Τμήμα Χημείας

Hypertension study in anesthetized rabbits: Protocol proposal for AT1 antagonist screening

Αγγλικά

Introduction: The aim of this study was to
establish an optimized fast and safe protocol
for the pharmacological screening of AT1
antagonists.
Materials and methods: The pharmaceutical
prototype AT1 antagonist losartan, its active
metabolite EXP3174 and the synthetic
compound MMK1 were analysed in order
to validate the protocol. Ang II was
continuously infused while the animals
received the drugs in two procedures.
Results: In the post-treatment procedure
drugs were administered either in a single
bolus dose or in a sequential manner. When
losartan was administered in a single bolus
dose, efficacy was evident until the 7th min
(p=0.012) whilst EXP3174 infusion extended
the efficiency up to the end of the study
(p=0.006). In addition, the sequential
injections of losartan prolonged the
inhibitory time interval until the end of the
study (p=0.045). In the pre-treatment
procedure, results suggested a dosedependent inhibitory effect for both
antagonists. The pressor response to Ang II
was unchanged after MMK1 administration
either in the post- or in the pre-treatment
mode.
Conclusions: The proposed protocol
appears to be safe, simple and fast for
the pharmacological screening of AT1
antagonists and enables the evaluation of
new antagonists using lower doses than any
other reported in the literature.

2010

A. P. Politi, M. V. Zervou, H. Triantafyllidi, P. G. Zoumpoulakis, T. M. Mavromoustakos, A. A. Zoga, P. Moutevelis-Minakakis, G. Kokotos, E. K. Iliodromitis, D. Th. Kremastinos

Journal of the Renin Angiotensin Aldosterone System

Sage

11

2

103-110

animal model, AT1 antagonist, EXP3174, hypertension, losartan

Θετικές Επιστήμες

https://doi.org/10.1177/1470320310365016

10.1177/1470320310365016

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https://pergamos.lib.uoa.gr/uoa/dl/object/2956827