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. 1996 Sep 12;311(2-3):305-10.
doi: 10.1016/0014-2999(96)00428-1.

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

J D Brown  1 , C T O'Shaughnessy, G J Kilpatrick, D I Scopes, P Beswick, J W Clitherow, J C Barnes
Affiliations

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

J D Brown et al. Eur J Pharmacol. .

Abstract

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.

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