Quinacrine inhibits the calcium-induced calcium release in heavy sarcoplasmic reticulum vesicles.
Quinacrine is a fluorescence probe useful for studying the effect of local anesthetics. The interaction of quinacrine and sarcoplasmic reticulum membranes measured by fluorescence spectroscopy indicates the presence of a saturable binding site. Typical local anesthetics are able to displace quinacrine bound to heavy sarcoplasmic reticulum membranes. The effectiveness of that displacement decreases in the order dibucaine greater than tetracaine greater than benzocaine greater than lidocaine greater than procaine greater than procainamide, indicating that the size and hydrophobicity of quinacrine are major determinants in the binding process. The use of radioactive tracer and a rapid filtration technique reveals that quinacrine interacts, at lower concentrations, with sarcoplasmic reticulum membranes by blocking the Ca2+-induced Ca2+ release. Higher quinacrine concentrations also affect the Ca2+-pump activity.
Fernandez-Belda
F
F
Departamento de Bioquimica, Facultad de Veterinaria, Universidad de Murcia, Spain.
Soler
F
F
Gomez-Fernandez
J C
JC
D000251:Adenosine Triphosphatases / Q000378:metabolism; D000777:Anesthetics / Q000494:pharmacology; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002118:Calcium / Q000378:metabolism*; D002462:Cell Membrane / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D011796:Quinacrine / Q000494:pharmacology*; D011817:Rabbits; D012519:Sarcoplasmic Reticulum / Q000187:drug effects* / Q000201:enzymology
D000777:Anesthetics; D000251:Adenosine Triphosphatases; D011796:Quinacrine; D002118:Calcium