Propofol activates vanilloid receptor channels expressed in human embryonic kidney 293 cells

• Published in: Neuroscience letters 2001-10, Vol.312 (1), p.45-49
• Main Authors: Tsutsumi, Satoshi, Tomioka, Akihiro, Sudo, Makoto, Nakamura, Akio, Shirakura, Kenji, Takagishi, Kenji, Kohama, Kazuhiro
• Format: Article
• Language: English
• Subjects: Anesthetics, Intravenous - pharmacology; Anesthetics. Neuromuscular blocking agents; Binding Sites - drug effects; Binding Sites - physiology; Biological and medical sciences; Calcium - metabolism; Calcium imaging; Calcium Signaling - drug effects; Calcium Signaling - physiology; Capsaicin; Capsaicin - analogs & derivatives; Capsaicin - pharmacology; Cells, Cultured - drug effects; Cells, Cultured - metabolism; Diterpenes - pharmacology; Dose-Response Relationship, Drug; Human embryonic kidney 293 cell; Humans; Intravenous anesthetic; Medical sciences; Membrane Potentials - drug effects; Membrane Potentials - physiology; Nervous System - drug effects; Nervous System - metabolism; Neuropharmacology; Pain - drug therapy; Pain - metabolism; Pain - physiopathology; Patch-Clamp Techniques; Pharmacology. Drug treatments; Propofol; Propofol - pharmacology; Receptors, Drug - drug effects; Receptors, Drug - metabolism; Vanilloid receptor
• ISSN: 0304-3940; 1872-7972
• DOI: 10.1016/S0304-3940(01)02185-1

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.