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Eur J Pharmacol. 1996 Sep 12;311(2-3):305-10.

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

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Department of Pharmacology, Glaxo Research & Development Ltd., Stevenage, Hertfordshire, UK.


We have examined the specific binding of the tritiated derivative of the potent histamine H3 receptor antagonist, [3,4-3H2]-cyclohex-yl-┬┐[4-(3H-imidazol-4-yl)-piperidin-l-yl] iminomethyl┬┐- amine ([3H]GR168320), to homogenates of rat cerebral cortex. Specific binding of [3H]GR168320 at 37 degrees 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 N alpha-methylhistamine.

[Indexed for MEDLINE]

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