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), Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Vol. 45:4; ISSN FEPRA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ALKALINE EARTH METAL COMPOUNDS
AMINES
ANIMAL CELLS
ANIMALS
AZOLES
CALCIUM COMPOUNDS
CATIONS
CHARGED PARTICLES
CHEMICAL REACTIONS
DECOMPOSITION
ENZYME ACTIVITY
ENZYMES
ESTERASES
ESTERS
HETEROCYCLIC COMPOUNDS
HISTAMINE
HYDROLASES
HYDROLYSIS
IMIDAZOLES
IONS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIPIDS
LYSIS
MAMMALS
MAN
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
PHOSPHODIESTERASES
PHOSPHOLIPIDS
PRIMATES
PROTEINS
RECEPTORS
SOLVOLYSIS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
TUMOR CELLS
VERTEBRATES