TY - JOUR
T1 - Opioid binding properties of the purified kappa receptor from human placenta
AU - Ahmed, Mahmoud S.
AU - Zhou, De he
AU - Cavinato, Anna G.
AU - Maulik, Dev
N1 - Funding Information:
This work was supported in part by NSF grant was a postdoctoral fellow supported by the same grant.
PY - 1989
Y1 - 1989
N2 - A glycoprotein with a molecular weight of 63,000 has been purified, in an active form, from human placental villus tissue membranes. The binding properties of this glycoprotein to opioid alkaloids and peptides indicates that it is the kappa opiate receptor of human placenta. The receptor binds the tritiated ligands etorphine, bremazocine, ethylketocyclazocine and naloxone specifically and reversibly with Kd values of 3.3, 4.4, 5.1 and 7.0nM, respectively. The binding of 3H-Bremazocine to the purified receptor is inhibited by the following compounds with the corresponding Ki values EKC, 1.3×10-8M; Dynorphin 1-8, 3.03×10-7; U50,488H, 4.48×10-9; U69-593, 2.28×10-8, morphine, 4.05×10-6 DADLE, 6.47×10-6 and naloxone, 2.64×10-8. The purified receptor binds 8 nmole of 3H-Etorphine and 1.7 nmole 3H-BZC per mg protein. The theoretical binding capacity of a protein of this molecular weight is 15.8. Although the iodinated purified receptor appears by autoradiography as one band on SDS-PAGE, yet homogeneity of the preparation is not claimed.
AB - A glycoprotein with a molecular weight of 63,000 has been purified, in an active form, from human placental villus tissue membranes. The binding properties of this glycoprotein to opioid alkaloids and peptides indicates that it is the kappa opiate receptor of human placenta. The receptor binds the tritiated ligands etorphine, bremazocine, ethylketocyclazocine and naloxone specifically and reversibly with Kd values of 3.3, 4.4, 5.1 and 7.0nM, respectively. The binding of 3H-Bremazocine to the purified receptor is inhibited by the following compounds with the corresponding Ki values EKC, 1.3×10-8M; Dynorphin 1-8, 3.03×10-7; U50,488H, 4.48×10-9; U69-593, 2.28×10-8, morphine, 4.05×10-6 DADLE, 6.47×10-6 and naloxone, 2.64×10-8. The purified receptor binds 8 nmole of 3H-Etorphine and 1.7 nmole 3H-BZC per mg protein. The theoretical binding capacity of a protein of this molecular weight is 15.8. Although the iodinated purified receptor appears by autoradiography as one band on SDS-PAGE, yet homogeneity of the preparation is not claimed.
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U2 - 10.1016/0024-3205(89)90586-9
DO - 10.1016/0024-3205(89)90586-9
M3 - Article
C2 - 2538693
AN - SCOPUS:0024520722
SN - 0024-3205
VL - 44
SP - 861
EP - 871
JO - Life Sciences
JF - Life Sciences
IS - 13
ER -