Species variations in RU 24969 interactions with non-5-HT1A binding sites

The interaction of RU 24969 with [3H]5-hydroxytryptamine ([3H]5-HT) binding to non-5-HT1A binding sites was analyzed in nine species. Non-5-HT1A binding was defined as specific [3H]5-HT binding observed in the presence of 100 nM 8-OH-DPAT. Computer-assisted iterative curve fitting of RU 24969 compet...

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Bibliographic Details
Published inEuropean journal of pharmacology Vol. 122; no. 2; p. 279
Main Authors Heuring, R E, Schlegel, J R, Peroutka, S J
Format Journal Article
LanguageEnglish
Published Netherlands 18.03.1986
Subjects
8-Hydroxy-2-(di-n-propylamino)tetralin
Animals
Binding, Competitive - drug effects
Brain Chemistry - drug effects
Cattle
Chickens
Dogs
Guinea Pigs
Humans
Indoles - pharmacology
Kinetics
Mice
Mice, Inbred BALB C
Rana pipiens
Rats
Rats, Inbred Strains
Receptors, Serotonin - metabolism
Species Specificity
Tetrahydronaphthalenes - pharmacology
Turtles
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Summary:The interaction of RU 24969 with [3H]5-hydroxytryptamine ([3H]5-HT) binding to non-5-HT1A binding sites was analyzed in nine species. Non-5-HT1A binding was defined as specific [3H]5-HT binding observed in the presence of 100 nM 8-OH-DPAT. Computer-assisted iterative curve fitting of RU 24969 competition studies indicate that RU 24969 distinguishes two distinct components of non-5-HT1A sites in rat and mouse brain. These two binding components display apparent Ki values of 0.33-0.39 and 66-130 nM for RU 24969. By contrast, RU 24969 competition for non-5-HT1A binding in guinea-pig, cow, human, dog, chicken, turtle and frog brain membranes is consistent with a homogeneous population of [3H]5-HT binding sites. This population of sites displays apparent Ki values of 23-130 nM for RU 24969 and appear to be analogous to the low affinity component of non-5-HT1A sites identified in rat and mouse.
ISSN:0014-2999
DOI:10.1016/0014-2999(86)90114-7