caa a22 4500 469078103 CHVBK 20180323132941.0 cr unu---uuuuu 170328e19920901xx s 000 0 eng 10.1007/BF00173536 doi (NATIONALLICENCE)springer-10.1007/BF00173536 "5-HT1R” or 5-HT1D sites? Evidence for 5-HT 1D binding sites in rabbit brain [Elektronische Daten] [Daniel Hoyer, Hugues Lery, Christian Waeber, Anne Bruinvels, Joachim Nozulak, Jose Palacios] Summary: Radioligand binding studies were performed in membranes of rabbit whole brain and striatum using the novel iodinated radioligand for 5-hydroxytryptamine 5-HT1B and 5-HT1D sites, Serotonin-5-O-Carboxymethyl-Glycyl[125I]Tyrosinamide ([125I]GTI). [125I]GTI labelled a finite number of high affinity sites in rabbit brain membranes, Bmax = 191 +- 47 fmol/mg protein, pKD (-log mol/1) = 8.50 +- 0.13, n = 5. The pharmacological profile of [152I]GTI binding was fully comparable to that reported previously in human and other brain preparations known to possess 5-HT1D sites (using either [3H]5-HT or [125I]GTI) and displayed a characteristic rank order of affinity: 5-carboxamidotryptamine > 5-HT = dihydroergotamine _> ergotamine ≥_ sumatriptan >_ CGS 12066 >- metergoline > yohimbine >_ methysergide > ICYP > 8-OH-DPAT >_ CP 93129 > (-)pindolol > ketanserin > isamoltane > mesulergine > corynanthine > buspirone > MDL 72222. Autoradiographic studies were performed on rabbit brain slices using [3H]5-HT in the presence of 100 nmol/1 8-OH-DPAT and mesulergine (in order to mask 5-HT1A and 5-HT1c binding sites) and [125I]CYP (iodocyanopindolol) in the presence of β µmol/I isoprenaline and 100 nmol/l 8-OH-DPAT (in order to mask β adrenoceptor and 5-HT1A binding sites). There was no detectable specific binding of [125I]CYP through the brain, thus excluding the presence of 5-HT1B sites in rabbit brain. By contrast, [3H]5-HT labelled a high density of sites in globus pallidus, substantia nigra and superior colliculus. Other regions displaying labelling include the striatum, the dentate gyrus of the hippocampus and the periaqueductal grey matter. This pattern of distribution is compatible with that reported for 5-HT1D sites in other species. The present data strongly suggest that rabbit brain has recognition sites with the pharmacological profile and distribution characteristic of the 5-HT1D recognition site. These findings are in agreement with results obtained by Limberger et al. (1991), suggesting the terminal 5-HT autoreceptor of the rabbit brain to belong to the 5-HT1D subtype. Except for limited species variations (see Bruinvels et al. 1992), the pharmacology of these sites does not justify an addition to the existing nomenclature ("5-HT1R”), in contrast to what has been proposed by Xiong and Nelson (1989). The rabbit represents another laboratory species in which 5-HT1D receptor mediated effects could be studied. Springer-Verlag, 1992 5-HT1D nationallicence "5-HT1R” receptors nationallicence Rabbit brain nationallicence Hoyer Daniel Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Lery Hugues Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Waeber Christian Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Bruinvels Anne Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Nozulak Joachim Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Palacios Jose Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/3(1992-09-01), 249-254 0028-1298 346:3<249 1992 346 210 https://doi.org/10.1007/BF00173536 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00173536 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Hoyer Daniel Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Lery Hugues Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Waeber Christian Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Bruinvels Anne Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Nozulak Joachim Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 700 1- Palacios Jose Preclinical Research, 360/604, Sandoz Pharma Ltd, CH-4002, Basel, Switzerland aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/3(1992-09-01), 249-254 0028-1298 346:3<249 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer