TY - JOUR
T1 - β-Adrenergic Receptors
AU - Atlas, Daphne
PY - 1977/1/1
Y1 - 1977/1/1
N2 - Recently, successful experiments on the probing of β-adrenergic receptors using radioactive reversible β-antagonists possessing high affinity such as propranolol, alprenolol, chloropractolol, and hydroxybenzylpindoloF have been reported. The binding studies have made it possible to calculate a turnover number for the hormone-stimulated adenylate cyclase. However, additional understanding as to the molecular organization of the hormone-receptor-enzyme complex in the merebrane can be tremendously advanced by developing a ligand that can bind covalently at the receptor site. A covalent affinity label for the β-receptor can become a powerful technique for the identification, characterization, and, it is hoped, the isolation of the fl-receptor. Solubilization of the β-receptor adenylate cyclase complex causes the loss of the responsiveness of the enzyme. Thus the ability to monitor the receptor by activity measurements in its solubilized state is lost. A radioactive affinity label for the β-receptor can provide one with a specific marker for the receptor even subsequent to solubilization. The chapter explains synthetic procedures of Epinephrine Derivative, Bromopractolol and Propranolol Analogs.
AB - Recently, successful experiments on the probing of β-adrenergic receptors using radioactive reversible β-antagonists possessing high affinity such as propranolol, alprenolol, chloropractolol, and hydroxybenzylpindoloF have been reported. The binding studies have made it possible to calculate a turnover number for the hormone-stimulated adenylate cyclase. However, additional understanding as to the molecular organization of the hormone-receptor-enzyme complex in the merebrane can be tremendously advanced by developing a ligand that can bind covalently at the receptor site. A covalent affinity label for the β-receptor can become a powerful technique for the identification, characterization, and, it is hoped, the isolation of the fl-receptor. Solubilization of the β-receptor adenylate cyclase complex causes the loss of the responsiveness of the enzyme. Thus the ability to monitor the receptor by activity measurements in its solubilized state is lost. A radioactive affinity label for the β-receptor can provide one with a specific marker for the receptor even subsequent to solubilization. The chapter explains synthetic procedures of Epinephrine Derivative, Bromopractolol and Propranolol Analogs.
UR - http://www.scopus.com/inward/record.url?scp=0017347271&partnerID=8YFLogxK
U2 - 10.1016/S0076-6879(77)46073-7
DO - 10.1016/S0076-6879(77)46073-7
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C2 - 198633
AN - SCOPUS:0017347271
SN - 0076-6879
VL - 46
SP - 591
EP - 601
JO - Methods in Enzymology
JF - Methods in Enzymology
IS - C
ER -