ΣΥΝΘΕΣΗ ΚΑΙ ΦΑΡΜΑΚΟΛΟΓΙΚΗ ΔΡΑΣΗ ΑΝΑΛΟΓΩΝ ΤΗΣ ΑΓΓΕΙΟΤΕΝΣΙΝΗΣ ΙΙ ΜΕ ΠΕΡΙΟΡΙΣΜΕΝΗ ΔΙΑΜΟΡΦΩΤΙΚΗ ΕΛΕΥΘΕΡΙΑ

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ΣΥΝΘΕΣΗ ΚΑΙ ΦΑΡΜΑΚΟΛΟΓΙΚΗ ΔΡΑΣΗ ΑΝΑΛΟΓΩΝ ΤΗΣ ΑΓΓΕΙΟΤΕΝΣΙΝΗΣ ΙΙ ΜΕ ΠΕΡΙΟΡΙΣΜΕΝΗ ΔΙΑΜΟΡΦΩΤΙΚΗ ΕΛΕΥΘΕΡΙΑ

Μπελτέ, Ουρανία-Αναστασία

PhD Thesis

1994


THE SYNTHESIS AND THE PHARMACOLOGICAL PROPERTIES OF TWENTY-ONE NEW ANGIOTENSIN II (AII) ANALOGUES. THIS STUDY WAS PERFORMED FOR FURTHER UNDERSTANDING OF THE STRUCTURE-ACTIVITY RELATIONSHIPS, AND THE IMPROVEMENT OF NEW POTENT LONG-ACTING AII ANTAGONISTS WITH THERAPEUTIC USE. THE PEPTIDES WERE SYNTHESIZED BY MERRIFIELD'S SOLID PHASE PROCEDURE, PURIFIED BY REVERSED- PHASE HPLC. THECOMPOUNDS WERE TESTED ON FABBIT AORTA STRIPS, IN THE RAT ISOLATA UTERUS ANDBORINE ADVENOCORTICAL MEMBRANES. THE CONCLUSION OF THEIR STUDIES CONCERNING STRUCTURE ACTIVITY RELATIONSHIPS INDICATE THAT : -THE PRESENCE OF Β-COOH AT THE TERMINAL PART OF AII IS CRITICAL FOR BOTH BINDING AFFINITY AND STIMULATION /-AN INCREASED IN BASICITY AT THE N-TEREMINAL NITROGEN ATOM OF AII IS NOT THE ONLY REASON FOR INCREASED POTENCY./-THE PRESENCE OF AIB0 IN THE N-TERMINAL RESTRICTS THE ROLE CONFORMATION OF THE PEPTIDE./-THE OH- OF TYR4 IS IMPORTANT FOR THE AGONIST ACTIVITY OF AII./-THE SIZE AND THE SPABE OF THE N-TERMINAL RESIDUE OF SARMESIN APPEARS TO BE SUBJECT TO UNSUALLY SEVERE RESTRICTIONS./-THE PROSENCE OF AIB7 PROVIDES STERIC HYNDRANCE./-THE POSITIVE CHARGE LOCATED ON THE GUANIDINE GROUP OF ARG2 RESIDUE IS MANDATORY FOR THE BIOLOGICAL ACTIVITY.(ABSTRACT TRUNCATED)

Ιατρική και Επιστήμες Υγείας ➨ Βασική Ιατρική

PHARMACOLOGICAL PROPERTIES
Basic Medicine
Medical and Health Sciences
Αγγειοτενσίνη II
ΑΝΑΛΟΓΑ
Φαρμακολογική δράση
ΔΙΑΜΟΡΦΩΤΙΚΗ ΕΛΕΥΘΕΡΙΑ
Βασική Ιατρική
ANGIOTENSINII
Ιατρική και Επιστήμες Υγείας
ANALOGUES

Greek

Πανεπιστήμιο Πατρών
University of Patras

Πανεπιστήμιο Πατρών. Σχολή Επιστημών Υγείας. Τμήμα Φαρμακευτικής




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