Chapter 9. Calcium Antagonists - New Opportunities

摘要: Publisher Summary The medicinal chemistry of the calcium antagonists is characterized at present by a large number new development compounds. However, majority these products resembles in their structure clinically established verapamil, nifedipine, and diltiazem. In addition, some cardiovascular drugs, which have already been introduced or are being developed, claimed to be antagonists. Completely structures whose pharmacological action primarily because inhibition influx into contractile cells still rare. Investigation binding sites basic structures, having calcium-antagonistic action, gives leads for drug design. Gallopamil, derived from superior potency parent substance verapamil but activity profile largely comparable. This also applies enantiomers. (−)-Gallopamil has pure “calcium-antagonistic” properties, whereas (+)-isomer significantly weaker effect this model. shows an interesting anti-arrhythmic higher doses, possibly additional stabilizing on membrane. greater (−)-isomer can demonstrated vitro guinea-pig ileum.