Receptor Binding Studies of the Flavone, REC 15/2053, and Other Bladder Spasmolytics
Receptor Binding Studies of the Flavone, REC 15/2053, and Other Bladder Spasmolytics
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黄酮、REC 15/2053 和其他膀胱解痉药的受体结合研究
作者：
G. Abbiati;R. Ceserani;D. Nardi;C. Pietra;R. Testa
新的黄酮衍生物REC 15/2053，下尿路痉挛活性的化合物，其在体外与α-和β-去甲肾上腺素能受体，多巴胺能，毒蕈碱，肾上腺素能，阿片受体和钙通道结合位点标记的1，4-二氢吡啶从正常大鼠大脑的相互作用进行了检查。所有研究的受体都直接或间接参与下尿路功能的神经控制。研究了REC 15/2053对这些受体的活性，并将其与膀胱疾病治疗中最常用的药物如黄伏沙酯、emepronium bromide、奥昔布宁、terodiline和imipramine进行了比较。REC 15/2053仅与[3 H]尼群地平位点（IC 50 =14 µM）和毒蕈碱受体（IC 50 = 18 µM）弱结合，而黄酮哌酯仅对毒蕈碱受体有轻微活性（IC 50 = 12.2 µM）。依美普溴铵、奥昔布宁和特罗地林仅对毒蕈碱受体有活性，IC 50值分别为236、5.4和588 nM。奥昔布宁对[3 H]尼群地平结合位点的亲和力较弱（IC 50 = 44.4 µM）。丙咪嗪对α 1-肾上腺素能和毒蕈碱受体具有活性（IC 50分别= 248和653 nM）。REC 15/2053在毒蕈碱受体和1，4-二氢吡啶结合位点的活性似乎太低，无法解释其作用机制。
The new flavone derivative REC 15/2053, a compound with spasmolytic activity on the lower urinary tract, was examined for its in vitro interaction with alpha- and beta-noradrenergic receptors, dopaminergic, muscarinic, serotoninergic, and opiate receptors, and calcium-channel binding sites labeled with 1,4-dihydropyridines from normal rat brain. All the investigated receptors are directly or indirectly involved in the nervous control of the lower urinary tract functions. The activity of REC 15/2053 on these receptors was studied in comparison to the most common drugs used in the management of urinary bladder disorders such as flavoxate, emepronium bromide, oxybutynin, terodiline, and imipramine. REC 15/2053 showed only weak binding to [3H]nitrendipine sites (IC50 =14 µM) and muscarinic receptors (IC50 = 18 µM), whereas flavoxate was slightly active only at muscarinic receptors (IC50 = 12.2 µM). Emepronium bromide, oxybutynin, and terodiline were active only at muscarinic receptors, with IC50 values of 236, 5.4, and 588 nM, respectively. Oxybutynin showed a weak affinity to [3H]nitrendipine binding sites (IC50 = 44.4 µM). Imipramine was active at alpha 1-adrenergic and muscarinic receptors (IC50 = 248 and 653 nM, respectively). The activity of REC 15/2053 at muscarinic receptors and 1,4-dihydropyridine binding sites seems too low to account for its mechanism of action.
DOI：
10.1056/nejm198509263131307
发表时间：
1985
期刊：
The New England journal of medicine
影响因子：
--
作者：
Resnick,NM;Yalla,SV
通讯作者：
Yalla,SV
DOI：
--
发表时间：
1984-07
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
E. Richelson;A. Nelson
通讯作者：
E. Richelson;A. Nelson
Ca 通道拮抗剂 [3H]尼群地平与豚鼠回肠平滑肌结合的表征。
DOI：
--
发表时间：
1983
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Bolger,GT;Gengo,P;Klockowski,R;Luchowski,E;Siegel,H;Janis,RA;Triggle,AM;Triggle,DJ
通讯作者：
Triggle,DJ