SUMMARYIn a double‐blind study of Latin square design, twelve healthy male subjects were dosed with combinations of ranitidine 300 mg or placebo (at 08.50 hours) and intravenous pentagastrin (0.6 µg. kg/h) or 0. 9% saline (07.00–18.00 hours). Breakfast and lunch were served at 08.15 and 13.15 hours, respectively; hourly intragastric acidity and plasma gastrin concentration were measured from 08.00‐18.00 hours.During oral dosing with placebo, intravenous pentagastrin raised median 10‐h integrated intragastric acidity (315 to 615 pmol. h/L; P < 0.001) and lowered gastrin (86 to 55 mmol. h/L; P < 0.001). During oral dosing with ranitidine 300 mg, compared with intravenous saline, the pentagastrin infusion returned acidity towards normal (67 to 293 pmol. h/L; P < 0.001) and lowered gastrin (209 to 135 pmol. h/L; P < 0.001).This study demonstrates that a continuous pentagastrin infusion can overcome H2‐blockade and return intragastric acidity towards normal. Hypergastrinaemia observed during continued dosing with an H2‐blocket may be the mechanism for the development of tolerance.

中文翻译：

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静脉注射五肽泌素可诱发男性对单剂量 H2 受体阻滞剂的“耐受”错觉


摘要在一项拉丁方设计的双盲研究中，12 名健康男性受试者接受了雷尼替丁 300 毫克或安慰剂（08.50 小时）和静脉注射五肽泌素（0.6 微克 kg/h）或 0.9% 盐水（07.00–18.00 小时）。早餐和午餐分别在 08.15 和 13.15 供应;在 08.00-18.00 小时测量每小时胃内酸度和血浆胃泌素浓度。在口服安慰剂期间，静脉注射五肽胃泌素提高了中位 10 小时综合胃酸度（315 至 615 pmol. h/L;P < 0.001）和胃泌素降低（86 至 55 mmol. h/L;P < 0.001）。在口服雷尼替丁 300 mg 期间，与静脉注射生理盐水相比，五肽胃泌素输注的酸度恢复到正常水平（67 至 293 pmol. h/L;P < 0.001）和降低的胃泌素（209 至 135 pmol. h/L;P < 0.001）。这项研究表明，连续输注五肽胃泌素可以克服 H2 阻断并使胃内酸度恢复正常。在持续服用 H2 阻滞剂期间观察到的高胃泌素血症可能是产生耐受性的机制。