PMID: 8474615Mar 1, 1993Paper

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

Neuropharmacology
L O WilkinsonD N Middlemiss

Abstract

The present studies examined the relative antagonist potencies of the optical isomers of the 5-HT receptor antagonist metitepine at the 5-HT1D binding site labelled by the novel radioligand serotonin-O-carboxymethylglycyl [125]iodotyrosinamide ([125I]GTI), and at the terminal 5-HT autoreceptor in guinea pig frontal cortex, a proposed model of 5-HT1D receptor activation. The pharmacological specificity of the [125I]GTI binding site in guinea pig frontal cortex was similar to previously published studies in the bovine cortical 5-HT1D recognition site labelled with [3H]5-HT. The (+) isomer of metitepine displaced [125I]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 pA2 of the (-) isomer was 8.0 (sumatriptan) and 7.7 (5-HT) while the apparent pA2 of the (+) isomer was 7.1 (sumatriptan) and 6.8 (5-HT). The (-) isomer was more effective than the (+) isomer at enhancing stimulated [3H]5-HT release. These findings support the identification of the guinea pig 5-HT terminal auto...Continue Reading

References

Jun 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·L O Wilkinson, D N Middlemiss
Jan 1, 1991·Journal of Receptor Research·D Hoyer, P Schoeffter
Apr 1, 1989·Trends in Pharmacological Sciences·D Hoyer, D N Middlemiss
Jan 14, 1986·European Journal of Pharmacology·D N Middlemiss
Jul 7, 1988·European Journal of Pharmacology·R BouhelalJ Bockaert
Jun 1, 1988·Naunyn-Schmiedeberg's Archives of Pharmacology·P SchoeffterD Hoyer
Apr 7, 1987·European Journal of Pharmacology·R F NealeM Williams

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Citations

Nov 1, 1993·British Journal of Pharmacology·M S BeerD N Middlemiss
Oct 1, 1996·Alcoholism, Clinical and Experimental Research·Y WangJ Y Wang
Dec 5, 2000·Alcoholism, Clinical and Experimental Research·C H JengY Wang
Jan 24, 2006·Progress in Neuro-psychopharmacology & Biological Psychiatry·Mostafa El Mansari, Pierre Blier
Jul 4, 2009·Journal of the International Neuropsychological Society : JINS·Karen L SiedleckiClinton B Wright
Jul 29, 2009·Journal of the International Neuropsychological Society : JINS·R Scott Mackin, Patricia A Areán
Dec 21, 2011·Journal of the International Neuropsychological Society : JINS·Karen L SiedleckiClinton B Wright
Nov 30, 2018·Journal of the International Neuropsychological Society : JINS·Rebecca L KoscikSterling C Johnson
Jun 2, 2006·Journal of Abnormal Psychology·Rebecca L FullerJames M Gold
Jul 8, 2015·Journal of the International Neuropsychological Society : JINS·Adam GersteneckerKristen L Triebel
Sep 30, 2016·Archives of Clinical Neuropsychology : the Official Journal of the National Academy of Neuropsychologists·Herman BuschkeRichard B Lipton
Apr 25, 2007·Psychological Medicine·Mark A LauZindel V Segal
Aug 12, 2010·Multiple Sclerosis : Clinical and Laboratory Research·Francesca BagnatoHenry F McFarland

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