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Effect of a Selective and Potent Central Nervous System Penetrant, neurokinin-3 Receptor Antagonist (SB-222200), on Cisplatin-Induced Emesis in the Ferret

Effect of a Selective and Potent Central Nervous System Penetrant, neurokinin-3 Receptor Antagonist (SB-222200), on Cisplatin-Induced Emesis in the Ferret

Andrew G King, Gareth J Sanger

Neurosci Lett. 2005 Mar 7;376(1):5-8.

PMID: 15694264

Abstract:

The anti-emetic activity of selective NK-1 receptor antagonism is well established. However, little is known of the possibility that other NK receptors might also be involved in the emetic reflex. Given the reported location of NK-3 receptors within the rat brainstem vagal motor and sensory nuclei, we investigated the ability of SB-222200, a brain-penetrant NK-3 receptor antagonist, to interfere with emesis evoked in ferrets by the emetogenic cytotoxic agent cisplatin. In contrast to control anti-emetic experiments using the 5-HT3 receptor antagonist ondansetron, SB-222200 was found to have no effects on cisplatin-induced vomiting or on the associated reductions in feeding and drinking behaviors at any dose tested. We suggest that if NK-3 receptors are involved in the mechanisms of cisplatin-induced nausea and vomiting, they play only a minor role, relative to the major anti-emetic activity exhibited by 5-HT3 or NK-1 receptor antagonism.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP174635699	SB 222200		174635-69-9	Price

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