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首页> 外文期刊>Journal of pharmacological sciences. >Effects of 4-Ethylamino-2-butynyl(2-cyclohexyl-2-phenyl)glycolate Hydrochloride, a Metabolite of Oxybutynin, on Bladder Specimens and Rhythmic Bladder Contraction in Rats in Comparison With Oxybutynin.
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Effects of 4-Ethylamino-2-butynyl(2-cyclohexyl-2-phenyl)glycolate Hydrochloride, a Metabolite of Oxybutynin, on Bladder Specimens and Rhythmic Bladder Contraction in Rats in Comparison With Oxybutynin.

机译：与奥昔布宁相比，盐酸奥昔布宁的代谢产物4-乙基氨基-2-丁炔基（2-环己基-2-苯基）乙二醇盐酸盐对大鼠膀胱标本和节律性膀胱收缩的影响。

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摘要

Oxybutynin has been used for neurogenic bladder disorders and is known to have anti-cholinergic and antispasmodic properties. However, the anti-cholinergic and antispasmodic properties of 4-ethylamino-2-butynyl(2-cyclohexyl-2-phenyl)glycolate hydrochloride (N-desethyloxybutynin: DEOB), a metabolite of oxybutynin, have not been clarified. Therefore, in the present study, we studied these properties by using rat urinary bladder specimens in comparison with oxybutynin. Moreover, the effect of DEOB on rhythmic urinary bladder contraction was also evaluated using anesthetized rats. DEOB and oxybutynin concentration-dependently inhibited the carbachol-induced contraction, the pA(2) values being 7.19 and 7.11, respectively. DEOB and oxybutynin also concentration-dependently inhibited the 100 mM KCl-induced contraction, the ED(50) values being 12.1 and 10.4 microM, respectively. Intravenously administered DEOB and oxybutynin dose-dependently (0.03 - 0.3 mg/kg) inhibited the amplitude of the rhythmic bladder contraction to similar degrees, but had no affect on the frequency. From the above results, it was determined that DEOB has anti-cholinergic and antispasmodic properties and that these activities were almost equal to those of oxybutynin. Therefore, DEOB may play an important role during oxybutynin therapy for neurogenic bladder disorder.
机译：奥昔布宁已用于神经源性膀胱疾病，并已知具有抗胆碱能和抗痉挛性质。然而，4-羟乙基氨基-2-丁炔基（2-环己基-2-苯基）乙二醇盐酸盐（N-desethyloxybutynin：DEOB），一种奥昔布宁的代谢产物，其抗胆碱能和解痉性质尚未阐明。因此，在本研究中，我们通过与奥昔布宁相比使用大鼠膀胱标本研究了这些特性。此外，还使用麻醉的大鼠评价了DEOB对节律性膀胱收缩的作用。 DEOB和奥昔布宁浓度依赖性抑制卡巴胆碱引起的收缩，pA（2）值分别为7.19和7.11。 DEOB和奥昔布宁也浓度依赖性地抑制100 mM KCl诱导的收缩，ED（50）值分别为12.1和10.4 microM。静脉内施用DEOB和奥昔布宁剂量依赖性（0.03-0.3 mg / kg）抑制节律性膀胱收缩的幅度相似，但对频率没有影响。从以上结果可以确定DEOB具有抗胆碱能和抗痉挛性质，并且这些活性几乎与奥昔布宁相同。因此，DEOB可能在奥昔布宁治疗神经源性膀胱疾病中起重要作用。

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