Bioorganicheskaia khimiia 1994-07-01

[Synthesis and biological activity of new analogs of beta-casomorphine-5].

M M Sobirov, Sh Kh Khalikov, S S Saidov, M Z Kodirov, S V Zaĭtsev, O N Chichenkov, S D Varfolomeev

Index: Bioorg. Khim. 20(7) , 740-50, (1994)

Full Text: HTML

Abstract

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.

Related Compounds

  • β-Casomorphin (1-5...

Related Articles:

Tyr-c[D-Orn-Tyr(Bzl)-Pro-Gly]: a novel antiproliferative acting somatostatin receptor agonist with mu-opioid receptor-sensitizing properties.

2003-09-01

[Br. J. Pharmacol. 140(1) , 13-22, (2003)]

Metabolism of D-proline beta-casomorphin derivatives in the rat brain.

1988-01-01

[Biomed. Biochim. Acta 47(9) , 865-9, (1988)]

Morphiceptin and beta-casomorphin-5 analogues containing a reduced peptide bond: selective mu-receptor agonists and a novel mu antagonist, H-Tyr-Pro psi (CH2-NH)Phe-Pro-Gly-OH.

1992-08-01

[Biopolymers 32(8) , 957-69, (1992)]

Assignment of the 1H-NMR resonances of the four rotamers of beta-casomorphin-5 in DMSO.

1991-10-15

[Biopolymers 31(12) , 1409-16, (1991)]

Nonopioid effects of beta-casomorphin-5 in guinea pig heart: alterations to the beta-adrenoceptor-G-protein complex and inhibition of myocardial responses to isoproterenol.

1991-01-01

[Peptides 12(2) , 265-70, (1991)]

More Articles...