Conversely, when bitopic linker-A ligands were compared in D2R, PF S,S -A, and SM-A showed no potency difference; whereas in D3R, PF S,S -A showed 13–35-fold greater potency than SM-A (except D3R-βarr1). When evaluating other bitopic PF vs SM pairs of identical linkers in D2R, bitopic PF ligands generally showed a trend of lower potency compared to their specific linker pair from SM series (except for more potent PF S,S -D S,R over SM-D S,R ).
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Linkers in Bitopic Agonists Shape Bias Profile among Transducers for the Dopamine D2 and D3 Receptors.
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