ラットのフェニレフリン誘発尿道内圧上昇及び血圧に対するシロドシン(KMD-3213)の作用 : 下部尿路選択性の検討(<特集>シロドシン)

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The effects of silodosin, an α_<1A>-adrenoceptor (AR) antagonist, and of other α_1-AR antagonists on the phenylephrine (PE)-induced increase in intraurethral pressure (IUP) and on blood pressure (BP) were studied in anesthetized rats. The drugs were administered intravenously (i.v. study) or intraduodenally (i.d. study). IUP and BP were measured via catheters inserted into the prostatic urethra and common carotid artery, respectively. In the i.v. study, drugs were administered every 30 min for effects on BP, and 5 min before each PE-injection (30μg/kg, every 60 min) with stepwise increases in dose for effects on IUP. In the i.d. study, one dose of drug was administered per rat, then IUP and BP were observed for 4h [IUP being measured time-dependently following PE-injection (30μg/kg)], and IUP and BP were expressed as a percentage of the values without any drugs. ID_<50> for IUP and ED_<15> for BP were calculated, and uroselectivity was determined as ED_<15>/ID_<50> for each drug. All drugs both inhibited the IUP increase and lowered BP, each effect being dose-dependent. The order of uroselectivities was silodosin (11.7)>tamuslosin (2.24)>naftopidil (0.133) in the i.v. study, and silodosin (26.0)>tamuslosin (3.82) >naftopidil (1.39) in the i.d. study. Selectivity for the lower urinary tract (LUT) was higher for silodosin than for tamsulosin (α_<1A>/α_<1D>-AR), naftopidil (α_<1D>-AR), or prazosin (non-selective α_1-AR). These results suggested that an α_<1A>-AR selective antagonist like silodosin might be effective in the LUT without causing hypotension.
2006-03-01

ラットのフェニレフリン誘発尿道内圧上昇及び血圧に対するシロドシン(KMD-3213)の作用 : 下部尿路選択性の検討(<特集>シロドシン)

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