title: [Binding characteristics of new synthesized opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell].
abstract: OBJECTIVE
  To determine the affinity of new opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell.
  
  
  METHODS
  The binding characteristics of the opioid ligand [3H] diprenorphine (3H-dip) were studied by cellular biological techniques and radioligands binding in cloned mu opioid receptors stably expressed in CHO cells in saturation binding experiments, and were followed by competition binding experiments with a variety of new synthesized opioid receptor ligands.
  
  
  RESULTS
  The Kd and Bmax of [3H] diprenorphine bound to mu receptors were 1.06 nmol/L and 930 fmol/mg protein, respectively. Competition binding experiments revealed that ligand 3# and 12# displayed much higher affinity than DAMGO and Morphine for the cloned mu opioid receptor. However, the affinities of ligands 2#, 6#, 8# and 9# were lower than DAMGO and Morphine.
  
  
  CONCLUSIONS
  The present results suggest that the new ligands 3# and 12# have higher affinity to mu opioid receptors. However, ligands 2#, 6#, 8# and 9# have lower affinity to mu opioid receptors.
authors.affiliation: Department of Pharmacology, Institute of Basic Medical Sciences, CAMS, PUMC, Beijing 100005, China.
authors.forename: Ping
authors.initials: P
authors.lastname: Hu
authors.forename: Cai-ying
authors.initials: CY
authors.lastname: Ye
authors.forename: Zhui-bai
authors.initials: ZB
authors.lastname: Qiu
authors.forename: Hui-fen
authors.initials: HF
authors.lastname: Yang
authors.forename: De-chang
authors.initials: DC
authors.lastname: Zhang
mesh_terms: D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D016466:CHO Cells / Q000378:metabolism; D003001:Cloning, Molecular; D006224:Cricetinae; D004174:Diprenorphine / Q000494:pharmacology; D008024:Ligands; D017450:Receptors, Opioid, mu / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism*
chemical_list: D008024:Ligands; D017450:Receptors, Opioid, mu; D004174:Diprenorphine