guinea pig terminal 5-HT autoreceptor; the apparent pA 2 of the (-) isomer was 8.0 (sumatriptan) and 7.7 (5-HT) while the apparent pA 2 of the (+) isomer was 7.1 (sumatriptan) and 6.8 (5-HT). The (-) isomer was more effective than the (+) isomer at enhancing stimulated [ 3 H]5-HT release. These findings support the identification of the guinea pig 5-HT terminal autoreceptor as a 5-HT 1D receptor and reinforce the species homology between the 5-HT 1B and 5-HT 1D receptors.


  • 주제어

    metitepine .   5-HT1D .   terminal autoreceptor .   guinea pig.  

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