Propofol potentiates ATP-activated currents of recombinant P2X(4) receptor channels expressed in human embryonic kidney 293 cells.
We examined the effects of a general anesthetic 2, 6-diisopropylphenol (propofol) on ATP- and alpha,beta-methylene ATP (alphabetameATP)-activated currents in the human embryonic kidney 293 (HEK 293) cells expressing recombinant P2X receptor channels, using the whole-cell patch-clamp method. Propofol at clinical relevant concentrations ( approximately 56 microM) potentiated the current responses through the P2X(4) receptor in a dose-dependent manner, whereas propofol did not affect the responses through the P2X(2) receptor or through the heterologous complex of the P2X(2) and P2X(3) (P2X(2+3)) receptor. These results suggest that activation of P2X(4) subtype in the brain and the motor neurons of the spinal anterior horn might be involved in the excitatory effect by propofol such as convulsion and unexpected movements.
Tomioka
A
A
Department of Anesthesiology and Reanimatology, Gunma University School of Medicine, Gunma, Japan.
Ueno
S
S
Kohama
K
K
Goto
F
F
Inoue
K
K
D000255:Adenosine Triphosphate / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D018686:Anesthetics, Intravenous / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D004553:Electric Conductivity; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D015742:Propofol / Q000494:pharmacology*; D020033:Protein Isoforms / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D058910:Purinergic P2 Receptor Agonists; D051381:Rats; D018048:Receptors, Purinergic P2 / Q000235:genetics / Q000378:metabolism*; D058476:Receptors, Purinergic P2X2; D058477:Receptors, Purinergic P2X3; D058848:Receptors, Purinergic P2X4; D011994:Recombinant Proteins / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D014162:Transfection
D018686:Anesthetics, Intravenous; C546401:P2RX2 protein, human; C546407:P2RX3 protein, human; C548226:P2RX4 protein, human; D020033:Protein Isoforms; D058910:Purinergic P2 Receptor Agonists; D018048:Receptors, Purinergic P2; D058476:Receptors, Purinergic P2X2; D058477:Receptors, Purinergic P2X3; D058848:Receptors, Purinergic P2X4; D011994:Recombinant Proteins; D000255:Adenosine Triphosphate; C002630:alpha,beta-methyleneadenosine 5'-triphosphate; D015742:Propofol