| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
|
|
|
|||||||
|
|||||||||
J. Biol. Chem., Vol. 258, Issue 6, 3496-3502, Mar, 1983
M Staehelin, P Simons, K Jaeggi and N Wigger
A new, hydrophilic beta-adrenergic receptor radioligand, (+/-)-[3H]CGP-
12177 (4-(3-tertiarybutylamino-2-hydroxypropoxy)-benzimidazole-2-on
hydrochloride), was synthesized and radiolabeled to 40 Ci/mmol. The
nonspecific binding of this compound to turkey erythrocyte ghosts and C6
glioma cell membranes was less than 5% of the total binding at five times
the appropriate KD. Binding assays of intact C6 glioma cells also showed
low nonspecific binding, less than 20% of the total binding at five times
the appropriate KD. The affinities of the antagonists (-)- and
(+)-propranolol as well as of the agonist (-)-isoproterenol were examined
by their potency to displace various radioligands from intact C6 glioma
cell and membrane preparations. With membrane preparations, both [3H]
CGP-12177 and [3H]dihydroalprenolol (DHA) were displaced stereospecifically
by the antagonists (-)- and (+)-propranolol and the agonist
(-)-isoproterenol. With whole cells, [3H]CGP-12177 and [3H]DHA behaved
differently. [3H]DHA and [3H]carazolol could be stereospecifically
displaced by antagonists but only partially displaced by agonists, while
[3H]CGP-12177 could be completely displaced by both antagonists and
agonists as in membranes. In contrast to [3H]CGP-12177, the lipophilic
ligand [3H]DHA is actually taken up by cells. The inability of agonists to
displace lipophilic radioligands from receptors on intact cells may not be
due to a low affinity of agonists for receptors on cells, but to an
agonist-induced change in the receptors which renders them inaccessible to
hydrophilic agonists and antagonists. This change is likely to be their
internalization into the cell.
CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells
CiteULike 
Complore 
Connotea 
Del.icio.us 
Digg 
Reddit 
Technorati What's this?
This article has been cited by other articles:
|
|
 |
|
  T. Tsukamoto, K. Morita, M. Naya, M. Inubushi, C. Katoh, K. Nishijima, Y. Kuge, H. Okamoto, H. Tsutsui, and N. Tamaki Decreased Myocardial {beta}-Adrenergic Receptor Density in Relation to Increased Sympathetic Tone in Patients with Nonischemic Cardiomyopathy J. Nucl. Med., November 1, 2007; 48(11): 1777 - 1782. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. G. Baker Site of Action of {beta}-Ligands at the Human {beta}1-Adrenoceptor J. Pharmacol. Exp. Ther., June 1, 2005; 313(3): 1163 - 1171. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 G. Cheng, F. Qiao, T. N. Gallien, D. Kuppuswamy, and G. Cooper IV Inhibition of {beta}-adrenergic receptor trafficking in adult cardiocytes by MAP4 decoration of microtubules Am J Physiol Heart Circ Physiol, March 1, 2005; 288(3): H1193 - H1202. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 A. Breit, M. Lagace, and M. Bouvier Hetero-oligomerization between {beta}2- and {beta}3-Adrenergic Receptors Generates a {beta}-Adrenergic Signaling Unit with Distinct Functional Properties J. Biol. Chem., July 2, 2004; 279(27): 28756 - 28765. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. A. Gardner, N. M. D. Santos, S. G. Matta, M. A. Whitt, and S. W. Bahouth Role of the Cyclic AMP-dependent Protein Kinase in Homologous Resensitization of the {beta}1-Adrenergic Receptor J. Biol. Chem., May 14, 2004; 279(20): 21135 - 21143. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P. C. Simons, S. M. Biggs, A. Waller, T. Foutz, D. F. Cimino, Q. Guo, R. R. Neubig, W.-J. Tang, E. R. Prossnitz, and L. A. Sklar Real-time Analysis of Ternary Complex on Particles: DIRECT EVIDENCE FOR PARTIAL AGONISM AT THE AGONIST-RECEPTOR-G PROTEIN COMPLEX ASSEMBLY STEP OF SIGNAL TRANSDUCTION J. Biol. Chem., April 2, 2004; 279(14): 13514 - 13521. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
V. Leblais, F. Pourageaud, M. D. Ivorra, C. Guibert, R. Marthan, and B. Muller Role of {alpha}-Adrenergic Receptors in the Effect of the {beta}-Adrenergic Receptor Ligands, CGP 12177, Bupranolol, and SR 59230A, on the Contraction of Rat Intrapulmonary Artery J. Pharmacol. Exp. Ther., April 1, 2004; 309(1): 137 - 145. [Abstract] [Full Text]
