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Provedor de dados:  Ciência Rural
País:  Brazil
Título:  Multi-drug resistance gene (MDR1) and opioid analgesia in horses
Autores:  Natalini,Cláudio Corrêa
Cunha,Anderson Fávaro da
Linardi,Renata Lehn
Data:  2006-02-01
Ano:  2006
Palavras-chave:  Molecular biology
Opioids
Equine
Gene
MDR1
ABCB1
Analgesia
Resumo:  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.
Tipo:  Info:eu-repo/semantics/article
Idioma:  Inglês
Identificador:  http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-84782006000100055
Editor:  Universidade Federal de Santa Maria
Relação:  10.1590/S0103-84782006000100055
Formato:  text/html
Fonte:  Ciência Rural v.36 n.1 2006
Direitos:  info:eu-repo/semantics/openAccess
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