(-)-Stepholidine vs 12-chloroscoulerine enantiomers on firing activity of substantia nigral dopamine neurons

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	(-)-Stepholidine vs 12-chloroscoulerine enantiomers on firing activity of substantia nigral dopamine neurons
	Zhang, XX; Jin, GZ
刊名	ACTA PHARMACOLOGICA SINICA
	1996-01
卷号	17 期号:1 页码:18-22
关键词	stepholidine 12-chloroscoulerine electrophysiology dopamine receptors reserpine substantia nigra apomorphine benzazepines
ISSN号	0253-9756
文献子类	Article
英文摘要	To compare the potencies between (-)stepholidine ((-)-SPD) and 12-chloroscoulerine (CSL) enantiomers on firing of substantia nigra (SN) dopamine (DAS neurons. METHODS: Extracellular single unit recordings in paralyzed rats. RESULTS: In rats, (-)-SPD, (-)-, (+/-)-, and (+)-CSL attneuated iv apomorphine (Apo, 10 mu g . kg(-1)-induced inhibition on firing of DA cell, and their ED(50) values were 15.1 (11.9 - 19.4), 7.8 (7.0 - 8.7), 12.6 (2.0 - 17.9) mu g . kg(-1), and 2.9 (2.6 - 3.3) mg . kg(-1)), respectively. Thus, (-)-CSL was 1 time more potent than (-)-SPD and 371 times more potent than (+)-CSL on D-2 receptors. In reserpinized rats, (-)-SPD, (-)-, (+/-)-, and (+)-CSL blocked the inhibition caused by iv 4 mg . kg(-1) SKF-38393, with ED(50) values of 0.53 (0.51 - 0.55), 0.51 (0.43-0.60), 1.2 (0.7-2.0), and 5.9 (4.9 - 7.1) mg . kg(-1), respectively. The potency of (-)-CSL was similar to that of (-)-SPD on D-1 receptors and 11 times higher than that of (+)-CSL. CONCLUSION: CSL enantiomers are D-1/D-2 mixed antagonists as (-)-SpD. (-)-CSL is the most, while (+)-CSL is the least, potent one among them.
WOS关键词	RESERPINE TREATMENT ; CELL-ACTIVITY ; RECEPTORS ; SCH-23390 ; BRAIN
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:A1996TQ30000004
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275008]
专题	药物制剂研究中心
作者单位	CHINESE ACAD SCI,SHANGHAI INST MAT MED,SHANGHAI 200031,PEOPLES R CHINA
推荐引用方式 GB/T 7714	Zhang, XX,Jin, GZ. (-)-Stepholidine vs 12-chloroscoulerine enantiomers on firing activity of substantia nigral dopamine neurons[J]. ACTA PHARMACOLOGICA SINICA,1996,17(1):18-22.
APA	Zhang, XX,&Jin, GZ.(1996).(-)-Stepholidine vs 12-chloroscoulerine enantiomers on firing activity of substantia nigral dopamine neurons.ACTA PHARMACOLOGICA SINICA,17(1),18-22.
MLA	Zhang, XX,et al."(-)-Stepholidine vs 12-chloroscoulerine enantiomers on firing activity of substantia nigral dopamine neurons".ACTA PHARMACOLOGICA SINICA 17.1(1996):18-22.