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.
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Bruinvels, A.T., Lery, H., Nozulak, J. et al. 5-HT1D binding sites in various species: similar pharmacological profile in dog, monkey, calf, guinea-pig and human brain membranes. Naunyn-Schmiedeberg's Arch Pharmacol 346, 243–248 (1992). https://doi.org/10.1007/BF00173535
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DOI: https://doi.org/10.1007/BF00173535