Davies R R, Miller M, Turner S J, Goodship T H, Cook D B, Watson M, McGill A, Orskov H, Alberti K G, Johnston D G
Clin Endocrinol (Oxf). 1986 Jun;24(6):665-74. doi: 10.1111/j.1365-2265.1986.tb01663.x.
Long-acting somatostatin analogues may be of benefit in certain hypersecretory endocrine and gastrointestinal disorders. The 24 h hormonal and metabolic profiles of six normal male subjects receiving a twice daily subcutaneous injection of one such analogue SMS 201-995, 50 micrograms, has been compared to that obtained following placebo injection. Spontaneous daytime peaks of GH secretion were delayed until 1400 h following SMS 201-995 but nocturnal and total 24 h GH secretion were unaffected. The nocturnal rise in thyrotrophin was abolished by SMS 201-995 but thyroid function was unaffected. Insulin levels were suppressed following SMS 201-995 and the response to meals was inhibited. Glucose intolerance followed main meals. Glucagon levels were suppressed for up to 6 h. Circulating alanine levels were raised between 1200 h and 0600 h and there were intermittent elevations in lactate, pyruvate, glycerol and 3-hydroxybutyrate. Amino acid levels, including branched chain amino acids, were also increased. All six subjects suffered gastrointestinal side-effects. SMS 201-995, 50 micrograms, given twice daily shortly before meals does not suppress 24 h GH secretion, but demonstrates significant effects on metabolism and causes side effects in normal subjects.
长效生长抑素类似物可能对某些内分泌和胃肠道分泌过多性疾病有益。对6名正常男性受试者进行了研究,他们每日两次皮下注射50微克的此类类似物SMS 201-995,并将其24小时激素和代谢情况与注射安慰剂后的情况进行了比较。注射SMS 201-995后,生长激素(GH)分泌的白天自发峰值延迟至14:00,但夜间及24小时总GH分泌未受影响。促甲状腺激素的夜间升高被SMS 201-995消除,但甲状腺功能未受影响。SMS 201-995使胰岛素水平降低,对进餐的反应受到抑制。主餐后出现葡萄糖耐量异常。胰高血糖素水平被抑制长达6小时。12:00至06:00期间循环丙氨酸水平升高,乳酸、丙酮酸、甘油和3-羟基丁酸间歇性升高。包括支链氨基酸在内的氨基酸水平也升高。所有6名受试者均出现胃肠道副作用。每日两次在饭前短时间注射50微克的SMS 201-995不会抑制24小时GH分泌,但对代谢有显著影响,并在正常受试者中引起副作用。