Trichloroethanol inhibits ATP-induced membrane currents in cultured HEK 293-hP2X3 cells.
Membrane currents in response to the application of alpha, beta-methylene ATP (alpha,beta-meATP) were recorded by the whole-cell patch-clamp technique in human embryonic kidney 293 cells transfected with the human P2X3 receptor (HEK 293-hP2X3 cells). Trichloroethanol, the biologically active metabolite of chloral hydrate, but not ethanol itself concentration-dependently and reversibly inhibited the current responses. It was concluded that the reported analgesic effect of chloral hydrate may be due to the interruption of pain transmission in dorsal root ganglia expressing P2X3 receptors.
Köles
L
L
Rudolf-Boehm-Institute of Pharmacology and Toxicology, University of Leipzig, Haertelstrasse 16-18, D-04107, Leipzig, Germany.
Wirkner
K
K
Fürst
S
S
Wnendt
S
S
Illes
P
P
D000255:Adenosine Triphosphate / Q000031:analogs & derivatives* / Q000494:pharmacology; D002460:Cell Line; D002492:Central Nervous System Depressants / Q000494:pharmacology; D000431:Ethanol / Q000494:pharmacology; D005023:Ethylene Chlorohydrin / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D007473:Ion Channels / Q000187:drug effects* / Q000502:physiology; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D018048:Receptors, Purinergic P2 / Q000187:drug effects* / Q000502:physiology; D058477:Receptors, Purinergic P2X3
D002492:Central Nervous System Depressants; D007473:Ion Channels; C546407:P2RX3 protein, human; D018048:Receptors, Purinergic P2; D058477:Receptors, Purinergic P2X3; D000431:Ethanol; D005023:Ethylene Chlorohydrin; D000255:Adenosine Triphosphate; C005849:2,2,2-trichloroethanol; C002630:alpha,beta-methyleneadenosine 5'-triphosphate