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Reagent Details

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Catalogue number: CA200843
Product: H3 antagonist [clobenpropit]
Selectivity: H1: 6.55 | H2: 5.71 | H3: 7.09

 
 
Pharmacophore Clobenpropit-derivative Catalogue Number Pack Size Price
Molecular Weight 850 CA200843-TK0* 0.05 mg £137.50*
Purity ≥97% CA200843-020 0.2 mg £500
Excitation 633 nm CA200843-050 0.5 mg £1200
Emission 650 nm CA200843-100 1.0 mg £2150
 
* Ordered as part of a TestKit comprising a selection of 4 ligands, listing 4 catalogue numbers ending in -TK0
 

Imaging information

For imaging at H3, H2 and H1 receptors use solutions up to 100 nM.

Pharmacological Validation

The CA200843 ligand was shown to antagonize the activity of the agonist, histamine, in a recombinant CHO cell line expressing the human H3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene, and in similar cell lines expressing either the human H2 or H1 receptors.

For the H3, H2 and H1 expressing cell lines, the cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. Addition of CA200843 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CA200843 has no intrinsic agonist activity.

To determine the apparent KD for CA200843 at histamine H3, H2 and H1 receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1µM CA200843, and the cyclic AMP-induced expression of SPAP measured.

The apparent KD at H3, H2 and H1 was calculated from the rightward shift of the agonist response curve in the presence of CA200843, compared to the response curve for the agonist alone.

 

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