Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 3 of 3 for “"orthosteric agonists"”.
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Synthesis of fluorinated cannabinoid derivatives; Towards PET radiotracers for imaging the cannabinoid receptor
… psychotropic effects associated with CB1R orthosteric agonists remain a challenge to the development of novel cannabinoid-derived therapeutics leading to the development of GAT211 as CB1R-positive allosteric modulators (PAMs)5,6. In the second part of this project, we embarked on modifying …
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Characterising the conformational dynamics of β₁-adrenergic receptor activation and G protein coupling
… activity. Stimulation by agonist binding into an orthosteric pocket induces conformational changes in a highly interconnected allosteric activation network which enables coupling to intracellular signalling partners, including selective coupling to specific G protein α-subtypes. Investigations in …
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An Investigation into the pharmacology of the ghrelin receptor
… and L-692,429 were reported to act both as co-agonists (increasing the efficacy of the ghrelin response) and as negative or positive (respectively) regulators of the potency of ghrelin. This study sought to investigate the pharmacology of the GRLN-R through the Gai/o pathway. [35S]GTPyS binding …