Several analogs of verapamil, which are characterized by a reduced molecular flexibility, have been synthesized. Their pharmacological activity has been evaluated on guinea-pig atria (negative chronotropic and inotropic activities) and guinea-pig aorta strips (vasorelaxing activity). Their ability to displace the calcium antagonist (-)-desmethoxyverapamil ((-)-[3H]-D888) on kitten cardiac tissue has also been evaluated. The pharmacological results are in accord with the previously reported models for negative inotropic and chronotropic activities of verapamil-like compounds, but fail to give information about the conformation(s) that act on smooth muscle. © 1994.
Synthesis and pharmacological evaluation of verapamil analogs with restricted molecular flexibility / Teodori E.; Dei S.; Romanelli M.; Scapecchi S.; Gualtieri F.; Budriesi R.; Chiarini A.; Lemoine H.; Mannhold R.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 29:2(1994), pp. 139-148. [10.1016/0223-5234(94)90211-9]
Synthesis and pharmacological evaluation of verapamil analogs with restricted molecular flexibility
Budriesi R.;Chiarini A.;
1994
Abstract
Several analogs of verapamil, which are characterized by a reduced molecular flexibility, have been synthesized. Their pharmacological activity has been evaluated on guinea-pig atria (negative chronotropic and inotropic activities) and guinea-pig aorta strips (vasorelaxing activity). Their ability to displace the calcium antagonist (-)-desmethoxyverapamil ((-)-[3H]-D888) on kitten cardiac tissue has also been evaluated. The pharmacological results are in accord with the previously reported models for negative inotropic and chronotropic activities of verapamil-like compounds, but fail to give information about the conformation(s) that act on smooth muscle. © 1994.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
