H/sub 1/-histamine receptors regulate phosphoinositide hydrolysis in human astrocytoma cells
Activation of H/sub 1/-histamine receptors on 1321N1 human astrocytoma cells resulted in a rapid formation of the inositol phosphates (InsP), IP/sub 3/, IP/sub 2/, and IP/sub 1/. Histamine-induced mobilization of Ca/sup + +/ and stimulated of a Ca/sup + +/ calmodulin-regulated phosphodiesterase occurred concurrently with histamine-stimulated InsP formation. The K/sub 0.5/ values for histamine for activation of phosphodiesterase, mobilization of Ca/sup + +/, and stimulation of InsP formation were 3,4, and 10 ..mu..M, respectively. The K/sub i/ for histamine determined in competition binding experiments with the H/sub 1/-receptor antagonist, /sup 3/H-mepyramine, was 11 ..mu..M. As with muscarinic receptor-mediated effects in these cells, inactivation of G/sub i/ with pertussis toxin had no effect on H/sub 1/-receptor mediated responses. Both histamine and muscarinic receptor stimulation resulted in the formation of Ins 1,4,5P/sub 3/ and Ins 1,3,4P/sub 3/. In contrast to muscarinic receptor stimulation, which results in a linear accumulation of InsP for greater than 30 min, histamine-stimulated formation of InsP rapidly desensitized.
- Research Organization:
- Univ. of North Carolina School of Medicine, Chapel Hill
- OSTI ID:
- 6991847
- Report Number(s):
- CONF-8604222-
- Journal Information:
- Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Vol. 45:4; Conference: 70. annual meeting of the Federation of American Society for Experimental Biology, St. Louis, MO, USA, 13 Apr 1986
- Country of Publication:
- United States
- Language:
- English
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HISTAMINE
RECEPTORS
PHOSPHODIESTERASES
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PHOSPHOLIPIDS
HYDROLYSIS
CALCIUM COMPOUNDS
CATIONS
MAN
TRACER TECHNIQUES
TRITIUM COMPOUNDS
TUMOR CELLS
ALKALINE EARTH METAL COMPOUNDS
AMINES
ANIMAL CELLS
ANIMALS
AZOLES
CHARGED PARTICLES
CHEMICAL REACTIONS
DECOMPOSITION
ENZYMES
ESTERASES
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HETEROCYCLIC COMPOUNDS
HYDROLASES
IMIDAZOLES
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LABELLED COMPOUNDS
LIPIDS
LYSIS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
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PRIMATES
PROTEINS
SOLVOLYSIS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques