皮啡肽
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皮啡肽(dermorphin )是阿片肽(opioids)的一種。
內(nèi)源性類阿片肽(Endogenous opioids)是指由機(jī)體產(chǎn)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(zhì),包括腦啡肽、內(nèi)啡肽、強(qiáng)啡肽、皮啡肽和新皮啡肽等,其作用相當(dāng)廣泛,以鎮(zhèn)痛方面的研究較多,但目前對其鎮(zhèn)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(fā)現(xiàn)的具有很強(qiáng)鎮(zhèn)痛活性的一類神經(jīng)肽,它選擇性地結(jié)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(zhèn)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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