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Characteristics of Binding of [$^{3}$H]WAY100635 to Rat Hippocampal Membranes

Content Provider	Springer Nature Link
Author	Parkel, Sven Rinken, Ago
Copyright Year	2006
Abstract	Kinetic analysis of binding of [$^{3}$H][N-[2-[4-(2-[O-methyl-$^{3}$H]methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexane carboxamide ([$^{3}$H]WAY100635) to 5-HT$_{1A}$ receptors in rat hippocampal membranes has revealed complex regulation mechanism for this radioligand. Saturation binding experiments revealed that [$^{3}$H]WAY100635 binds to a single class of receptors with very high apparent affinity (K $_{D}$ = 87 ± 4 pM, B $_{max}$ = 15.1 ± 0.2 fmol/mg protein). The binding was almost irreversible, as the dissociation rate constant obtained k $_{off}$ = (7.8 ± 1.1) × 10$^{−3}$ min$^{−1}$, means that equilibrium with this radioligand cannot be achieved before 7.5 h incubation at 25°C. Systematic association kinetic studies of [$^{3}$H]WAY100635 binding revealed sharp reaction acceleration at higher radioligand concentration, proposing mechanism of positive cooperativity. The affinities of antagonists determined from competition with [$^{3}$H]WAY100635 did not coincide with their abilities to inhibit 5-HT-dependent activation of [$^{35}$S]GTPγS binding probably due to the ligand’s kinetic peculiarities. Thus, [$^{3}$H]WAY100635 appears to be an excellent tool for determining receptor binding sites, but its applicability in equilibrium studies is strongly limited.
Starting Page	1135
Ending Page	1140
Page Count	6
File Format	PDF
ISSN	03643190
Journal	Neurochemical Research
Volume Number	31
Issue Number	9
e-ISSN	15736903
Language	English
Publisher	Springer US
Publisher Date	2006-08-26
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	[$^{3}$H]WAY100635 5-HT$_{1A}$ receptor Rat Hippocampus Kinetics Saturation binding Serotonergic antagonist Neurology Biochemistry Neurosciences
Content Type	Text
Resource Type	Article
Subject	Medicine Biochemistry Cellular and Molecular Neuroscience

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