caa a22 4500 469079096 CHVBK 20180323132944.0 cr unu---uuuuu 170328e19920601xx s 000 0 eng 10.1007/BF00164585 doi (NATIONALLICENCE)springer-10.1007/BF00164585 Metitepine distinguishes two receptors mediating inhibition of [3H]-5-hydroxytryptamine release in guinea pig hippocampus [Elektronische Daten] [Lynn Wilkinson, Derek Middlemiss] Summary: Inhibition of [3H]-5-hydroxytryptamine ([3H]-5-HT) release from guinea pig brain slices via activation of the terminal 5-HT autoreceptor has previously been characterised as a model of 5-HT1D receptor activation, based on the rank potencies of a range of agonists, and the potent antagonism of the inhibitory effects of 5-HT by metitepine. The present study uses this model, in slices of the guinea pig hippocampus, to examine the antagonist potency of metitepine against the 5-HT receptor agonists sumatriptan, 5-carboxamidotryptamine (5-CT) and 5-HT Addition of metitepine to the perfusion buffer (30, 300 and 1000 nmol/l) significantly shifted the concentration-response curve to 5-HT, producing a Schild slope of 1.1, and a pA2 value of 7.6. However, the ability of metitepine to antagonise the effects of sumatriptan or 5-CT in this model was less marked. A clear-cut shift in the concentration-response curve to sumatriptan was only achieved at1000 nmol/l metitepine (apparent pA2 = 6.7),and this was similar to the ability of metitepine to attenuate the effects of 5-CT (apparent pA2 7.0 at 300 nmol/l and 6.7 at 1000 nmol/l). These findings suggest heterogeneity in the receptor mediating inhibition of [3H]-5-HT release in guinea pig hippocampus. Springer-Verlag, 1992 Serotonin nationallicence 5-HT1D-receptor nationallicence Autoreceptor nationallicence Guinea pig nationallicence Hippocampus nationallicence Wilkinson Lynn Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, CM20 2QR, Harlow, Essex, UK aut Middlemiss Derek Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, CM20 2QR, Harlow, Essex, UK aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/6(1992-06-01), 696-699 0028-1298 345:6<696 1992 345 210 https://doi.org/10.1007/BF00164585 text/html Onlinezugriff via DOI 1 brief-communication jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00164585 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Wilkinson Lynn Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, CM20 2QR, Harlow, Essex, UK aut NATIONALLICENCE 700 1- Middlemiss Derek Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, CM20 2QR, Harlow, Essex, UK aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/6(1992-06-01), 696-699 0028-1298 345:6<696 1992 345 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer