Rivier C, Rivier J, Vale W
Endocrinology. 1978 Feb;102(2):519-22. doi: 10.1210/endo-102-2-519.
Bombesin and other related peptides isolated from the skin of anuran species and found in mammalian brain stimulate PRL and GH release in steroid-primed male rats. On a molar basis, bombesin and alytesin are the most active peptides in this assay system. Their PRL- and GH-releasing activity is not affected by the type of anesthetics used, but their minimal effective dose is lower after intravenous administration as compared with intracisternal administration. The in vivo stimulatory effect of bombesin on PRL secretion is not modified by the histamine antagonist diphenhydramine or the opiate antagonist naloxone. By contrast, naloxone reverses the GH-releasing activity of bombesin, suggesting an opiate-dependent mechanism of action of this peptide on GH secretion. The absence of an in vitro effect of bombesin and related peptides on PRL and GH secretion and a minimal effective dose of approximately 30 ng in bombesin and alytesin administered in steroid-primed rats, make them the most active peptides reported so far to act on the brain to modify PRL and GH secretion.
从无尾两栖类动物皮肤中分离出来并在哺乳动物大脑中发现的蛙皮素及其他相关肽,可刺激经类固醇预处理的雄性大鼠释放催乳素(PRL)和生长激素(GH)。在该测定系统中,按摩尔计算,蛙皮素和产婆蟾肽是最具活性的肽。它们的PRL和GH释放活性不受所用麻醉剂类型的影响,但与脑池内给药相比,静脉给药后的最小有效剂量更低。蛙皮素对PRL分泌的体内刺激作用不受组胺拮抗剂苯海拉明或阿片类拮抗剂纳洛酮的影响。相比之下,纳洛酮可逆转蛙皮素的GH释放活性,这表明该肽对GH分泌的作用机制依赖于阿片类物质。蛙皮素及相关肽对PRL和GH分泌无体外作用,且在经类固醇预处理的大鼠中给予蛙皮素和产婆蟾肽时最小有效剂量约为30 ng,这使它们成为迄今为止报道的作用于大脑以调节PRL和GH分泌的最具活性的肽。