Rapid communicationδ-Opioid receptor: the third extracellular loop determines naltrindole selectivity
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2007, Biochemical PharmacologyCitation Excerpt :Three point mutations in the α1B-AR (Gly196Gln, Val197Ile, Thr198Asn) were additive in increasing affinity for phentolamine and WB4101 to those at the α1A-AR (Fig. 5). Similar results on the role of the second extracellular loop on antagonist binding were also obtained for the 5-HT1D receptor [72], the opioid receptor [73] and the dopamine D2 receptor [74], suggesting that GPCRs in general may make use of extracellular loop 2 in antagonist binding. These observations indicate that, in contrast to agonist binding, which is localized closer to the interior core of the receptor, antagonists interact with residues closer to the extracellular surface of adrenergic receptors, above the plane of the agonist-binding pocket.
The delta opioid receptor
2013, ACS Symposium Series
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