PMID: 3746302Oct 1, 1986Paper

Characterization of xylamine binding to proteins of PC12 pheochromocytoma cells

Journal of Neurochemistry
M KoideB D Howard

Abstract

PC12 pheochromocytoma cells take up 3,4-dihydroxyphenylethylamine (dopamine) and norepinephrine by a Na+-dependent, cocaine-sensitive system. The kinetics suggest that the same transporter functions for both substrates. Xylamine, a nitrogen mustard that blocks catecholamine uptake into neurons, irreversibly inhibited norepinephrine uptake into PC12 (IC50 = 15 microM). Pretreatment with 10 microM xylamine did not inhibit norepinephrine transport if 10 microM cocaine or 100 microM norepinephrine was also present during the pretreatment period or if Na+ was absent. These results indicate that xylamine must interact with the norepinephrine transporter to inhibit norepinephrine uptake. PC12 accumulated [3H]xylamine; this uptake had Na+-dependent and Na+-independent components. The Na+-dependent uptake was saturable (Km = 13 microM), and it was inhibited by cocaine (IC50 = 0.6 microM), desipramine (IC50 less than 1 nM), and norepinephrine (IC50 = 1 microM). Several proteins became prominently labeled when intact PC12 cells were incubated with [3H]xylamine; these proteins were enriched in a plasma membrane fraction and have molecular weights of 17,000, 24,000, 31,000, 33,000, 41,000, 42,000, 52,000, and 80,000. Other proteins were lab...Continue Reading

References

Nov 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·D Schubert, F G Klier
Apr 1, 1979·Journal of Medicinal Chemistry·R C KammererA K Cho
Jul 1, 1976·Proceedings of the National Academy of Sciences of the United States of America·L A Greene, A S Tischler
Aug 15, 1975·European Journal of Biochemistry·R A Laskey, A D Mills
Oct 1, 1986·Journal of Neurochemistry·C M BitlerB D Howard
Feb 1, 1968·Proceedings of the National Academy of Sciences of the United States of America·K BrewR L Hill
May 15, 1970·Science·C H Suelter
Jul 21, 1981·Biochemistry·W P Melega, B D Howard
Sep 1, 1971·The Journal of Membrane Biology·D M Brunette, J E Till

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Citations

Oct 1, 1986·Journal of Neurochemistry·C M BitlerB D Howard
Oct 20, 2009·Naunyn-Schmiedeberg's Archives of Pharmacology·Birger Wenge, Heinz Bönisch
Jun 1, 1990·Journal of Neuroscience Research·B D HowardS Lin
Mar 12, 1998·Brain Research. Molecular Brain Research·M BrüssH Bönisch
Jul 9, 2002·Brain Research. Developmental Brain Research·Shuang ZhengBruce D Howard

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