Elucidation and characteristics of non-opioid beta-endorphin receptors in rat adrenal cortex.
beta-Endorphin-like decapeptide immunorphin (SLTCLVKGFY), a selective agonist of non-opioid beta-endorphin receptor, was labeled with tritium to specific activity of 24 Ci/mmol. It was used for the detection and characterization of non-opioid beta-endorphin receptors on rat adrenal cortex membranes (Kd1 = 39.6 +/- 2.0 nM, Bmax1 = 40.7 +/- 2.3 pmol/mg protein; Kd2 = 0.25 +/- 0.01 micro M, Bmax2 = 187.8 +/- 9.4 pmol/mg protein). beta-Endorphin was found to inhibit the [3H]immunorphin specific binding to membranes (Ki = 70.0 +/- 9.2 nM); naloxone, [Met5]enkephalin, and alpha- and gamma-endorphins tested in parallel were inactive. Immunorphin at concentrations of 10(-9)-10(-6) M was found to inhibit the adenylate cyclase activity in adrenocortical membranes, while intramuscular injection of immunorphin at doses of 10-100 micro g/kg was found to reduce the secretion of 11-oxycorticosteroids from the adrenals to the bloodstream.
Navolotskaya
E V
EV
Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Pushchino, Moscow Region, 142290, Russia. navolots@fibkh.serpukhov.su
Kovalitskaya
Yu A
YA
Zolotarev
Yu A
YA
Kudryashova
N Yu
NY
Goncharenko
E N
EN
Kolobov
A A
AA
Kampe-Nemm
E A
EA
Malkova
N V
NV
Yurovsky
V V
VV
Lipkin
V M
VM
D015062:11-Hydroxycorticosteroids / Q000097:blood / Q000378:metabolism; D000262:Adenylyl Cyclases / Q000378:metabolism; D000302:Adrenal Cortex / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D002462:Cell Membrane / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D007127:Immunoglobulin Constant Regions; D007142:Immunoglobulin gamma-Chains; D008297:Male; D009842:Oligopeptides / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011957:Receptors, Opioid / Q000819:agonists / Q000378:metabolism*; D014316:Tritium; D001615:beta-Endorphin / Q000494:pharmacology
D015062:11-Hydroxycorticosteroids; D007127:Immunoglobulin Constant Regions; D007142:Immunoglobulin gamma-Chains; D009842:Oligopeptides; D010446:Peptide Fragments; D011957:Receptors, Opioid; C445661:immunorphin; D014316:Tritium; D001615:beta-Endorphin; D000262:Adenylyl Cyclases