Probing the opioid receptor complex with (+)-trans-SUPERFIT. II. Evidence that μ ligands are noncompetitive inhibitors of the δcx opioid peptide binding site

Studies of the Biogenic Amine Transporters. 14. Identification of Low-Efficacy “Partial” Substrates for the Biogenic Amine Transporters

“…The data of three independent experiments were pooled and fit to one-and two-component dissociation models by using MLAB-PC as described elsewhere (Rothman et al, 1991). Graphs were generated with KaleidaGraph 3.6 software.…”

Molecular Pharmacology of δ-Opioid Receptors

“…Being allosteric proteins, receptors are not conformationally unique but rather exist in a multiplicity of states that are partly determined by their interaction with natural allosteric modulators (e.g., Na + ions) (Fenalti et al, 2014) as well as other membrane (e.g., other receptors, effectors) and/ or cytosolic proteins (e.g., signaling partners, regulatory proteins) (Kenakin and Miller, 2010). Based on such allosteric properties, interactions of the receptor with other cellular proteins were earlier considered as plausible explanations of the observed diversity, with the DOPr1 subtype being correlated with noncomplexed receptors, whereas DOPr2 was considered the result of DOPr association with other receptors of unknown type (Vaught et al, 1982;Schoffelmeer et al, 1988a,b;Rothman et al, 1992;Cha et al, 1995). More recently, the actual observation that DOPr dimerization with other receptors could change DOPr pharmacology (George et al, 2000;Gomes et al, 2001;Levac et al, 2002;Fan et al, 2005;Hasbi et al, 2007;Rozenfeld and Devi, 2007;Fujita et al, 2015) lent further support to this hypothesis (van Rijn et al, 2010(van Rijn et al, , 2013.…”

Salvinorin A: Allosteric Interactions at the μ-Opioid Receptor

“…For binding surface experiments (Rothman, 1986;Rothman et al, 1991), two different concentrations of radioligand were each displaced by ten concentrations of nonradioactive ligand agents in the absence or presence of various blockers.…”