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Chemicals and Drugs

UT GSBS Dissertations and Theses (Open Access)

Drug partial agonism

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Modelling Β2ar Regulation, Sharat J. Vayttaden Dec 2011

Modelling Β2ar Regulation, Sharat J. Vayttaden

UT GSBS Dissertations and Theses (Open Access)

The β2 adrenergic receptor (β2AR) regulates smooth muscle relaxation in the vasculature and airways. Long- and Short-acting β-agonists (LABAs/SABAs) are widely used in treatment of chronic obstructive pulmonary disorder (COPD) and asthma. Despite their widespread clinical use we do not understand well the dominant β2AR regulatory pathways that are stimulated during therapy and bring about tachyphylaxis, which is the loss of drug effects. Thus, an understanding of how the β2AR responds to various β-agonists is crucial to their rational use. Towards that end we have developed deterministic models that explore the mechanism of drug- induced β2AR regulation. These mathematical ...