Search results for "Dietary aminoacid"

showing 2 items of 2 documents

Partially competitive inhibition of intestinal baclofen absorption by beta-alanine, a nonessential dietary aminoacid.

1991

In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption rate pseudoconstants of the spasmolytic drug decrease as beta-alanine concentration increases, until a limiting value is obtained (36.8 per cent of that found for baclofen alone). A computer method was developed in order to calculate parameters governing baclofen absorption in the presence of beta-aminoacid, with the following results: Vm = 11.22 mM h-1; Km = 7.42 mM; Ki = 2.4…

Absorption (pharmacology)MaleBaclofenStereochemistryPharmaceutical Sciencebeta-AlanineMichaelis–Menten kineticsIntestinal absorptionchemistry.chemical_compoundNon-competitive inhibitionPharmacokineticsIntestine SmallAnimalsPharmacology (medical)Drug InteractionsPharmacologyChromatographyWaterRats Inbred StrainsGeneral MedicineRatsDietary aminoacidBaclofenchemistryIntestinal Absorptionbeta-AlanineBiopharmaceuticsdrug disposition
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Influence of leucine on intestinal baclofen absorption as a model compound of neutral α-aminoacids

1995

The inhibitory effect of the essential alpha-aminoacid L-leucine on the intestinal absorption of the antispastic drug baclofen was examined by means of an in situ rat gut perfusion technique. When 0.5 mM baclofen solutions were perfused in the presence of increasing concentrations of the aminoacid (5-100 mM), the apparent absorption rate constant of the drug decreased as the initial leucine concentration increased. Higher leucine concentrations however did not completely abolish the absorption of the drug (at 100 mM of leucine, only 76% inhibition was observed). The interaction can be mathematically described as a complete competitive inhibition with a second component, K = 0.35 (+/- 0.08)h…

MaleAbsorption (pharmacology)Baclofenmedicine.medical_specialtyTime FactorsPharmaceutical ScienceModels BiologicalIntestinal absorptionchemistry.chemical_compoundNon-competitive inhibitionLeucineInternal medicinemedicineAnimalsPharmacology (medical)Amino AcidsRats WistarPharmacologychemistry.chemical_classificationChromatographyDose-Response Relationship DrugChemistryGeneral MedicineRatsAmino acidBioavailabilityDietary aminoacidKineticsBaclofenEndocrinologyIntestinal AbsorptionLeucineBiopharmaceutics & Drug Disposition
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