Effects of volatile anesthetics on cardiac calcium channels.
In order to investigate how volatile anesthetics affect cardiac calcium channels, the effects of halothane, enflurane, and isoflurane on the specific binding of [3H]-nitrendipine to bovine heart sarcolemmal membranes were studied. All three anesthetics added in liquid form inhibited [3H]-nitrendipine binding in a dose-dependent manner, and more interestingly, the order of inhibition by these volatile anesthetics roughly followed that of their anesthetic potencies. The partial pressures, calculated using the gas/water partition coefficients of halothane, enflurane, and isoflurane which inhibited [3H]-nitrendipine binding by 30% at 37 degrees C were about 1.48 x 10(-2) atm. (1.48%), 4.89 x 10(-2) atm. (4.89%) and 2.76 x 10(-2) atm. (2.76%), respectively. One mmol/l halothane altered not only the maximal binding (Bmax) from 189 f mol/mg protein to 136 f mol/mg protein, but also the dissociation constant (Kd) from 0.074 nmol/l to 0.18 nmol/l. Halothane was also added to the reaction mixture in the gaseous form with air. The partial pressure of halothane needed to bring about 30% inhibition was 0.82 x 10(-2) (0.82%), a value almost similar to that for halothane added in the liquid form. These results indicate that all three volatile anesthetics have direct effects on cardiac calcium channels, and that the magnitude of the effects depends on their anesthetic potencies.
Nakao
S
S
Department of Anesthesia, Kyoto University Hospital, Japan.
Hirata
H
H
Kagawa
Y
Y
D000818:Animals; D015220:Calcium Channels / Q000187:drug effects*; D002417:Cattle; D004737:Enflurane / Q000494:pharmacology*; D006221:Halothane / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects*; D066298:In Vitro Techniques; D007530:Isoflurane / Q000494:pharmacology*; D009568:Nitrendipine / Q000378:metabolism; D012508:Sarcolemma / Q000378:metabolism; D014316:Tritium; D014835:Volatilization
D015220:Calcium Channels; D014316:Tritium; D004737:Enflurane; D009568:Nitrendipine; D007530:Isoflurane; D006221:Halothane