Inhibitory effect of local anesthetics on Na+/H+ antiporter in brush border membrane-reconstituted vesicles.
The effects of three local anesthetics, lidocaine, dibucaine, and tetracaine, on Na+/H+ antiporter activity were examined in brush border membrane-reconstituted vesicles. Lidocaine at 10 microM inhibited H+ efflux in the presence of an inward Na+ gradient, suggesting that this anesthetic specifically inhibits the Na+/H+ antiporter. On the other hand, dibucaine and tetracaine decreased H+ efflux even in the absence of a Na+ gradient.
Shibamoto
S
S
Department of Biochemistry, Faculty of Pharmaceutical Sciences, Setsunan University, Japan.
Hori
T
T
Hayakawa
M
M
Nango
M
M
Cragoe
E J
EJ
Oku
N
N
Ito
F
F
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D017920:Antiporters; D002352:Carrier Proteins / Q000187:drug effects*; D003992:Dibucaine / Q000494:pharmacology; D066298:In Vitro Techniques; D007668:Kidney / Q000187:drug effects / Q000378:metabolism; D008012:Lidocaine / Q000494:pharmacology; D008871:Microvilli / Q000187:drug effects* / Q000378:metabolism; D011522:Protons; D051381:Rats; D012964:Sodium / Q000378:metabolism*; D013748:Tetracaine / Q000494:pharmacology
D000779:Anesthetics, Local; D017920:Antiporters; D002352:Carrier Proteins; D011522:Protons; D013748:Tetracaine; D008012:Lidocaine; D012964:Sodium; D003992:Dibucaine