scholarly journals The role of ABC transporters of the blood-brain barrier in opioid tolerance development

2018 ◽  
Vol 72 ◽  
pp. 58-68
Author(s):  
Kamila Środa-Pomianek ◽  
Anna Palko-Łabuz ◽  
Przemysław Pomianek ◽  
Olga Wesołowska
Keyword(s):  
Chronic Pain ◽  
Substrate Specificity ◽  
Blood Brain Barrier ◽  
Abc Transporters ◽  
Pain Treatment ◽  
Brain Barrier ◽  
P Glycoprotein ◽  
Blood Brain ◽  
Chronic Pain Treatment

Opioids constitute an important group of drugs used in chronic pain treatment, e.g. cancer pain. Unfortunately, the development of the organism’s tolerance to the analgesic activity of opioids, the tendency to develop addictions and undesirable side effects are the main causes reducing opioid efficiency in chronic pain treatment. Among many mechanisms connected to emerging of opioid resistance the ATP-binding cassette (ABC) transporters present at the blood-brain barrier may play an important role. These transporter proteins, especially P-glycoprotein (ABCB1, MDR1), affect pharmacokinetics of many drugs and xenobiotics that are their substrates. ABC transporters reduce cellular uptake of drugs and/or increase their export from brain tissue to blood. Substrate specificity of P-glycoprotein is extremely wide and comprises many structurally and functionally unrelated compounds. What is interesting, substrate specificity of P-glycoprotein overlaps to a great extent the specificity of the isoforms of cytochrome P450 involved in drug metabolism. In the present review, the ABC proteins-mediated transport of opioids was discussed as well as the mechanisms of transport regulation. Cellular metabolism of various opioid drugs and the role of ABC transporters in their absorption, distribution and elimination were also described.

scholarly journals The role of P-glycoprotein in blood-brain barrier transport of morphine: transcortical microdialysis studies in mdr1a (−/−) and mdr1a (+/+) mice

1999 ◽  
Vol 128 (3) ◽  
pp. 563-568 ◽  
Author(s):  
Rujia Xie ◽  
Margareta Hammarlund-Udenaes ◽  
Albertus G De Boer ◽  
Elizabeth C M De Lange
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
P Glycoprotein ◽  
Blood Brain

Evaluation of the role of P-glycoprotein in inflammation induced blood–brain barrier damage

Neuroreport ◽  
2002 ◽  
Vol 13 (18) ◽  
pp. 2593-2597 ◽  
Author(s):  
Kian H. Tan ◽  
Wendy M. Purcell ◽  
Simon J. R. Heales ◽  
Julie D. McLeod ◽  
Roger D. Hurst
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
P Glycoprotein ◽  
Blood Brain ◽  
Blood Brain Barrier Damage

scholarly journals Role of Two Efflux Proteins, ABCB1 and ABCG2 in Blood-Brain Barrier Transport of Bromocriptine in a Murine Model of MPTP-Induced Dopaminergic Degeneration

2009 ◽  
Vol 12 (2) ◽  
pp. 199 ◽  
Author(s):  
Sarah Vautier ◽  
Aline Milane ◽  
Christine Fernandez ◽  
Helene Chacun ◽  
Lucette Lacomblez ◽  
...  
Keyword(s):  
Experimental Model ◽  
Blood Brain Barrier ◽  
Abc Transporters ◽  
Murine Model ◽  
Drug Transport ◽  
Brain Barrier ◽  
Blood Brain ◽  
Mptp Model ◽  
Dopaminergic Degeneration

Purpose: MPTP-induced dopaminergic degeneration is an experimental model commonly used to explore Parkinson’s disease. Cerebral drug transport by ABC transporters in MPTP models has never been reported. Methods: We have investigated the transport of bromocriptine through the blood-brain barrier (BBB) in a MPTP model to understand the influence of the dopaminergic degeneration on ABCB1 and ABCG2. Results: We have shown that in MPTP treated mice, bromocriptine is widely distributed to brain (2.3-fold versus control, p

The Functional Role of P-Glycoprotein in the Blood–Brain Barrier

1997 ◽  
Vol 86 (8) ◽  
pp. 881-884 ◽  
Author(s):  
Judith Van Asperen ◽  
Ulrich Mayer ◽  
Olaf Van Tellingen ◽  
Jos H. Beijnen
Keyword(s):  
Blood Brain Barrier ◽  
Functional Role ◽  
Brain Barrier ◽  
P Glycoprotein ◽  
Blood Brain

The Role of P-Glycoprotein at the Blood–Brain Barrier in Neurological and Psychiatric Disease

2020 ◽  
pp. 45-81
Author(s):  
Pascalle Mossel ◽  
Anna L. Bartels ◽  
Peter Paul de Deyn ◽  
Gert Luurtsema
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Psychiatric Disease ◽  
P Glycoprotein ◽  
Blood Brain

scholarly journals The Role of P-Glycoprotein in Transport of Danshensu across the Blood-Brain Barrier

2011 ◽  
Vol 2011 ◽  
pp. 1-5 ◽  
Author(s):  
Peng-Fei Yu ◽  
Wen-Yan Wang ◽  
Gaowa Eerdun ◽  
Tian Wang ◽  
Lei-Ming Zhang ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Salvia Miltiorrhiza ◽  
Water Soluble ◽  
Brain Barrier ◽  
Saline Control ◽  
Control Group ◽  
P Glycoprotein ◽  
Blood Brain ◽  
The Brain

Danshensu (3-(3, 4-dihydroxyphenyl) lactic acid), a water-soluble active component isolated from the root ofSalvia miltiorrhizaBunge, is widely used for the treatment of cerebrovascular diseases. The present study aims to investigate the role of P-glycoprotein in transport of Danshensu across the blood-brain barrier. Sprague-Dawley rats were pretreated with verapamil at a dose of 20 mg kg−1(verapamil group) or the same volume of normal saline (control group). Ninety minutes later, the animals were administrated with Danshensu (15 mg kg−1) by intravenous injection. At 15 min, 30 min, and 60 min after Danshensu administration, the levels of Danshensu in the blood and brain were detected by high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). The results showed that Danshensu concentrations in the brain of the rats pretreated with verapamil were significantly increased. In addition, the brain-plasma ratios of the group pretreated with verapamil were much higher than that of the control group. There was no difference in Danshensu level in plasma between the verapamil group and control group. The findings indicated that Danshensu can pass the blood-brain barrier, and P-glycoprotein plays an important role in Danshensu transportation in brain.

scholarly journals Role of blood-brain barrier P-glycoprotein in limiting brain accumulation and sedative side-effects of asimadoline, a peripherally acting analgaesic drug

1999 ◽  
Vol 127 (1) ◽  
pp. 43-50 ◽  
Author(s):  
J W Jonker ◽  
E Wagenaar ◽  
L Van Deemter ◽  
R Gottschlich ◽  
H M Bender ◽  
...  
Keyword(s):  
Side Effects ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
P Glycoprotein ◽  
Blood Brain
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