皮啡肽

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皮啡肽(dermorphin )是阿片(opioids)的一种。

内源性类阿片肽(Endogenous opioids)是指由机体产生的具有与吗啡(鸦片有效成分)相似生理作用的一些肽类物质,包括脑啡肽内啡肽强啡肽、皮啡肽和新皮啡肽等,其作用相当广泛,以镇痛方面的研究较多,但目前对其镇痛的作用原理仍不甚了解.其中新皮啡肽(Deltorphins)是1989年从一种南美洲树蛙的皮肤中发现的具有很强镇痛活性的一类神经肽,它选择性地结合δ受体.

the receptor affinities of dermorphin and antinociceptive properties have been tested and

compared with the parent dermorphin. Dermorphin has been selected as the parent compound due

to its biological and antinociceptive properties(镇痛特征). Dermorphin expresses high affinity for the μ opioid

receptor type, and potent antinociceptive activity after application either by systemic (intraperitoneal,

ip., intravenous, i.v.) or central (intrathecal, i.t.) application. The systemic antinociceptive activity

of dermorphin is a result of significant blood-brain barrier (BBB) permeability. Therefore,

dermorphin is a good initial peptide to explore the effect of modification of a prototype molecule, as

a gamma-glutamyl analogue, on its activity following systemic or central administration.

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