大鼠离体组织α_1受体放射配基结合分析方法的研究
Study on α1-adrenoceptor radioligand binding assay in rat tissues
作者:姜清芳;付晓晶;赵鑫;黄珺珺;袁牧;
Author:
收稿日期: 年卷(期)页码:2012,27(06):-666-669
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:α1受体;放射配基结合分析方法;3H-哌唑嗪;大鼠
Key words:
基金项目:2010年广州市科技专项(编号:2010U1-E00531-2)
中文摘要
目的建立大鼠下颌腺、肝脏、胸主动脉的α1受体放射配基结合实验的方法。方法以3H-哌唑嗪为标记配基,♂SD大鼠的下颌腺、肝脏和胸主动脉的细胞膜蛋白为受体材料,冰浴并玻璃纤维滤膜抽滤终止实验,液闪技术进行测定。结果大鼠的下颌腺、肝脏和胸主动脉的α1受体符合简单单位点受体结合模型,用Scatchard作图求出α1受体的3种亚型受体的结合参数分别为:下颌腺Bmax=155.9±1.67 pmol.L-1,KD=682.7±18.73 pmol.L-1;肝脏Bmax=149.8±1.61 pmol.L-1,KD=381.0±11.68 pmol.L-1;主动脉Bmax=146.1±2.37 pmol.L-1,KD=338.2±16.01 pmol.L-1。结论大鼠下颌腺、肝脏和胸主动脉的α1受体放射配基结合实验方法符合受体结合实验方法学的要求。
参考文献
[1]Hieble JP,Bylund DB,Clarke DE,et al.α1-Adrenoceptor sub-type substitution in knockout mice[J].Pharmacol Rev,1995,47(2):267-270.
[2]Michel AD,Loury DH,Whiting RL.Identification of a singlealpha1-adrenoceptor corresponding to the alpha-1A-subtypein rat sub maxillary gland[J].Br J Pharmacol,1989,98:883-889.
[3]Han C,J Li,KP Minneman.Subtypes of alpha-1 adrenoceptorsin rat blood vessels[J].Eur J Pharmacol,1990,190:97.
[4]Bylund DB,Toews ML.Radioligand binding methods:Practicalguide and tips[J].Am J Physiol,265:421-429.
[5]Kawabe K,Morivama N,Yamada S,et al.Rationale for the use ofalpha-blockers in the treatment of benign prostatic hyperplasia(BPH)[J].Int J Urol,1994,1(3):203-211.
[6]A Sanbe,Y Tanaka,Y Fujiwara,et al.α1-Adrenoceptors arerequired for normal male sexual function[J].Br J Pharmacol,2007,152(3):332-340.
[7]Michel MC,Insel PA.Comparison of cloned and pharmacological-ly defined rat tissue alpha 1-adrenoceptor subtypes[J].NaunynSchmiedebergs Arch Pharmacol,1994,350(2):136-142.
[8]Melinda Wuest,Lambertus PW,Martina BMR,et al.The musca-rinic receptor antagonist propiverine exhibitsα1-adrenoceptorantagonism in human prostate and porcine trigonum[J].World JUrol,2011,29(2):149-155.
【关闭】