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Tamoxifen aziridine, a novel affinity probe for P-glycoprotein in multidrug resistant cells.
Biochem Biophys Res Commun
July 1994
Department of Medicine, University of Chicago, IL 60637.
In this study for the first time we used an electrophilic analog of tamoxifen, [3H]tamoxifen aziridine, and demonstrated that it covalently and specifically binds to P-glycoprotein in multidrug resistant cells. Tamoxifen and its metabolites, N-desmethyltamoxifen and 4-hydroxytamoxifen, were potent inhibitors of [3H]tamoxifen aziridine binding to P-glycoprotein with 4-hydroxytamoxifen > tamoxifen > N-desmethyltamoxifen. The multidrug resistance-related drugs inhibited [3H]tamoxifen aziridine binding with vinblastine > vincristine > doxorubicin > actinomycin D, while colchicine enhanced the binding.
View Article and Find Full Text PDFPotent, extra-channel influence of several calcium-channel modulators on striatal binding of [3H]tyramine.
Neurochem Res
November 1993
Department of Neuroscience B. Brodie, Cagliari, Italy.
A number of Ca(2+)-, K(+)-, and Na(+)-channel modulators has been tested with respect to their effects on [3H]tyramine (TY) binding, as a putative marker for the vesicular dopamine (DA) transporter in striatal membrane preparations containing vesicle ghosts. Among organic Ca(2+)-channel modulators, the diphenylalkylamines tested consistently inhibited TY binding: the order of potency was prenylamine > lidoflazine > flunarizine > cinnarizine, with Ki values of 0.1, 0.
View Article and Find Full Text PDFThe tyramine binding site in the central nervous system: an overview.
Neurochem Res
August 1993
Department of Neuroscience, B. Brodie, Cagliari, Italy.
The [3H]Tyramine (TY) binding site is proposed as a high affinity marker of the membrane carrier for dopamine (DA) in synaptic vesicles from DA-rich brain regions. Under precise assay conditions, there is neither a consistent association of TY with the neuronal, cocaine-sensitive DA transporter, nor with mitochondrial or microsomal targets. TY-labeled sites have a high affinity for selected toxins such as the Parkinsonian agent MPP+ (1-methyl-4-phenylpyridinium ion), or drugs such as diphenylalkylamine Ca(2+)-channel antagonists.
View Article and Find Full Text PDFThe alpha 1-adrenergic photoaffinity probe [125I]arylazidoprazosin binds to a specific peptide of P-glycoprotein in multidrug-resistant cells.
Biochem Biophys Res Commun
January 1990
Department of Medicine, University of Chicago, Pritzker School of Medicine, IL 60637.
Much evidence suggests that P-glycoprotein (P-gp) confers multidrug-resistance (MDR) in tumor cells by energy-dependent efflux of hydrophobic cytotoxic agents. In this study, we have used the alpha 1-adrenergic photoaffinity probe, [125I]arylazidoprazosin ([125I]AAP), and identified P-gp as a specific acceptor for prazosin. Drugs to which MDR cells are resistant, including vincristine, vinblastine, doxorubicin, actinomycin D and colchicine as well as agents reversing MDR, including verapamil, nicardipine, prenylamine, diltiazem, trifluoperazine, dibucaine, reserpine, monensin, and progesterone, differentially reduced [125I]AAP photolabeling of P-gp.
View Article and Find Full Text PDFAntidopaminergic action of verapamil and several other drugs: inactivation of vesicular dopamine.
Life Sci
May 1990
Nathan S. Kline Institute for Psychiatric Research, Orangeburg, New York 10962.
Verapamil was tested for its effect upon dopamine in striatal and olfactory tubercle synaptosomes (P2) in the presence of L-alpha-methyl p-tyrosine, an inhibitor added to block new amine formation. Verapamil significantly potentiated the decline of dopamine in a concentration dependent manner. Several other calcium channel associated drugs such as gallopamil, diltiazem, flunarizin and prenylamine, also enhanced the decline of dopamine.
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