Degli Uberti E C, Trasforini G, Salvadori S, Tomatis R, Margutti A, Bianconi M, Rotola C, Pansini R
J Clin Endocrinol Metab. 1983 May;56(5):1032-4. doi: 10.1210/jcem-56-5-1032.
Dermorphins (D) are heptapeptides (H-Tyr-D-Ala-Phe-Gly-Tyr-X-Ser-NH2; X, Pro or Hyp) with powerful central and peripheral opiate-like activity, originally isolated from the skin of South American frogs. To study the effect of a synthetic D on PRL secretion in man, either D (5.5 micrograms/kg . min for 30 min) or D-placebo (0.9% saline) infusion over 30 min was administered iv in random sequence to 11 volunteers (6 women and 5 men). In all the subjects, D induced a significant increase in the levels of PRL, more consistently in women than in men. To investigate whether the increase in PRL was due to the opiate agonist properties of D, the study was repeated in the same subjects during naloxone infusion. The PRL response to D was completely suppressed, suggesting that the peptide exerts its effect on PRL release via an opiate receptor stimulation of the mu-type. These data allow us to conclude that D may affect PRL release in humans; however, further investigation is necessary before any physiological significance might be attributed to D in man.
皮啡肽(D)是一种七肽(H-Tyr-D-Ala-Phe-Gly-Tyr-X-Ser-NH2;X为脯氨酸或羟脯氨酸),具有强大的中枢和外周类阿片样活性,最初是从南美青蛙的皮肤中分离出来的。为了研究一种合成皮啡肽对人体催乳素分泌的影响,11名志愿者(6名女性和5名男性)被随机静脉注射皮啡肽(5.5微克/千克·分钟,持续30分钟)或皮啡肽安慰剂(0.9%生理盐水),持续30分钟。在所有受试者中,皮啡肽均使催乳素水平显著升高,女性比男性更明显。为了研究催乳素升高是否归因于皮啡肽的阿片类激动剂特性,在同一受试者中于纳洛酮输注期间重复该研究。对皮啡肽的催乳素反应被完全抑制,表明该肽通过μ型阿片受体刺激对催乳素释放发挥作用。这些数据使我们得出结论,皮啡肽可能影响人体催乳素释放;然而,在赋予皮啡肽在人体中的任何生理意义之前,还需要进一步研究。