[3H]-Dynorphin A (1-8): degradation profile and binding characteristics in brain homogenates.
[3H]-Dynorphin A (1-8) was degraded in brain homogenates at 25 degrees and even at 0 degree C. The peptidase inhibitors bestatin and captopril almost completely protected[3H]-dynorphin A (1-8) from degradation at 0 degree C but had only little effect on binding at this temperature. At 25 degrees C, the binding of [3H]-dynorphin A (1-8) was markedly improved by addition of bestatin, captopril and L-leucyl-L-arginine, which afforded some, but not complete protection from degradation. The results of saturation binding assays at 25 degrees C in the presence of the peptidase inhibitors were variable. However, it was found from saturation binding assays at 0 degree C that the maximum binding capacity for [3H]-dynorphin A (1-8) at the kappa-site is similar to that of [3H]-(-)-bremazocine and [3H]-dynorphin A (1-9).
Gillan
M G
MG
Robson
L E
LE
McKnight
A T
AT
Kosterlitz
H W
HW
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002216:Captopril / Q000494:pharmacology; D004399:Dynorphins / Q000378:metabolism*; D006168:Guinea Pigs; D007930:Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D010446:Peptide Fragments / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism; D017473:Receptors, Opioid, kappa
D010446:Peptide Fragments; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D004399:Dynorphins; C026770:dynorphin (1-8); D002216:Captopril; D007930:Leucine; C012211:ubenimex