The region in the μ opioid receptor conferring selectivity for sufentanil over the δ receptor is different from that over the κ receptor

We determined the binding domains of sufentanil and lofentanil in the μ opioid receptor by comparing their binding affinities to seven μ/δ and six μ/κ chimeric receptors with those to μ, δ and κ opioid receptors. TMHs 6 and 7 and the e3 loop of the μ opioid receptor were important for selective bind...

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Veröffentlicht in:	FEBS letters 1996-04, Vol.384 (2), p.198-202
Hauptverfasser:	Zhu, Jinmin, Xue, Ji-Chun, Law, Ping-Yee, Claude, Patricia A., Luo, Lai-Yi, Yin, Jinling, Chen, Chongguang, Liu-Chen, Lee-Yuan
Format:	Artikel
Sprache:	eng
Schlagworte:	aa, amino acid Animals Binding Sites Binding, Competitive Chimeric receptor CHO Cells CHO cells, Chinese hamster ovary cells Cricetinae DAMGO, [d-Ala,MePhe4,Gly(ol)5]enkephalin Diprenorphine - metabolism e1 loop, the first extracellular loop e3 loop, the third extracellular loop Fentanyl - analogs & derivatives Fentanyl - metabolism Kinetics Lofentanil Opioid receptor Protein Binding Rats Receptors, Opioid, delta - chemistry Receptors, Opioid, delta - metabolism Receptors, Opioid, kappa - chemistry Receptors, Opioid, kappa - metabolism Receptors, Opioid, mu - chemistry Receptors, Opioid, mu - metabolism Recombinant Fusion Proteins - metabolism Structure-Activity Relationship Structure-function relationship Substrate Specificity Sufentanil Sufentanil - metabolism SUPERFIT, cis-(+)-3-methylfentanyl isothiocyanate TMH, transmembrane helix
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