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
- Resource Relation:
- Other Information: Thesis (Ph. D.)
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
ANESTHETICS
BIOLOGICAL EFFECTS
RECEPTORS
CHEMICAL COMPOSITION
TRH
BIOCHEMICAL REACTION KINETICS
CELL MEMBRANES
CLONE CELLS
INHIBITION
LTH
PITUITARY GLAND
SECRETION
TRACER TECHNIQUES
TRITIUM COMPOUNDS
BODY
CELL CONSTITUENTS
CELL CULTURES
CENTRAL NERVOUS SYSTEM DEPRESSANTS
DRUGS
ENDOCRINE GLANDS
GLANDS
GONADOTROPINS
HORMONES
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
ORGANS
PEPTIDE HORMONES
PITUITARY HORMONES
PROTEINS
REACTION KINETICS
550201* - Biochemistry- Tracer Techniques