Further Quinolizidine Derivatives as Antiarrhythmic Agents. 3

Bruno Tasso; Laura Beatrice Mattioli; Michele Tonelli; Vito Boido; Alberto Chiarini; Fabio Sparatore; Roberta Budriesi

doi:10.20944/preprints202308.0877.v1

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preprints.org > medicine and pharmacology > pharmacology and toxicology > doi: 10.20944/preprints202308.0877.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Further Quinolizidine Derivatives as Antiarrhythmic Agents. 3

Bruno Tasso

Laura Beatrice Mattioli

^* ,

Version 1 : Received: 10 August 2023 / Approved: 10 August 2023 / Online: 11 August 2023 (03:03:24 CEST)

A peer-reviewed article of this Preprint also exists.

Tasso, B.; Mattioli, L.B.; Tonelli, M.; Boido, V.; Chiarini, A.; Sparatore, F.; Budriesi, R. Further Quinolizidine Derivatives as Antiarrhythmic Agents- 3. Molecules 2023, 28, 6916. Tasso, B.; Mattioli, L.B.; Tonelli, M.; Boido, V.; Chiarini, A.; Sparatore, F.; Budriesi, R. Further Quinolizidine Derivatives as Antiarrhythmic Agents- 3. Molecules 2023, 28, 6916.

Abstract

Fourteen quinolizidine derivatives, structurally related to the alkaloids lupinine and cytisine and previously studied for other pharmacological aims, were presently tested for antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues, and to assess calcium antagonism in comparison to amiodarone, lidocaine, procainamide, and quinidine. All compounds, but two, compared favorably with the reference drugs. Potent antiarrhythmic activity was observed for compounds (in increasing order) 4, 1, 6 and 5. The last compound N-(3,4,5-trimethoxybenzoyl)aminohomolupinane) was outstanding, exhibiting a nanomolar potency (EC50 = 0.017 µM) for the increase of threshold of ac-arrhythmia, and being devoid of antihypertensive activity against spontaneously hypertensive rats.

Keywords

Quinolizidine derivatives; Lupinine, Cytisine; Sparteine; Antiarrhythmic activity; Inotropic and chronotropic activities; Vasorelaxant activity

Subject

Medicine and Pharmacology, Pharmacology and Toxicology

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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