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生长抑素类似物SMS 201-995对大鼠正常生长激素分泌的影响。与溴隐亭对正常催乳素分泌的影响的比较。

The effect of the somatostatin analog SMS 201-995 on normal growth hormone secretion in the rat. A comparison with the effect of bromocriptine on normal prolactin secretion.

作者信息

Lamberts S W, Verleun T, Zuiderwijk J M, Oosterom R

出版信息

Acta Endocrinol (Copenh). 1987 Jun;115(2):196-202. doi: 10.1530/acta.0.1150196.

Abstract

The somatostatin analog SMS 201-995 was recently shown to be effective in suppressing GH secretion and in causing tumour shrinkage in patients with GH-secreting pituitary tumours. In this respect, the action of SMS 201-995 seems similar to that of the dopamine-agonist bromocriptine in patients with PRL-secreting pituitary tumours. In the present study we compared the respective effects of SMS 201-995 and bromocriptine on normal rat GH and PRL release in vivo and in vitro. Both in vitro and in vivo, repeated administration of SMS for up till 6 days suppressed circulating GH concentrations, and the ability of the pituitary glands to release GH in vitro. A dose-dependent diminution occurred of the total pituitary GH content in rats treated in vivo with SMS 201-995 for 4-6 days. During short-term in vitro incubation for only 4 h, the total amount of GH measured in the medium + gland was also diminished. Chronic administration with SMS 201-995 (2 micrograms/kg twice daily for 15 days), however, resulted in a complete desensitization of its inhibitory effect on GH synthesis and release. In similar experiments it was shown that the dopamine agonist bromocriptine affects normal PRL secretion in a different manner. Both in vitro (10 nmol/l) and in vivo administration for 6 days (0.2 mg/kg twice daily) greatly inhibited circulating PRL levels and the ability of the pituitary glands to release PRL in vitro. This is, however, in all instances accompanied by an accumulation of PRL within the pituitary gland.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

生长抑素类似物SMS 201-995最近被证明在抑制生长激素(GH)分泌以及使分泌GH的垂体瘤患者肿瘤缩小方面有效。在这方面,SMS 201-995的作用似乎与多巴胺激动剂溴隐亭对分泌催乳素(PRL)的垂体瘤患者的作用相似。在本研究中,我们比较了SMS 201-995和溴隐亭在体内和体外对正常大鼠GH和PRL释放的各自影响。在体外和体内,重复给予SMS长达6天可抑制循环中的GH浓度以及垂体在体外释放GH的能力。用SMS 201-995在体内处理4至6天的大鼠,其垂体GH总含量出现剂量依赖性减少。在仅4小时的短期体外孵育期间,培养基+腺体中测得的GH总量也减少。然而,长期给予SMS 201-995(2微克/千克,每日两次,共15天)导致其对GH合成和释放的抑制作用完全脱敏。在类似实验中表明,多巴胺激动剂溴隐亭以不同方式影响正常PRL分泌。体外(10纳摩尔/升)和体内给予6天(0.2毫克/千克,每日两次)均极大地抑制了循环中的PRL水平以及垂体在体外释放PRL的能力。然而,在所有情况下,这都伴随着垂体腺体内PRL的积累。(摘要截短于250字)

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