[Analysis of new opiate-like peptides using a radioreceptor method].
A screening of new synthetic opioid-like peptides has been carried out by the radioreceptor assay using selective labeled ligands to mu-, delta- and gamma-opioid receptors of the rat brain membranes. With this aim peptides from sequences of the following proteins were used: kapporphin-Tyr-Ser-Phe-Gly-Gly and its analogues-Tyr-Ser-Phe-Gly-Gly-NH2, Tyr-D-Ser-Phe-Gly-Gly, Tyr-D-Ser-Phe-Gly-Gly-NH2, myelorphin-Phe-Gly-Tyr-Gly-Gly, interenkephalin B-Arg-Arg-Gln-Phe-Lys and chimeric peptide IEPhBin 1-Tyr-Gly-Gly-Phe-Leu-Arg-Pro-Tyr-Ile-Leu consisting of leu-enkephalin and pentaneurotensin. It has been found that myelorphin has a prevalent affinity to mu-receptor, while the kapporphin analogues both to mu- and delta-receptors. The presence of pentaneurotensin in chimeric peptide does not affect the specificity of binding to opioid receptors, but decreases affinity to mu- and delta-receptors approximately by an order as compared to leu-enkephalin. Kapprorphin and interenkephalin B displace neither of the selective labeled opioid ligands under study.
Shestak
K I
KI
Sergeeva
M G
MG
Zaĭtsev
S V
SV
Kharchenko
E P
EP
Varfolomeev
S D
SD
Kalikhevich
V N
VN
Ardemasova
Z A
ZA
D000595:Amino Acid Sequence; D000701:Analgesics, Opioid / Q000032:analysis*; D000818:Animals; D001923:Brain Chemistry; D004723:Endorphins / Q000032:analysis* / Q000494:pharmacology; D008969:Molecular Sequence Data; D011869:Radioligand Assay; D051381:Rats; D011957:Receptors, Opioid / Q000032:analysis*
D000701:Analgesics, Opioid; D004723:Endorphins; D011957:Receptors, Opioid
Analiz novykh opiatopodobnykh peptidov radioretseptornym metodom.