Effect of milrinone analogues on intracellular calcium increase in single living H9C2 cardiac cells.
The synthesis of milrinone analogues where the 4-pyridyl moiety was replaced by an ester or amide group is reported. Only amide derivatives are able to support intracellular calcium influx following chemical depolarization with 60 mM KCl in a percentage varying from 20 to 45% of differentiated H9C2 cardiomyocytes. Those cells were differentiated after chronic exposure to 10 nM retinoic acid which induces the expression of voltage-gated calcium channels. Analogues of milrinone containing an ester function did not show significant activity.
Pietrangelo
Tiziana
T
Dipartimento di Scienze Mediche di Base e Applicate, Università degli Studi G. d'Annunzio, via dei Vestini 31, 66100 Chieti, Italy.
Giampietro
Letizia
L
De Filippis
Barbara
B
La Rovere
Rita
R
Fulle
Stefania
S
Amoroso
Rosa
R
D002118:Calcium / Q000378:metabolism*; D015220:Calcium Channels / Q000378:metabolism; D002316:Cardiotonic Agents / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D006321:Heart / Q000187:drug effects*; D006801:Humans; D015640:Ion Channel Gating; D020105:Milrinone / Q000494:pharmacology* / Q000633:toxicity; D009206:Myocardium / Q000166:cytology / Q000378:metabolism*
D015220:Calcium Channels; D002316:Cardiotonic Agents; D020105:Milrinone; D002118:Calcium