Expression of the human beta-2 adrenergic receptor in mammalian cells

Conference · Fri May 01 04:00:00 EDT 1987 · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)

OSTI ID:6028664

Register, R B; Strader, C D; Sigal, I S; Rands, E; Candelore, M R; Dixon, R A.F.

The gene encoding the human beta-adrenergic receptor (BAR) was expressed in mammalian cells and the binding properties of the expressed protein examined. The human BAR could be expressed at high levels in mammalian cells and was able to mediate the stimulation of adenylate cyclase when expressed in a stable cell line. The expressed receptor was found to bind the radiolabeled antagonist /sup 125/I-cyano-pindolol with a high affinity, comparable to that observed for native receptor in a variety of systems and to the hamster cloned BAR expressed in the same cells. The pharmacology of the receptor was investigated in membranes prepared from the cells. Agonist competition binding showed the human BAR to be of the beta-2 subtype, with isoproterenol > epinephrine > norepinephrine in binding to the receptor. EC50 values for the three agonists were 0.2 ..mu..M, 1 ..mu..M, and 10 ..mu..M, respectively. This is in agreement with their findings for the cloned BAR from hamster, which shares sequence homology with the human protein.

• Research Organization: Merck Sharp and Dohme Research Labs., West Point, PA
• OSTI ID: 6028664
• Report Number(s): CONF-870644-
• Conference Information: Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Journal Volume: 46:6
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMAL CELLS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CELL CONSTITUENTS
CELL MEMBRANES
CYCLASES
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENZYMES
GENE REGULATION
GENES
HAMSTERS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LYASES
MAMMALS
MAN
MEMBRANE PROTEINS
MEMBRANES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PRIMATES
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RECEPTORS
RODENTS
SYMPATHOMIMETICS
TRACER TECHNIQUES
VERTEBRATES