Abstract

Mexiletine is a very well-known class IB antiarrhythmic drug, whose enantiomers differ in both pharmacodynamic and pharmacokinetic properties, the (R)-isomer being the eutomer on experimental arrhythmias and in binding studies on cardiac voltage-gated sodium channels. meta-Hydroxymexiletine (MHM) is a minor metabolite of mexiletine, which has demonstrated to be more potent than the parent compound. Herein we report the synthesis and biological evaluation of MHM enantiomers for their potential antiarrhythmic activity. The same stereoselectivity pattern observed for mexiletine was found for MHM: the (R)-enantiomer of MHM was the eutomer on ac-arrhythmia also showing a negative inotropism higher than the one displayed by mexiletine and, at the same time, a decreased vasorelaxant activity on guinea-pig left atrium and guinea-pig ileum longitudinal smooth muscle.

Autore Pugliese

• Carocci Alessia , Catalano Alessia , Franchini Carlo , Lentini Giovanni , Cavalluzzi Maria Maddalena

Tutti gli autori

• CAROCCI A.;CATALANO A.;FRANCHINI C.;LENTINI G.;CAVALLUZZI M.M.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2013

ISSN

0223-5234

ISBN

Non Disponibile

Numero di citazioni Wos

12

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

12

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile