Morita T, Kondo S
Department of Urology, Tokyo Medical and Dental University School of Medicine.
Nihon Hinyokika Gakkai Zasshi. 1992 Mar;83(3):334-7. doi: 10.5980/jpnjurol1989.83.334.
The adrenergic alpha-1 and -2 adrenoceptors in six human hypertrophied prostatic adenomas were measured in the saturation experiment using 3H-prazosin and 3H-yohimbine. Not only alpha-1 adrenoceptons, but also alpha-2 adrenoceptors were found to exist in large amounts in prostatic adenomas. In the inhibition experiment selective alpha-1 antagonists inhibited the 3H-prozosin or 3H-yohimbine bindings to adenomas. The potency of alpha-1 antagonists in the order prazosin greater than bunazosin greater than alfuzosin greater than urapidil greater than terazosin and that of alpha-2 antagonists is urapidil greater than alfuzosin greater than terazosin greater than bunazosin greater than prazosin. These data suggest that urapidil, alfuzosin and terazosin may affect the human hypertrophied prostatic adenoma like phenoxybenzamine, nonselective alpha-1 antagonist, which was used for benign prostatic hypertrophy.
采用³H-哌唑嗪和³H-育亨宾饱和实验测定了6例人前列腺增生腺瘤中的肾上腺素能α-1和α-2肾上腺素受体。结果发现,不仅α-1肾上腺素受体,而且α-2肾上腺素受体在前列腺腺瘤中也大量存在。在抑制实验中,选择性α-1拮抗剂抑制³H-哌唑嗪或³H-育亨宾与腺瘤的结合。α-1拮抗剂的效力顺序为哌唑嗪>布那唑嗪>阿夫唑嗪>乌拉地尔>特拉唑嗪,α-2拮抗剂的效力顺序为乌拉地尔>阿夫唑嗪>特拉唑嗪>布那唑嗪>哌唑嗪。这些数据表明,乌拉地尔、阿夫唑嗪和特拉唑嗪可能像用于良性前列腺增生的非选择性α-1拮抗剂酚苄明一样影响人前列腺增生腺瘤。