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Orthosteric/Allosteric Bitopic Ligands
Figure 1.
Some examples of bivalent orthosteric GPCR ligands. Structures are shown for (A) a homobivalent muscarinic receptor agonist; (B) a homobivalent serotonin receptor agonist; (C) a δ/κ opioid heterodimer–selective agonist; and (D) a heterobivalent dimer-selective antagonist. The inset shows that 6′-GNTI has higher efficacy for promoting intracellular calcium mobilization in HEK cells containing the δ/κ heterodimer over cells individually expressing either the δ or κ opioid receptor. Data replotted from (22).
