Molecular and structural requirements of the ß1L-adrenoceptor

Klenowski, Paul Mark (2012) Molecular and structural requirements of the ß1L-adrenoceptor. PhD thesis, Queensland University of Technology.


Noradrenaline which occurs naturally in the body binds to beta-adrenoceptors on the heart, causing the heart to beat faster and with greater force in response to increased demand. This enables the heart to provide oxygenated blood to vital organs. Prolonged overstimulation by noradrenaline can be harmful to the heart and lead to the progression of heart disease. In these circumstances beta-adrenoceptors are blocked with drugs called beta-blockers. Beta-blockers block the effects of noradrenaline by binding to the same site on the beta-adrenoceptor. Some beta-blockers such as CGP12177 can also cause increases in heart rate. Therefore it was proposed that CGP12177 could bind in a different place to noradrenaline. The aim of this study was to determine where CGP12177 binds to on the beta-adrenoceptor. The results have revealed a separate binding site named beta-1-low. These results may lead to the development of improved -blockers for the management of heart conditions.

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ID Code: 57327
Item Type: QUT Thesis (PhD)
Supervisor: Molenaar, Peter & Semmler, Annalese
Keywords: affinity, agonist, antagonist, ß1l-adrenoceptor, ß1h-adrenoceptor, ß2-adrenoceptor, ß3-adrenoceptor, ß-blocker, (-)-bupranolol, cardiostimulation, cardiovascular, catecholamines, (-)-CGP 12177, (-)-[3h]- CGP 12177, chimera, contractility, crystal structure, cyclic AMP, G-protein coupled receptor, heterologous, human atrial force, human heart failure, (-)-isoprenaline, L-748,337, ligand, low-affinity binding site, L-type Ca2 channel, molecular modelling, non-conventional partial agonists, noradrenaline, pindolol, positive inotropic effect, potency, radioligand binding, recombinant, site-directed mutagenesis, transmembrane domain
Divisions: Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Institution: Queensland University of Technology
Deposited On: 15 Feb 2013 07:27
Last Modified: 03 Nov 2015 01:42

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