PMID: 11311732Apr 20, 2001Paper

In vitro metabolism of opioid tetrapeptide agonists in various tissues and subcellular fractions from rats

Peptides
Eva KrondahlHans Lennernäs

Abstract

The metabolism of three mu-selective opioid tetrapeptide agonists, Tyr-D-Arg-Phe-Nva-NH(2) (TArPN), Tyr-D-Arg-Phe-Phe-NH(2) (TArPP), and Tyr-D-Ala-Phe-Phe-NH(2) (TAPP), was investigated in different rat tissues. High metabolic activity (<20% peptide remaining after 30 min) was found against the three peptides in the kidney homogenate and against TArPN in spleen homogenate. Low metabolic activity (>80% peptide remaining after 30 min) was found for all peptides in brain homogenate and plasma, and for TArPN and TArPP in blood. The other tissue homogenates, prepared from the small and large intestine, liver and lung, all exhibited intermediate metabolic activity (20-80% peptide remaining after 30 min) against the peptides. In all tissues investigated, the tetrapeptides were metabolized at the C-terminal amide by deamidation.A further in depth metabolic investigation was performed in subcellular fractions isolated from three tissues (small intestine, liver and kidney). In the liver, the deamidation was predominantly localized to the mitochondrial/lysosomal fraction, while hydrolysis at the N-terminal Tyr residue was the major metabolic pathway in the microsomal/brush-border membrane fraction from the kidney and small intestine.

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Citations

Feb 5, 2011·Journal of Peptide Science : an Official Publication of the European Peptide Society·Sylvia Van DorpeBart De Spiegeleer
Nov 30, 2006·British Journal of Neurosurgery·Vladimir PetrikMarios C Papadopoulos

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