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


CONCLUSIONS
CSL enantiomers are antagonists to DA receptors: l-CSL > dl-CSL >> d-CSL.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 200031, China.
L J
LJ
Chen
Q T
QT
Zhou
Z J
ZJ
Dong
L P
LP
Yu
G Z
GZ
Jin
D000818:Animals; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001522:Behavior, Animal / Q000187:drug effects; D001600:Berberine Alkaloids / Q000494:pharmacology*; D002375:Catalepsy / Q000139:chemically induced; D018491:Dopamine Agonists / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000494:pharmacology; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013239:Stereotyped Behavior / Q000187:drug effects*
C099468:12-chloroscoulerine; D001600:Berberine Alkaloids; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D001058:Apomorphine