Ho C L, Ko J L, Li C H
Int J Pept Protein Res. 1987 Apr;29(4):521-4. doi: 10.1111/j.1399-3011.1987.tb02279.x.
The peripheral opioid activity of six homologous beta-endorphins (beta-EPs) were assayed on the guinea pig ileum and the vas deferens of the mouse, the rat and the rabbit. In the guinea pig ileum assay, human beta-EP (beta h-EP) was less potent than camel, turkey, and ostrich beta-EPs, of the same potency as equine beta-EP and more active than des-acetyl salmon beta-EP. In the rat vas deferens, mammalian beta-EPs showed higher activity than those from the bird and the fish, whereas in the mouse vas deferens assay, beta h-EP is more active than those from other species. In the rabbit vas deferens, however, all homologous beta-EPs show very weak activity. The relative potency of beta-EP homologues obtained from rat vas deferens assay is in good correlation with the analgesic potency, while the receptor binding activity does not correlate with any of the four bioassays, but appears to be related to the charge properties of the peptides.
在豚鼠回肠以及小鼠、大鼠和家兔的输精管上测定了六种同源β-内啡肽(β-EP)的外周阿片样物质活性。在豚鼠回肠试验中,人β-EP(βh-EP)的效力低于骆驼、火鸡和鸵鸟β-EP,与马β-EP效力相同,且比去乙酰基鲑鱼β-EP活性更高。在大鼠输精管试验中,哺乳动物β-EP的活性高于鸟类和鱼类的β-EP,而在小鼠输精管试验中,βh-EP比其他物种的β-EP活性更高。然而,在家兔输精管试验中,所有同源β-EP的活性都非常弱。从大鼠输精管试验中获得的β-EP同系物的相对效力与镇痛效力具有良好的相关性,而受体结合活性与四种生物测定中的任何一种均无相关性,但似乎与肽的电荷性质有关。