[Experimental study of the biological activities of several alpha1-adrenoceptor antagonists in vitro].
OBJECTIVE
To study the biological activities of several alpha1-adrenoceptor antagonists in vitro.


METHODS
The anococcygeal muscle from male Sprague-Dawley rats (300-350 g) was isolated, removed and suspended in a 20-ml organ chamber containing Krebs solution at 37 degrees C, pH 7.4. The muscle preparations were set at a resting tension of 1.0 g and allowed to equilibrate for 1 h in the Krebs solution. After thorough washing, the anococcygeal muscle preparations were examined for the effects of the tested compounds with increased concentrations on its contractile/relaxant responses and the pA2 of antagonistic activity was assessed.


RESULTS
Some of the target compounds displayed blocking activity to alpha1-adrenoceptor.


CONCLUSIONS
Compounds WB IV-1 and WB IV-3 showed good inhibiting activity, and were worth further studying.
Wu
Bin
B
School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu 210029, China. wubin@njmu.edu.cn
Zhong
Yan
Y
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D001003:Anal Canal / Q000187:drug effects; D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D051381:Rats; D017207:Rats, Sprague-Dawley
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists