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Registration Number

0208U002202, 0105U002252 , R & D reports

Title

Search the effective myotropic spasmolytics among the guanidine and 1,4-dihydropyridine derivatives.

Head

Mochort N,

Registration Date

18-01-2008

Organization

Institute of Pharmacology and Toxicology Academy of Medical sciences of Ykraine

Description

The influence of the new fluor-containing derivatives of guanidine, 1,4- dihydropyridine derivatives, the oxygen-containing analogues of the last, the derivatives of adamantane and cyclopenta [d] pyrimidine on contractile activity of the vessels (aortha of rats) and of the urinary bladder on the background of constriction caused by hyperpotassic solution with KC1 60 mM and with the phenylenylephrine was first experimentally studied. The experimental compounds are concentration-dependent to spasmolytic property. On the background of the constriction by phenylephrine the most active compounds possess EC50 within 10 -7 M-10 -9M. The average magnitude of lethal doses determined by the method of smaller squares allow to consider its as belonging to class of low toxic compounds. The basis for creation of the new myotropic spasmolytic agent and it's inculcation into medical practice is the confirmation of specific activity of the most effective compounds under systemic and it's innocence under the prolonged administration.

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