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Circe La Mache

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Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression - Nature Communications

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By Mark Wall, Emily Hill, Giuseppe Deganutti, Dewi Safitri, Wendy L. Imlach, Chris Reynolds Verified, Martin Lochner, Bruno G. Frenguelli, Robert Huckstepp, Michele Leuenberger, Circe La Mache, David Spanswick
| Nature Verified
Abstract The development of therapeutic agonists for G protein-coupled receptors (GPCRs) is hampered by the propensity of GPCRs to couple to multiple intracellular signalling pathways. This promiscuous coupling leads to numerous downstream cellular effects, some of which are therapeutically undesirable. This is especially the case for adenosine A1 receptors (A1Rs) whose clinical potential is undermined by the sedation and cardiorespiratory depression caused by conventional agonists.
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