Trends in Pharmacological Sciences
ViewpointIs there a third heart β-adrenoceptor?
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Cited by (187)
Evolution of β-blockers: From anti-anginal drugs to ligand-directed signalling
2011, Trends in Pharmacological SciencesCitation Excerpt :Following initial observations [107,108], most detailed observations have been for CGP12177A [109], but β-adrenoceptor antagonists with similar properties include oxprenolol, alprenolol, carazolol, pindolol and carvedilol. These ligands either stimulate agonist responses at concentrations much higher than those required to fully occupy and block the conventional catecholamine β1-adrenoceptor site, or have biphasic concentration–response curves [92,95,100,105,110,111]. Activation of this low-affinity state of the β1-adrenoceptor has been demonstrated in model cell systems [99,101,112], cardiomyocytes [113,114], tissues [115], whole animals [116,117] and humans [118].
The β<inf>3</inf>-adrenoceptor as a therapeutic target: Current perspectives
2009, Pharmacological ResearchEvaluation of β<inf>1L</inf>-adrenoceptors in rabbit heart by tissue segment binding assay
2009, Journal of Pharmacological SciencesComparison of the binding affinity of CGP-12177A at recombinant rat α<inf>1D</inf>-adrenoceptors expressed in BHK-21 cell membranes and α<inf>1</inf>-adrenoceptors present in rat cerebral cortex membranes
2008, European Journal of PharmacologyCitation Excerpt :CGP-12177A was also shown to be a partial agonist for the “putative β4-adrenoceptor” (Galitzky et al., 1997; Kaumann and Molenaar, 1997; Molenaar et al., 1997), which is, indeed, a different state or conformation of the β1-adrenoceptor, currently known as the low-affinity state of β1-adrenoceptors (Granneman, 2001; Konkar et al., 2000a,b). Therefore, CGP-12177A is referred to as a non conventional partial agonist, able to block β1- and β2-adrenoceptors at low (nano- or subnanomolar) concentrations, but activating them at considerably higher (2–3 log units) concentrations (Kaumann, 1989; Sarsero et al., 1998). CGP-12177A was an important tool in the identification of the low-affinity state of β1-adrenoceptors in cardiac tissue of different species (Lowe et al., 2002; Sarsero et al., 1998, 1999, 2003), and has been extensively used in an attempt to ascertain the presence of β3-adrenoceptors and/or of the low-affinity state of β1-adrenoceptors in other organs and tissues, such as blood vessels.
The low-affinity site of the β<inf>1</inf>-adrenoceptor and its relevance to cardiovascular pharmacology
2008, Pharmacology and TherapeuticsCitation Excerpt :Low blocking potencies of bupranolol and CGP20712. As found on other species (Kaumann, 1989) including man (Kaumann, 1996), CGP12177 also causes cardiostimulation at nanomolar concentrations on rat cardiac tissues (Kaumann & Molenaar, 1996; Malinowska & Schlicker, 1996, 1997; Sarsero et al., 1999) but vascular relaxation at micromolar concentrations (Brawley et al., 2000a 2000b; Koslowska et al., 2003; Mallem et al., 2004, 2005; Briones et al., 2005). The vascular relaxant potency of (±)-cyanopindolol (Brawley et al., 2000a,b; Kozlowska et al., 2003; Mallem et al., 2004, 2005) is also consistently lower than its cardiostimulant potency (Kaumann & Molenaar, 1996; Malinowska & Schlicker, 1996; Sarsero et al., 1999).