Elucidation of the rapid in vivo metabolism of arecoline

1. 1. The metabolism of arecoline (ARE) was examined in homogenates of mouse blood, brain, kidney, and liver tissue. 2. 2. Liver and kidney tissues exhibited the greatest rates of ARE metabolism. 3. 3. The specific carboxylesterase inhibitor TOCP (tri- o-tolyl-phosphate) as well as ISO-OMPA (tetrais...

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Veröffentlicht in:	General pharmacology 1993-05, Vol.24 (3), p.641-647
Hauptverfasser:	Patterson, T.A., Kosh, J.W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arecoline - metabolism Biological and medical sciences Carboxylic Ester Hydrolases - antagonists & inhibitors Carboxylic Ester Hydrolases - metabolism Cholinergic system Hydrolysis In Vitro Techniques Kinetics Liver - drug effects Liver - enzymology Liver - metabolism Male Medical sciences Mice Mice, Inbred ICR Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Swine Tetraisopropylpyrophosphamide - pharmacology Tritolyl Phosphates - pharmacology
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Zusammenfassung:	1. 1. The metabolism of arecoline (ARE) was examined in homogenates of mouse blood, brain, kidney, and liver tissue. 2. 2. Liver and kidney tissues exhibited the greatest rates of ARE metabolism. 3. 3. The specific carboxylesterase inhibitor TOCP (tri- o-tolyl-phosphate) as well as ISO-OMPA (tetraisopropyl-pyrophosphoramide) completely blocked ARE metabolism in liver homogenate. 4. 4. ISO-OMPA significantly inhibited ARE metabolism by purified porcine liver carboxylesterase. 5. 5. The data suggest that carboxylesterase (EC 3.1.1.1) is primarily responsible for the metabolism of ARE in the mouse.
ISSN:	0306-3623 1879-0011
DOI:	10.1016/0306-3623(93)90224-L