Rapid desensitization and resensitization of 5-HT sub 2 receptor mediated phosphatidyl inositol hydrolysis by serotonin agonists in quiescent calf aortic smooth muscle cells

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(90)90435-T· OSTI ID:6291700

Pauwels, P J; Van Gompel, P; Leysen, J E ^[1]

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1. Janssen Research Foundation, Beerse (Belgium)

Agonist regulation of 5-hydroxytryptamine{sub 2} (5-HT{sub 2}) receptors was studied in calf aortic smooth muscle cultures incubated in a quiescent, defined synthetic medium that does not stimulate cell proliferation, but that provides cells with supplements that maintain cell viability. In these cells, 5-hydroxytryptamine (5-HT)-induced ({sup 3}H)inositol phosphates accumulation showed the characteristics of a 5-HT{sub 2} receptor coupled transducing system according to the inhibition of the response by 5-HT{sub 2} antagonists at nanomolar concentrations. The 5-HT{sub 2} receptor coupled response became rapidly desensitized during continued incubation with 5-HT and 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM); nearly full desensitization was obtained in two hours with 10 {mu}M 5-HT and DOM pretreatment. The recovery of the response had a half-live of 5 hours after 2 hours pretreatment and of 9.5 to 12.5 hours after 24 to 96 hours agonist pretreatment. The DOM-induced desensitization of the 5-HT{sub 2} receptor coupled response was fully blocked by 0.1 {mu}M cinanserin. Cinanserin alone did not induce desensitization or up-regulation of the 5-HT{sub 2} receptor coupled response at 0.1 {mu}M.

• OSTI ID: 6291700
• Journal Information: Life Sciences; (USA), Vol. 47:22; ISSN 0024-3205
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
PHOSPHOLIPIDS
METABOLISM
SEROTONIN
RECEPTORS
ANIMAL CELLS
AORTA
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL HALF-LIFE
CALVES
CELL PROLIFERATION
IN VITRO
INOSITOL
MUSCLES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
AMINES
ANIMALS
AROMATICS
ARTERIES
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BLOOD VESSELS
BODY
CARBOHYDRATES
CARDIOVASCULAR SYSTEM
CATTLE
DOMESTIC ANIMALS
DRUGS
ESTERS
HETEROCYCLIC COMPOUNDS
HYDROGEN COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
INOSITOLS
ISOTOPE APPLICATIONS
KINETICS
LIPIDS
MAMMALS
MEMBRANE PROTEINS
MONOSACCHARIDES
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
ORGANS
PROTEINS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
REACTION KINETICS
RUMINANTS
SACCHARIDES
SYMPATHOMIMETICS
TRYPTAMINES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques