Uptake of quaternary ammonium compounds into rat intestinal brush border membrane vesicles

Ruifrok, Peter G.

doi:10.1016/0006-2952(81)90531-1

Cited by 13 publications

(3 citation statements)

References 12 publications

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“…As one absorption mechanism of a QAC like propantheline, the following was considered: firstly the rapid binding to the brush border membrane would take place and thereafter the QAC would enter into the epithelium stimulated by the transmembrane electrical potential difference (interior negative). Our present results are partly consistent with those of Ruifrok (1981) in that the transmembrane potential difference stimulates the transport of the QAC across brush border membrane, but he made no mention of rapid binding to the brush border membrane.…”

Section: Effect Of Transmembrane Electrical Potential Difference (Inssupporting

confidence: 91%

Transport Characteristics of Propantheline Across Rat Intestinal Brush Border Membrane

Shinmoto

Kawai

Miyazaki

et al. 1988

Journal of Pharmacy and Pharmacology

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The transport mechanism of propantheline, an anti-acetylcholine quaternary ammonium compound, has been studied using brush border membrane vesicles isolated from rat small intestine. The uptake of propantheline was facilitated by the transmembrane electrical potential difference (cell interior negative) induced by NaSCN, NaI or valinomycin. But this effect was a secondary action; in the initial phase of propantheline uptake (less than 5 min), there was no facilitating effect. When the transmembrane potential difference was induced after propantheline uptake had reached a steady state, there was an overshoot of the drug. Therefore, it is suggested that the transport of propantheline across the brush border membrane consists of at least two processes. In the first, propantheline rapidly binds to the brush border membrane, in the second it enters into epithelium driven by the negative transmembrane electrical potential difference. Cationic tertiary amines such as chlorpromazine, imipramine and promethazine markedly inhibited propantheline uptake. These results suggest that there is a common absorption process for tertiary amines and quaternary ammonium compounds.

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Section: Effect Of Transmembrane Electrical Potential Difference (Inssupporting

confidence: 91%

Transport Characteristics of Propantheline Across Rat Intestinal Brush Border Membrane

Shinmoto

Kawai

Miyazaki

et al. 1988

Journal of Pharmacy and Pharmacology

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“…The suggestion of such a removal process operating in the mouse stomach assay is based on the reports of quaternary ammonium ion uptake processes which have been described in the gastrointestinal tract, kidney and liver (Ruifrok, 1981;. Preliminary attempts have been made to explore this hypothesis with the ultimate aim of blocking the removal process so that competitive behaviour is achieved over the full concentration range of N-methylatropine.…”

Section: When Investigating Agonist-antagonist Interactions Itmentioning

confidence: 99%

Pharmacological analysis of muscarinic receptors coupled to oxyntic cell secretion in the mouse stomach

Black¹,

Shankley²

1985

British J Pharmacology

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1 In the light of recent attempts to subclassify muscarinic receptors, agonist-antagonist interactions at muscarinic receptors have been re-examined using improved techniques, on the mouse, isolated, lumen-perfused stomach gastric acid assay.2 Using 5-methylfurmethide as the muscarinic agonist, the pKB estimated for atropine was significantly lower on the stomach assay (7.78) than on the guinea-pig trachea (8.93). However pKB values for N-methylatropine, the quaternary ammonium derivative of atropine, at concentrations producing dose-ratios above 20 on the stomach assay (pKB = 9.67), and over the full concentration range studied on the trachea (pKB = 9.69) were not significantly different.3 The deviation from simple competitive behaviour at low dose-ratios with N-methylatropine in the stomach assay is consistent with the effects of a saturable uptake mechanism for quaternary ammonium compounds. 4 The pKB values for pirenzepine on the stomach (6.67) and the trachea (6.87) were not significantly different suggesting that pirenzepine behaves more like N-methylatropine in terms of expressed affinity. 5 We conclude that the oxyntic cell muscarinic receptors are homogeneous with those in the guineapig trachea. An initial exploration suggests that there is a relationship between the lipophilicity (log P) of the antagonists and the degree of apparent underestimation of antagonist affinity in the stomach assay. This supports the hypothesis that the underestimation of antagonist affinity is due to the loss of antagonist into the gastric secretion from the receptor compartment. Apparently, relatively selective inhibition of acid secretion, compared to atropine, could be explained without the need to postulate heterogeneity of muscarinic receptor populations.

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“…Unfortunately, methotrexate is a poorly soluble and hydrophilic drug, and thus possesses low permeability across mucosal membranes. Ion pairing concepts for a hydrophilic drug with an appropriate counter ion, in order to improve its permeability and hence bioavailability have been well established by the research activity of Neubert et al2, 3 Also, the permeation of ion paired cationic as well as anionic hydrophilic drugs has been researched in vitro and in vivo by numerous investigators 4–15…”

Section: Introductionmentioning

confidence: 99%

Enhanced Permeation of Methotrexate In Vitro by Ion Pair Formation With L-Arginine

Ivaturi

Kim

2009

Journal of Pharmaceutical Sciences

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Uptake of quaternary ammonium compounds into rat intestinal brush border membrane vesicles

Cited by 13 publications

References 12 publications

Transport Characteristics of Propantheline Across Rat Intestinal Brush Border Membrane

Transport Characteristics of Propantheline Across Rat Intestinal Brush Border Membrane

Pharmacological analysis of muscarinic receptors coupled to oxyntic cell secretion in the mouse stomach

Enhanced Permeation of Methotrexate In Vitro by Ion Pair Formation With L-Arginine

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