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Effect of BU98008, an imidazoline1-binding Site Ligand, on Body Temperature in Mice

Effect of BU98008, an imidazoline1-binding Site Ligand, on Body Temperature in Mice

Naomi Cambridge, Emma S J Robinson

Eur J Pharmacol. 2005 Sep 5;519(1-2):86-90.

PMID: 16109403

Abstract:

Previous studies using the novel imidazoline1-binding site ligand 1-(4,5-dihydro-1H-imidazol-2-yl)isoquinoline hydrochloride, BU98008, have shown it induces a hypothermic response in rodents following intraperitoneal administration. Radioligand binding data has shown that BU98008 is a highly selective imidazoline1-binding site ligand with 300 fold selectively for the imidazoline1-binding site relative to alpha2-adrenoceptors. However, alpha2-adrenoceptor agonists are known to induce hypothermia, therefore, the present study has investigated the ability of the selective alpha2-adrenoceptor antagonist, RX811059 (2-ethoxy idazoxan) and the mixed imidazoline1-binding site/alpha2-adrenoceptor antagonist, efaroxan, to attenuate the BU98008-induced hypothermia. Preliminary experiments confirmed that BU98008 induced a dose-dependent decrease in body temperature in mice at 10 and 20 mg/kg. The response was not affected by pre-treatment with RX811059 but was significantly attenuated following pre-treatment with efaroxan. These data suggest that BU98008-induced hypothermia is mediated by activation of imidazoline1-binding site. Body temperature may therefore provide a novel assay for investigating agonist and antagonist action at the imidazoline1-binding site.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP89197002	Efaroxan hydrochloride		89197-00-2	Price

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