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Comparison of 12-chloroscoulerine enantiomers on animal behavior to dopamine receptors.

  
@article{APS8268,
	author = {Li-juan Chen and Qi-ting Zhou and Zhao-jun Dong and Lei-ping Yu and Guo-zhang Jin},
	title = {Comparison of 12-chloroscoulerine enantiomers on animal behavior to dopamine receptors.},
	journal = {Acta Pharmacologica Sinica},
	volume = {20},
	number = {10},
	year = {2016},
	keywords = {},
	abstract = {AIM:
To compare the pharmacological characteristics of 12-chloroscoulerine (CSL) enantiomers to dopamine (DA) receptors.
METHODS:
Radioligand receptor binding assay with calf striatum and behavioral tests of mice or rats were used.
RESULTS:
In the competitive binding assay, the affinities (Ki) of l-CSL to D1 and D2 receptors were 5.7 nmol.L-1, while those of d-CSL for D1 and D2 receptors were 135 and 9150 nmol.L-1, respectively. The Ki of dl-CSL to D1 and D2 receptors were 8.9 and 9.6 nmol.L-1, respectively, which were slightly weaker than that of l-CSL. In the behavioral experiments, CSL enantiomers 5-60 mg.kg-1 antagonized the stereotypy induced by apomorphine in rats, and 5-150 mg.kg-1 produced catalepsy. The enantiomers 10-60 mg.kg-1 reduced the mice jumping behavior induced by amphetamine + levodopa. l-CSL 10-80 mg.kg-1 antagonized the spontaneous locomotor activity of normal or amphetamine-treated mice.
CONCLUSION:
CSL enantiomers are antagonists to DA receptors: l-CSL > dl-CSL >> d-CSL.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/8268}
}