Phencyclidine inhibition of the acetylcholine receptor: measurement of cation flux in a sympathetic neuronal cell line using 22Na+ and spectroscopic detection of Cs+.
Sachs, A. B.; Leprince, Pierre; Karpen, J. W.et al.
1983 • In Archives of Biochemistry and Biophysics, 225 (2), p. 500-4
[en] The site of action of phencyclidine, a powerful and increasingly abused drug, in sympathetic nerve cells has not previously been identified. Here it is demonstrated that phencyclidine is a powerful, noncompetitive inhibitor of the nicotinic acetylcholine receptor in a sympathetic nerve cell line, PC-12. In the presence of 1 mM carbamoylcholine the rate of the receptor-controlled influx of 22Na+ is reduced by a factor of 2 by 0.7 microM phencyclidine. Increasing concentrations of carbamoylcholine cannot reverse the inhibitory effect of the drug. Both the transmission of electrical signals between nerve cells and the secretion of catecholamines in the PC-12 cell line depend on the receptor-controlled ion flux. Thus phencyclidine interferes with at least two specific, physiologically important functions of these nerve cells. A new spectroscopic method has been developed to measure cation flux in cells. It is shown that this method can replace measurements of tracer ion flux.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Sachs, A. B.
Leprince, Pierre ; Université de Liège - ULiège > CNCM/ Centre fac. de rech. en neurobiologie cell. et moléc.
Karpen, J. W.
Pasquale, E. B.
Abood, L. G.
Hess, G. P.
Language :
English
Title :
Phencyclidine inhibition of the acetylcholine receptor: measurement of cation flux in a sympathetic neuronal cell line using 22Na+ and spectroscopic detection of Cs+.
Publication date :
1983
Journal title :
Archives of Biochemistry and Biophysics
ISSN :
0003-9861
eISSN :
1096-0384
Publisher :
Academic Press, New York, United States - New York
Hughes, Smith, Kosterlitz, Fothergill, Morgan Nature (London) 1975, 258:577-580.
Li, Chung Proc. Natl. Acad. Sci. USA , 3rd ed.; 1976, 73:1145-1148.
Vincent, Cavey, Kamenka, Geneste, Lazdunski Brain Res 1978, 152:176-182.
Vincent, Kartalovski, Geneste, Kamenka, Lazdunski Proc. Natl. Acad. Sci. USA , 3rd ed.; 1979, 76:4678-4682.
Zukin, Zukin Proc. Natl. Acad. Sci. USA , 3rd ed.; 1979, 76:5372-5376.
Quirion, Hammer, Herkenham, Pert Proc. Natl. Acad. Sci. USA , 3rd ed.; 1981, 78:5881-5885.
Albuquerque, Tsai, Aronstam, Witkop, Eldefrawi, Eldefrawi Proc. Natl. Acad. Sci. USA , 3rd ed.; 1980, 77:1224-1228.
Petersen, Stillman (1978) Phencyclidine (PCP) Abuse: An Appraisal. National Institute on Drug Abuse Research Monograph 21, 3rd ed.; .
Greene, Tischler Proc. Natl. Acad. Sci. USA , 3rd ed.; 1976, 73:2424-2428.
.
Stallcup, Patrick Proc. Natl. Acad. Sci. USA , 3rd ed.; 1980, 77:634-638.
Nakagawa, Ogura, Sakata, Kuritani (1973) Optically Active Triptycenes, V. Synthesis, Optical Resolution and Absolute Configuration of 2,7-Disubstituted Triptycenes. Bulletin of the Chemical Society of Japan 46:605-610.
Katz, Thesleff (1957) J. Physiol. (London). J. Physiol. (London) 138:63-80.
Hess, Cash, Aoshima (1979) Acetylcholine receptor-controlled ion fluxes in membrane vesicles investigated by fast reaction techniques. Nature 288:329-331.
Cash, Hess Proc. Natl. Acad. Sci. USA , 3rd ed.; 1980, 77:842-846.
Cash, Aoshima, Hess Proc. Natl. Acad. Sci. USA , 3rd ed.; 1981, 78:3318-3322.
Burgen, Spero (1968) The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of the guinea-pig intestine. British Journal of Pharmacology 34:99-115.