Propofol activates vanilloid receptor channels expressed in human embryonic kidney 293 cells.
Propofol (2,6-diisopropylphenol) is an intravenous anesthetic agent structurally unrelated to any other intravenous anesthetics. We examined the effect of propofol on a rat vanilloid receptor that was expressed in the human embryonic kidney (HEK) 293 cells by using calcium imaging method. Propofol caused a concentration-dependent increase in [Ca(2+)](i) in the HEK293 cells with the receptor. These responses were inhibited by removing extracellular calcium ions. The propofol-evoked increase in [Ca(2+)](i) in the HEK293 cells with the receptor was partially inhibited by capsazepine, a competitive antagonist of capsaicin. We conclude that propofol acts as an agonist for the receptor.
Tsutsumi
S
S
Department of Pharmacology, Gunma University School of Medicine, Maebashi, Gunma 371-8511, Japan. stutumi@med.gunma-u.ac.jp
Tomioka
A
A
Sudo
M
M
Nakamura
A
A
Shirakura
K
K
Takagishi
K
K
Kohama
K
K
D018686:Anesthetics, Intravenous / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D002118:Calcium / Q000378:metabolism*; D020013:Calcium Signaling / Q000187:drug effects / Q000502:physiology; D002211:Capsaicin / Q000031:analogs & derivatives* / Q000494:pharmacology; D002478:Cells, Cultured / Q000187:drug effects* / Q000378:metabolism; D004224:Diterpenes / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D009420:Nervous System / Q000187:drug effects* / Q000378:metabolism; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D018408:Patch-Clamp Techniques; D015742:Propofol / Q000494:pharmacology*; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism
D018686:Anesthetics, Intravenous; D004224:Diterpenes; D011955:Receptors, Drug; C024353:resiniferatoxin; C071423:capsazepine; D002211:Capsaicin; D002118:Calcium; D015742:Propofol