Multi-drug resistance gene (MDR1) and opioid analgesia in horses
Opioid absorption in the intestinal tract as well as its effects in the central nervous system is modulated by the P-glycoprotein (P-gp) encoded in the Multi-drug Resistance gene (MDR1) also named ATP-binding cassete, subfamily B, member 1 (ABCB1). This MDR1 gene acts as a selective pump. The expression of this protein in humans and rodents inhibits cellular uptake of substrate opioids. The presence of the intestinal iso-enzyme CYP3A4 associated with MDR1 gene decreases the opioid analgesic activity due to an increase in intestinal metabolism, with a predicted intestinal first pass extraction around 20% which significantly influences the oral availability of opioids. In the central nervous system, P-gp expression decreases opioid neuronal uptake diminishing the analgesic effects. It is unknown if horses have the MDR1 gene and P-gp and what are the effects on opioid absorption, metabolism, and analgesia. Identifying the MDR1 gene and P-gp status in horses is of great importance in order to better understand opioid pharmacologic effects in horses.
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Universidade Federal de Santa Maria
2006
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oai:scielo:S0103-847820060001000552006-01-13Multi-drug resistance gene (MDR1) and opioid analgesia in horsesNatalini,Cláudio CorrêaCunha,Anderson Fávaro daLinardi,Renata Lehn molecular biology opioids equine gene MDR1 ABCB1 analgesia Opioid absorption in the intestinal tract as well as its effects in the central nervous system is modulated by the P-glycoprotein (P-gp) encoded in the Multi-drug Resistance gene (MDR1) also named ATP-binding cassete, subfamily B, member 1 (ABCB1). This MDR1 gene acts as a selective pump. The expression of this protein in humans and rodents inhibits cellular uptake of substrate opioids. The presence of the intestinal iso-enzyme CYP3A4 associated with MDR1 gene decreases the opioid analgesic activity due to an increase in intestinal metabolism, with a predicted intestinal first pass extraction around 20% which significantly influences the oral availability of opioids. In the central nervous system, P-gp expression decreases opioid neuronal uptake diminishing the analgesic effects. It is unknown if horses have the MDR1 gene and P-gp and what are the effects on opioid absorption, metabolism, and analgesia. Identifying the MDR1 gene and P-gp status in horses is of great importance in order to better understand opioid pharmacologic effects in horses.info:eu-repo/semantics/openAccessUniversidade Federal de Santa MariaCiência Rural v.36 n.1 20062006-02-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100055en10.1590/S0103-84782006000100055 |
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Natalini,Cláudio Corrêa Cunha,Anderson Fávaro da Linardi,Renata Lehn |
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Natalini,Cláudio Corrêa Cunha,Anderson Fávaro da Linardi,Renata Lehn Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
author_facet |
Natalini,Cláudio Corrêa Cunha,Anderson Fávaro da Linardi,Renata Lehn |
author_sort |
Natalini,Cláudio Corrêa |
title |
Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
title_short |
Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
title_full |
Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
title_fullStr |
Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
title_full_unstemmed |
Multi-drug resistance gene (MDR1) and opioid analgesia in horses |
title_sort |
multi-drug resistance gene (mdr1) and opioid analgesia in horses |
description |
Opioid absorption in the intestinal tract as well as its effects in the central nervous system is modulated by the P-glycoprotein (P-gp) encoded in the Multi-drug Resistance gene (MDR1) also named ATP-binding cassete, subfamily B, member 1 (ABCB1). This MDR1 gene acts as a selective pump. The expression of this protein in humans and rodents inhibits cellular uptake of substrate opioids. The presence of the intestinal iso-enzyme CYP3A4 associated with MDR1 gene decreases the opioid analgesic activity due to an increase in intestinal metabolism, with a predicted intestinal first pass extraction around 20% which significantly influences the oral availability of opioids. In the central nervous system, P-gp expression decreases opioid neuronal uptake diminishing the analgesic effects. It is unknown if horses have the MDR1 gene and P-gp and what are the effects on opioid absorption, metabolism, and analgesia. Identifying the MDR1 gene and P-gp status in horses is of great importance in order to better understand opioid pharmacologic effects in horses. |
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Universidade Federal de Santa Maria |
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2006 |
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http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100055 |
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AT nataliniclaudiocorrea multidrugresistancegenemdr1andopioidanalgesiainhorses AT cunhaandersonfavaroda multidrugresistancegenemdr1andopioidanalgesiainhorses AT linardirenatalehn multidrugresistancegenemdr1andopioidanalgesiainhorses |
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