[Synthesis and biological activity of new analogs of beta-casomorphine-5].
Four new analogues of beta-cazomorphine-5 modified at the C-end with ethylenediamine- and glycine-containing derivatives were synthesized by the standard method of peptide chemistry (mixed anhydrides, carbodiimide, activated esters): H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-II (I) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-II (II) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH3 (III) H-Tyr-Pro-Phe-Pro-Gly-EtDA-Gly-Gly-CO-CH2-CH2-COOH (IV) The level of affinity and the degree of selectivity of the peptides towards the mu- and delta-opioid receptors of the rat brain lyophilized membranes were studied by the radioreceptor method. All the new peptides displayed analgetic activity, largely depending upon their structure.
Sobirov
M M
MM
Khalikov
Sh Kh
ShKh
Saidov
S S
SS
Kodirov
M Z
MZ
Zaĭtsev
S V
SV
Chichenkov
O N
ON
Varfolomeev
S D
SD
D000595:Amino Acid Sequence; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002364:Caseins / Q000737:chemistry*; D004723:Endorphins / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008815:Mice, Inbred Strains; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D017465:Receptors, Opioid, delta / Q000187:drug effects
D000700:Analgesics; D002364:Caseins; D004723:Endorphins; D010446:Peptide Fragments; D017465:Receptors, Opioid, delta; C034812:beta-casomorphin 5
Sintez i biologicheskaia aktivnost' novykh analogov beta-kazomorfina-5.