Skip to main content
OSTI.GOVU.S. Department of Energy Office of Scientific and Technical Information
U.S. Department of Energy
Office of Scientific and Technical Information
 

Phorbol ester-mediated desensitization of histamine Hl receptors on a cultured smooth muscle cell line

Journal Article · · Life Sci.; (United States)
;
The present study was undertaken in order to examine the effect of protein kinase C (PKC) on histamine Hl receptors, (HlR) present on the smooth muscle cell line, DDT/sub 1/MF-2. (/sup 3/H)-pyrilamine binding revealed that specific (/sup 3/H)-pyrilamine binding sites were reduced be pretreatment with 12-O-tetra-decanoylphorbol-13-acetate (TPA), an activator of PKC, but not the Kd. The TPA analogue, 4..cap alpha.. phorbol 12,13-didecanoate, which does not activate PKC, failed to induce down-regulation of HlR. TPA-induced down regulation of HlR was inhibited by pretreatment with 1-(5-Isoquinilinesulfonyl)-2-methylpiperazine dihydrochloride (H-7), a PKC inhibitor, in a dose dependent manner. The H-7 analogue, H-8, which is a less potent inhibitor of PKC, but a potent inhibitor of cyclic nucleotide dependent protein kinase, had no effect on HlR. Moreover, treatment with TPA inhibited histamine-induced increases in (Ca/sup 2 +/)/sub i/ in cells loaded with the fluorescent indicator, indo-1. These data suggest that HlR in DDT/sub 1/MF-2 cells were functionally regulated by PKC.
Research Organization:
Univ. of California Medical Center, San Francisco (USA)
OSTI ID:
6686622
Journal Information:
Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 43:18; ISSN LIFSA
Country of Publication:
United States
Language:
English

Similar Records

Differential role of protein kinase C in desensitization of muscarinic receptor induced by phorbol esters and receptor agonists
Thesis/Dissertation · Sat Dec 31 23:00:00 EST 1988 · OSTI ID:6612860
The regulation of GRP78 and messenger RNA levels by hypoxia is modulated by protein kinase C activators and inhibitors
Journal Article · Thu Mar 31 23:00:00 EST 1994 · Radiation Research · OSTI ID:56768
Effects of protein kinase C activators on germinal vesicle breakdown and polar body emission of mouse oocytes
Journal Article · Tue Dec 31 23:00:00 EST 1985 · Exp. Cell Res.; (United States) · OSTI ID:5784820

Related Subjects

550201 -- Biochemistry-- Tracer Techniques
560300* -- Chemicals Metabolism & Toxicology
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AMINES
AZOLES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
CARCINOGENS
CELL CULTURES
DOSE-RESPONSE RELATIONSHIPS
ENZYME INHIBITORS
ENZYMES
ESTERS
HETEROCYCLIC COMPOUNDS
HISTAMINE
IMIDAZOLES
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MEMBRANE PROTEINS
MUSCLES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PHORBOL ESTERS
PHOSPHORUS-GROUP TRANSFERASES
PHOSPHOTRANSFERASES
PROTEINS
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRANSFERASES
TRITIUM COMPOUNDS