Giudici D, D'Urso R, Falaschi P, Negri L, Melchiorri P, Motta M
Neuroendocrinology. 1984 Sep;39(3):236-44. doi: 10.1159/000123985.
The effect of dermorphin, a new opioid peptide originally isolated from amphibian skin, on the release of prolactin (Prl) was studied in vivo and in vitro. In vivo experiments: subcutaneous administrations of different doses of dermorphin ranging from 0.1 to 5 mg/kg body weight to normal male rats induce a statistically significant, dose-related increase in serum Prl levels. Pretreatment with the specific opioid antagonist, naloxone (2 mg/kg i.p.) completely prevents the rise in serum Prl, induced by 2 mg/kg of dermorphin. In normal male rats, the intraventricular injection of 0.25 micrograms/kg of dermorphin is not able to induce any significant changes in serum Prl levels 10 min after injection. Serum Prl levels show a significant enhancement 30 min after the administration of this dose of dermorphin, and return to control values at 60 min. On the contrary, 1 microgram/kg of dermorphin significantly elevates Prl concentrations 10 min after injection, leaving serum Prl levels unchanged 30 and 60 min after the administration. Naloxone (25 and 100 micrograms/kg) alone does not substantially modify serum Prl concentrations at any time interval considered. Treatment with either dose of naloxone performed together with either 0.25 or 1 microgram/kg of dermorphin completely counteracts the stimulatory effect of the peptide at all time intervals in which dermorphin was active when given alone. In orchidectomized (3 weeks) rats, the intraventricular administration of dermorphin at the dose of 0.25 micrograms/kg appears effective in enhancing Prl levels only 30 min after treatment. No statistically significant modifications are observed at 10 and 60 min with this dose.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了一种最初从两栖动物皮肤中分离出的新型阿片肽——皮啡肽对催乳素(Prl)释放的体内和体外作用。体内实验:对正常雄性大鼠皮下注射0.1至5mg/kg体重的不同剂量皮啡肽,可导致血清Prl水平出现具有统计学意义的剂量相关升高。用特异性阿片拮抗剂纳洛酮(2mg/kg腹腔注射)预处理可完全阻止2mg/kg皮啡肽诱导的血清Prl升高。在正常雄性大鼠中,脑室内注射0.25μg/kg皮啡肽在注射后10分钟不能诱导血清Prl水平发生任何显著变化。注射该剂量皮啡肽30分钟后血清Prl水平显著升高,并在60分钟时恢复到对照值。相反,1μg/kg皮啡肽在注射后10分钟显著提高Prl浓度,给药后30分钟和60分钟血清Prl水平无变化。单独使用纳洛酮(25和100μg/kg)在任何考虑的时间间隔内都不会显著改变血清Prl浓度。与0.25或1μg/kg皮啡肽一起使用任一剂量的纳洛酮进行治疗,在皮啡肽单独给药时活跃的所有时间间隔内,都能完全抵消该肽的刺激作用。在去势(3周)大鼠中,脑室内注射0.25μg/kg皮啡肽仅在治疗后30分钟有效提高Prl水平。该剂量在10分钟和60分钟时未观察到统计学上的显著变化。(摘要截短至250字)