|
|
|
|
|
|
J. Jakubik, S. Tucek, and E. E. El-Fakahany Role of Receptor Protein and Membrane Lipids in Xanomeline Wash-Resistant Binding to Muscarinic M1 Receptors J. Pharmacol. Exp. Ther., January 1, 2004; 308(1): 105 - 110. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. Shi, G. Liapakis, R. Xu, F. Guarnieri, J. A. Ballesteros, and J. A. Javitch beta 2 Adrenergic Receptor Activation. MODULATION OF THE PROLINE KINK IN TRANSMEMBRANE 6 BY A ROTAMER TOGGLE SWITCH J. Biol. Chem., October 18, 2002; 277(43): 40989 - 40996. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Bundkirchen, K. Brixius, B. Bolck, and R. H. G. Schwinger Bucindolol Exerts Agonistic Activity on the Propranolol-Insensitive State of beta 1-Adrenoceptors in Human Myocardium J. Pharmacol. Exp. Ther., March 1, 2002; 300(3): 794 - 801. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Delforge, D. Mesangeau, F. Dolle, P. Merlet, C. Loc'h, M. Bottlaender, R. Trebossen, and A. Syrota In Vivo Quantification and Parametric Images of the Cardiac {beta}-Adrenergic Receptor Density J. Nucl. Med., February 1, 2002; 43(2): 215 - 226. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. G. Granneman The putative {beta}4-adrenergic receptor is a novel state of the {beta}1-adrenergic receptor Am J Physiol Endocrinol Metab, February 1, 2001; 280(2): E199 - E202. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Shan, R. J. Bick, B. J. Poindexter, S. F. Nagueh, S. Shimoni, M. S. Verani, F. Keng, M. J. Reardon, G. V. Letsou, J. F. Howell, et al. Altered Adrenergic Receptor Density in Myocardial Hibernation in Humans : A Possible Mechanism of Depressed Myocardial Function Circulation, November 21, 2000; 102(21): 2599 - 2606. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Shan, R. J. Bick, B. J. Poindexter, S. Shimoni, G. V. Letsou, M. J. Reardon, J. F. Howell, W. A. Zoghbi, and S. F. Nagueh Relation of tissue Doppler derived myocardial velocities to myocardial structure and beta-adrenergic receptor density in humans J. Am. Coll. Cardiol., September 1, 2000; 36(3): 891 - 896. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. A. Konkar, Z. Zhu, and J. G. Granneman Aryloxypropanolamine and Catecholamine Ligand Interactions with the beta 1-Adrenergic Receptor: Evidence for Interaction with Distinct Conformations of beta 1-Adrenergic Receptors J. Pharmacol. Exp. Ther., September 1, 2000; 294(3): 923 - 932. [Abstract] [Full Text]
|
|
|
|
 |
|
 A. A. Konkar, Y. Zhai, and J. G. Granneman beta 1-Adrenergic Receptors Mediate beta 3-Adrenergic-Independent Effects of CGP 12177 in Brown Adipose Tissue Mol. Pharmacol., February 1, 2000; 57(2): 252 - 258. [Abstract] [Full Text]
|
|
|
|
 |
|
 G. Bronnikov, T. Bengtsson, L. Kramarova, V. Golozoubova, B. Cannon, and J. Nedergaard {beta}1 to {beta}3 Switch in Control of Cyclic Adenosine Monophosphate during Brown Adipocyte Development Explains Distinct {beta}-Adrenoceptor Subtype Mediation of Proliferation and Differentiation Endocrinology, September 1, 1999; 140(9): 4185 - 4197. [Abstract] [Full Text]
|
|
|
|
 |
|
 K. Ohta, X.-P. Pang, L. Berg, and J. M. Hershman Growth Inhibition of New Human Thyroid Carcinoma Cell Lines by Activation of Adenylate Cyclase through the {beta}-Adrenergic Receptor J. Clin. Endocrinol. Metab., August 1, 1997; 82(8): 2633 - 2638. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. A. Javitch, D. Fu, G. Liapakis, and J. Chen Constitutive Activation of the beta 2 Adrenergic Receptor Alters the Orientation of Its Sixth Membrane-spanning Segment J. Biol. Chem., July 25, 1997; 272(30): 18546 - 18549. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. Moore, N Sadovnikoff, S Hoffenberg, S Liu, P Woodford, K Angelides, J. Trial, N. Carsrud, B. Dickey, and B. Knoll Ligand-stimulated beta 2-adrenergic receptor internalization via the constitutive endocytic pathway into rab5-containing endosomes J. Cell Sci., January 9, 1995; 108(9): 2983 - 2991. [Abstract] [PDF]
|
|
| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
| All ASBMB Journals | Molecular and Cellular Proteomics |
| Journal of Lipid Research | ASBMB Today |
