[Specific binding of mu- and delta-ligands by opiate receptors in the rat brain in the presence of reaferon].
The ability of recombinant alpha 2-interferon (reaferon) to compete for opiate binding sites with mu- and delta-selective compounds was determined. Reaferon was found to inhibit the binding of 3H-D-ala2, D-leu5-enkephalin, and Ki value calculated was equal to 8.5 +/- 2.6 U.10(-3)/ml. The mu-agonists reception levels were decreased in the presence of reaferon at concentrations above 500 U/ml; the Ki values for 3H-morphine, 3H-dihydromorphine, 3H-RX 783006 were found to be 3.25 +/- 0.35, 4.28 +/- 0.81 and 6.51 +/- 1.27 U.10(-4)/ml, respectively. When reaferon was added into reaction medium at concentrations more than 5.10(3) U/ml the specific receptor binding of opiate antagonist 3H-naloxone was demonstrated to be increased and this effect was reversed with 100 mM NaCl. The existence of allosteric reaferon binding site which coupled with naloxone sensitive receptor was suggested to explain the results obtained.
Panchenko
L F
LF
Aliab'eva
T N
TN
Petrichenko
O B
OB
Bumialis
V V
VV
Balashov
A M
AM
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000378:metabolism; D016308:Enkephalin, Leucine-2-Alanine; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000378:metabolism; D066298:In Vitro Techniques; D007370:Interferon Type I / Q000494:pharmacology*; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D011994:Recombinant Proteins
D007370:Interferon Type I; D000077190:Interferon alpha-2; D016898:Interferon-alpha; D008024:Ligands; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D011994:Recombinant Proteins; D004744:Enkephalin, Methionine; D004743:Enkephalin, Leucine; C022118:enkephalinamide-Met, Ala(2)-; D016308:Enkephalin, Leucine-2-Alanine
Spetsificheskoe sviazyvanie mu- i delta-ligandov opiatnymi retseptorami golovnogo mozga krys v prisutstvii reaferona.