Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320

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Abstract

We have examined the specific binding of the tritiated derivative of the potent histamine H3 receptor antagonist, [3,4-3H2]-cyclohexyl-{[4-(3H-imidazol-4-yl)-piperidin-1-yl]iminomethyl}-amine ([3H]GR168320), to homogenates of rat cerebral cortex. Specific binding of [3H]GR168320 at 37°C associated and dissociated rapidly. Binding was saturable (Bmax 412 ± 89 fmol/mg protein) and of high affinity (Kd 0.12 ± 0.11 nM). Saturation studies suggested the involvement of a single site. Histamine H3 receptor agonists and antagonists inhibited [3H]GR168320 binding with high affinity. Agonist and antagonist affinities correlated when compared with affinities obtained using the tritiated histamine H3 agonist radioligand Nα-methylhistamine.

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