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.
Subject(s)
Analgesics/chemical synthesis , Caseins/chemistry , Endorphins/chemical synthesis , Peptide Fragments/chemical synthesis , Amino Acid Sequence , Analgesics/pharmacology , Animals , Brain/drug effects , Brain/metabolism , Endorphins/pharmacology , Mice , Mice, Inbred Strains , Molecular Sequence Data , Peptide Fragments/pharmacology , Radioligand Assay , Receptors, Opioid, delta/drug effectsABSTRACT
The article deals with a complex study of parameters of the hemodynamics and volume of the cardiac cavities in comparison with a clinical state of patients suffering from mitral defect before and in different periods following prosthesis of the mitral valve. On the basis of the results obtained during examination of 54 patients there was revealed a complete conformity between their clinical state, data of the hemodynamics, the volume of the heart and left auricle. A reverse development of many signs characteristic of the defect was established. The absence of an absolute improvement of some clinical and hemodynamic indices in remote periods following the operation in a number of patients was connected with a marked increase of the cardiac volumes before the operation, an unsatisfactory contractile capacity of the myocardium, the remaining of cardiac fibrillation after the operation.
