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蛙皮素是最早由蛙的皮肤中提取出来的一种14肽,它的类似物已在哺乳动物的胃肠道、脑和肺中发现。这些肽有广泛而强烈的生物学效应,并且在胰腺腺泡、脑膜和垂体细胞的膜上存在受体,至今尚未发现其阻断剂。美国R.T.Jensen等最近发现了一种蛙皮素受体的竞争性阻断剂,它是人工合成的P物质(SP)类似物和拮抗剂,即[D-精,D-脯,D-色,亮]SP(简记作ASP)。他们用豚鼠的游离胰腺腺泡进行实验。已知腺泡上存在蛙皮素、P物质、胆碱(M型)、CCK、VIP和促胰液素的受体。其中蛙皮素受体仅对蛙皮素及其类似物有亲和力,它的激动可动员胞内钙并刺激胰酶分泌。蛙皮素(0.03～1nmol)可使胰淀粉酶释放增加(最大达10倍),剂量效应曲线呈S型。ASP本身(即使
Bombesin is the first 14 peptide extracted from the skin of frogs, and its analogs have been found in the gastrointestinal tract, brain and lungs of mammals. These peptides have a broad and strong biological effect and present receptors on the membranes of pancreatic acinar, meninges and pituitary cells, and no blocker has been found so far. A recent study by RT Jensen et al., USA, found a competitive blocker of the bombesin receptor, which is a synthetic analogue and antagonist of Substance P (SP), namely [D- , Bright] SP (abbreviated as ASP). They experimented with guinea pig’s free pancreatic acini. It is known that there are receptors for bombesin, substance P, choline (M type), CCK, VIP and secretin in acinar. Among them, the bombesin receptor has affinity only for bombesin and its analogs, and its activation mobilizes intracellular calcium and stimulates pancreatic enzyme secretion. Bombesin (0.03 ~ 1nmol) can increase pancreatic amylase release (up to 10 times), the dose-response curve was S-type. ASP itself (even though