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.
Teodori E., Dei S., Romanelli M., Scapecchi S., Gualtieri F., Budriesi R., et al. (1994). Synthesis and pharmacological evaluation of verapamil analogs with restricted molecular flexibility. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 29(2), 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.
