皮啡肽

皮啡肽(dermorphin )是阿片肽(opioids)的一種。

內源性類阿片肽(Endogenous opioids)是指由機體產生的具有與嗎啡(鴉片有效成分)相似生理作用的一些肽類物質,包括腦啡肽、內啡肽、強啡肽、皮啡肽和新皮啡肽等,其作用相當廣泛,以鎮痛方面的研究較多,但目前對其鎮痛的作用原理仍不甚了解.其中新皮啡肽(Deltorphins)是1989年從一種南美洲樹蛙的皮膚中發現的具有很強鎮痛活性的一類神經肽,它選擇性地結合δ受體.

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（鎮痛特徵）. 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.