Opioid receptor binding properties of analgesic analogues of cholecystokinin octapeptide.
Four analogues of cholecystokinin (CCK) octapeptide having analgesic activity after i.c.v. administration and high affinity for CCK-B receptors were studied for their ability to displace specific ligands, [3H]D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2. [3H][D-Pen2, 4'-Cl-Phe4,D-Pen5]enkephalin and [3H]U-69,593, for mu-, delta- and kappa-opioid receptors, respectively. None of the analogues tested have high affinity for either mu- or kappa-receptors (IC50 values greater than 0.7 microM), but their IC50 values for delta-receptors range from 29 to 1023 nM. The results suggest a relationship between the ligand requirements of CCK-B and delta-opioid receptors which further implies a possible structural relationship between these receptors.
Slaninova
J
J
Department of Pharmacology, University of Arizona Health Science Center, Tucson 85724.
Knapp
R J
RJ
Wu
J J
JJ
Fang
S N
SN
Kramer
T
T
Burks
T F
TF
Hruby
V J
VJ
Yamamura
H I
HI
D000595:Amino Acid Sequence; D000700:Analgesics / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D006168:Guinea Pigs; D008024:Ligands; D008969:Molecular Sequence Data; D011949:Receptors, Cholecystokinin / Q000378:metabolism; D011957:Receptors, Opioid / Q000378:metabolism*; D012844:Sincalide / Q000031:analogs & derivatives / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000700:Analgesics; D008024:Ligands; D011949:Receptors, Cholecystokinin; D011957:Receptors, Opioid; D012844:Sincalide