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Effect of GNTI, a kappa opioid receptor antagonist, on MK-801-induced hyperlocomotion and stereotypy in mice

  
@article{APS3624,
	author = {Chun-ting Qi and Hong Zou and Chen-hao Zhang and Qing-lian Xie and Mei-lei Jin and Lei Yu},
	title = {Effect of GNTI, a kappa opioid receptor antagonist, on MK-801-induced hyperlocomotion and stereotypy in mice},
	journal = {Acta Pharmacologica Sinica},
	volume = {27},
	number = {11},
	year = {2016},
	keywords = {},
	abstract = {Aim: To examine the effect of GNTI [5'-guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan], a selective antagonist for the kappa opioid receptor, in the MK-801 (dizocilpine maleate)-induced behavioral model of psychosis in schizophrenia as a way to explore the involvement of the kappa opioid receptor in modulating psychotic symptoms of schizophrenia.
Methods: Two doses of MK-801 (0.3 mg/kg and 0.6 mg/kg) were administered by systemic injection in mice to induce psychosis-like behavior as a rodent schizophrenia model, preceded by an injection of different doses of GNTI. Both locomotion and stereotypy were measured as the behavioral endpoints for quantitative analysis.
Results: GNTI inhibited MK-801-induced hyperlocomotion and stereotypy. In particular, GNTI showed differential modulation of stereotypy induced by 0.3 mg/kg vs. 0.6 mg/kg MK-801.
Conclusion: Antagonism of kappa opioid receptors attenuates MK-801-induced behavior, suggesting a potential involvement of the kappa opioid receptor in psychosis-like symptoms of schizophrenia. GNTI appears to be a useful pharmacological tool to explore the kappa opioid receptor function in vivo.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/3624}
}