caa a22 4500 469078197 CHVBK 20180323132941.0 cr unu---uuuuu 170328e19920901xx s 000 0 eng 10.1007/BF00173535 doi (NATIONALLICENCE)springer-10.1007/BF00173535 5-HT1D binding sites in various species: similar pharmacological profile in dog, monkey, calf, guinea-pig and human brain membranes [Elektronische Daten] [Anne Bruinvels, Hugues Lery, Joachim Nozulak, Jose Palacios, Daniel Hoyer] Summary: Radioligand binding studies were performed in membranes of calf caudate, guinea-pig cortex, dog caudate and whole brain, monkey caudate and whole brain, and human caudate using the novel iodinated radioligand, Serotonin-5-O-Carboxymethyl-Glycyl[125I] Tyrosinamide (abbreviated [125I]GTI for the sake of simplicity), a ligand known to label 5-HT 1B and 5-HT 1D sites. In all membrane preparations tested, [125I]GTI labelled high affinity sites with the following rank order of affinity: 5-carboxamidotryptamine > 5-HT = DHE = ergotamine >- sumatriptan >- metergoline = CGS 12066 >- yohimbine = methysergide >- methiothepin > 8-OHDPAT >_ mianserin >- CP 93129 >- (−)pindolol = ketanserin >_ isamoltane = mesulergine >- corynanthine = spiperone > MDL 72222. The affinity profiles were very similar in the membranes of the different species, especially in dog, monkey and human brain. The pharmacological profile of [1251]GTI binding (determined with up to 25 different drugs) was fully comparable to the binding profile reported previously in human substantia nigra (using [1251]GTI) or in a variety of brain preparations known to contain 5-HTID sites using [3H]5-HT as a radioligand. Although, the affinity profiles obtained in the various preparations displayed statistically highly significant correlations with slope values close to one, some drugs displayed slight species-related variations in affinity, as already reported in rabbit brain (see Xiong and Nelson 1989; Hoyer et al. 1992, accompanying report). The present report 1) establishes for the first time the pharmacological profile of 5-HT1D sites in dog and monkey brain, 2) shows that the pharmacological characteristics of these sites is indeed very similar in the brain of a variety of species including man, and 3) demonstrates the advantageous features of [1251]GTI as an iodinated 5-HT1D radioligand which can be used without the need to mask the binding to other 5-HT receptor subtypes. Springer-Verlag, 1992 [125I]GTI nationallicence 5-HTID receptors nationallicence Calf nationallicence Guinea-pig nationallicence Dog nationallicence Monkey nationallicence Human brain nationallicence Bruinvels Anne 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 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 Hoyer Daniel 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), 243-248 0028-1298 346:3<243 1992 346 210 https://doi.org/10.1007/BF00173535 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00173535 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Bruinvels Anne 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- 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 700 1- Hoyer Daniel 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), 243-248 0028-1298 346:3<243 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer