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

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 a...

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Bibliographic Details
Published in:European journal of pharmacology 1996-09, Vol.311 (2-3), p.305-310
Main Authors: BROWN, J. D, O'SHAUGHNESSY, C. T, KILPATRICK, G. J, SCOPES, D. I. C, BESWICK, P, CLITHEROW, J. W, BARNES, J. C
Format: Article
Language:English
Subjects:
Animals
Binding, Competitive
Biological and medical sciences
Cerebral Cortex - metabolism
Histamine and antagonists. Allergy
Imidazoles - chemistry
Imidazoles - metabolism
Male
Medical sciences
Methylhistamines - metabolism
Pharmacology. Drug treatments
Radioligand Assay
Rats
Receptors, Histamine H3 - metabolism
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Summary: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.
ISSN:0014-2999
1879-0712
DOI:10.1016/0014-2999(96)00428-1