Biochemical and pharmacological characterization of the thyrotropin releasing hormone (TRH) receptor from clonal GH sub 4 C sub 1 pituitary cells
The effect of drugs with anesthetic properties on the activity of the pituitary thyrotropin-releasing hormone (TRH) receptor was determined in the clonal GH{sub 4}C{sub 1} somatomammotropic cell line. Classic local anesthetics and other drugs with anesthetic activity inhibited binding of ({sup 3}H)methyl-TRH to cell receptors at concentrations known to produce anesthetic effects on the membrane. The inhibition of TRH receptor binding by tetracaine was competitive and temperature and pH dependent. Verapamil and tetracaine inhibited TRH-stimulated prolactin secretion at concentrations that inhibited peptide binding. TRH-stimulated prolactin secretion was equivalent with or without Ca{sup 2+} channel activity. Verapamil and tetracaine also inhibited basal prolactin and secretion stimulated by drugs that bypass membrane receptors, db-cAMP and TPA. These results indicate that inhibition of TRH binding and responses by diverse drugs results from an anesthetic effect on the cell membrane.
- Research Organization:
- Rochester Univ., NY (USA)
- OSTI ID:
- 5565826
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
59 BASIC BIOLOGICAL SCIENCES
ANESTHETICS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
BODY
CELL CONSTITUENTS
CELL CULTURES
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM DEPRESSANTS
CHEMICAL COMPOSITION
CLONE CELLS
DRUGS
ENDOCRINE GLANDS
GLANDS
GONADOTROPINS
HORMONES
HYDROGEN COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
KINETICS
LTH
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
ORGANS
PEPTIDE HORMONES
PITUITARY GLAND
PITUITARY HORMONES
PROTEINS
REACTION KINETICS
RECEPTORS
SECRETION
TRACER TECHNIQUES
TRH
TRITIUM COMPOUNDS