The enzymatic degradation and transport of leucine-enkephalin and 4-imidazolidinone enkephalin prodrugs at the blood-brain barrier

L. Lund; A. Bak; G.J. Friis; L. Hovgaard; Lona Louring Christrup

doi:10.1016/S0378-5173(98)00192-6

The enzymatic degradation and transport of leucine-enkephalin and 4-imidazolidinone enkephalin prodrugs at the blood-brain barrier

L. Lund, A. Bak, G.J. Friis, L. Hovgaard, Lona Louring Christrup

10 Citations (Scopus)

Abstract

In this study, the stability in and transport across a cell culture model of the blood-brain barrier (BBB) is investigated for leucine-enkephalin (Leu-enkephalin) and four 4-imidazolidinone prodrugs of Leu-enkephalin. The results show that Leu-enkephalin is degraded in the cell culture model of the BBB both by cytosolic and plasma membrane bound enzymes. It is likely that aminopeptidase is the predominant enzyme responsible for the degradation of Leu-enkephalin. All four 4-imidazolidinone prodrugs of Leu-enkephalin examined showed an increased stability of Leu-enkephalin against degradation by both plasma membrane bound and cytosolic enzymes. Consequently, the transport properties of Leu-enkephalin is also improved by up to 60% by formation of 4-imidazolidinone prodrugs. Copyright (C) 1998 Elsvier Science B.V.

Original language	English
Journal	International Journal of Pharmaceutics
Volume	172
Issue number	1-2
Pages (from-to)	97-101
Number of pages	5
ISSN	0378-5173
DOIs	https://doi.org/10.1016/S0378-5173(98)00192-6
Publication status	Published - 15 Oct 1998

Access to Document

10.1016/S0378-5173(98)00192-6

http://www.sciencedirect.com/science/article/pii/S0378517398001926

Cite this

@article{1e04eca457fb49a5a0658f2bc6c1eae5,

title = "The enzymatic degradation and transport of leucine-enkephalin and 4-imidazolidinone enkephalin prodrugs at the blood-brain barrier",

abstract = "In this study, the stability in and transport across a cell culture model of the blood-brain barrier (BBB) is investigated for leucine-enkephalin (Leu-enkephalin) and four 4-imidazolidinone prodrugs of Leu-enkephalin. The results show that Leu-enkephalin is degraded in the cell culture model of the BBB both by cytosolic and plasma membrane bound enzymes. It is likely that aminopeptidase is the predominant enzyme responsible for the degradation of Leu-enkephalin. All four 4-imidazolidinone prodrugs of Leu-enkephalin examined showed an increased stability of Leu-enkephalin against degradation by both plasma membrane bound and cytosolic enzymes. Consequently, the transport properties of Leu-enkephalin is also improved by up to 60% by formation of 4-imidazolidinone prodrugs. Copyright (C) 1998 Elsvier Science B.V.",

author = "L. Lund and A. Bak and G.J. Friis and L. Hovgaard and Christrup, {Lona Louring}",

year = "1998",

month = oct,

day = "15",

doi = "10.1016/S0378-5173(98)00192-6",

language = "English",

volume = "172",

pages = "97--101",

journal = "International Journal of Pharmaceutics",

issn = "0378-5173",

publisher = "Elsevier",

number = "1-2",

}

TY - JOUR

T1 - The enzymatic degradation and transport of leucine-enkephalin and 4-imidazolidinone enkephalin prodrugs at the blood-brain barrier

AU - Lund, L.

AU - Bak, A.

AU - Friis, G.J.

AU - Hovgaard, L.

AU - Christrup, Lona Louring

PY - 1998/10/15

Y1 - 1998/10/15

N2 - In this study, the stability in and transport across a cell culture model of the blood-brain barrier (BBB) is investigated for leucine-enkephalin (Leu-enkephalin) and four 4-imidazolidinone prodrugs of Leu-enkephalin. The results show that Leu-enkephalin is degraded in the cell culture model of the BBB both by cytosolic and plasma membrane bound enzymes. It is likely that aminopeptidase is the predominant enzyme responsible for the degradation of Leu-enkephalin. All four 4-imidazolidinone prodrugs of Leu-enkephalin examined showed an increased stability of Leu-enkephalin against degradation by both plasma membrane bound and cytosolic enzymes. Consequently, the transport properties of Leu-enkephalin is also improved by up to 60% by formation of 4-imidazolidinone prodrugs. Copyright (C) 1998 Elsvier Science B.V.

AB - In this study, the stability in and transport across a cell culture model of the blood-brain barrier (BBB) is investigated for leucine-enkephalin (Leu-enkephalin) and four 4-imidazolidinone prodrugs of Leu-enkephalin. The results show that Leu-enkephalin is degraded in the cell culture model of the BBB both by cytosolic and plasma membrane bound enzymes. It is likely that aminopeptidase is the predominant enzyme responsible for the degradation of Leu-enkephalin. All four 4-imidazolidinone prodrugs of Leu-enkephalin examined showed an increased stability of Leu-enkephalin against degradation by both plasma membrane bound and cytosolic enzymes. Consequently, the transport properties of Leu-enkephalin is also improved by up to 60% by formation of 4-imidazolidinone prodrugs. Copyright (C) 1998 Elsvier Science B.V.

UR - http://www.scopus.com/inward/record.url?scp=0032531892&partnerID=8YFLogxK

U2 - 10.1016/S0378-5173(98)00192-6

DO - 10.1016/S0378-5173(98)00192-6

M3 - Journal article

AN - SCOPUS:0032531892

SN - 0378-5173

VL - 172

SP - 97

EP - 101

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -

The enzymatic degradation and transport of leucine-enkephalin and 4-imidazolidinone enkephalin prodrugs at the blood-brain barrier

Abstract

Access to Document

Other files and links

Fingerprint

Cite this