Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity.
Allosteric modulation of mouse 5-Hydroxytryptamine(3A) (5-HT(3A)) and 5-HT(3A/B) receptor function by ethanol and trichloroethanol (TCEt) was assessed in HEK293 cells with whole cell patch-clamp electrophysiological recordings. Ethanol enhanced 5-HT(3A) receptor function, but had no effect on mouse 5-HT(3A/B) receptor mediated currents. The enhancing action of trichloroethanol (TCEt) on mouse 5-HT(3A/B) receptor function was much less than that observed in the mouse 5-HT(3A) receptor. Where alcohol-induced increases in peak amplitude were observed, the slope of the 20-80% rising phase of current onset was also enhanced, suggesting that increases in activation rate may be one mechanism through which alcohols enhance function of the 5-HT(3) receptors.
Hayrapetyan
Volodya
V
Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Blvd., Fort Worth, TX 76107-2699, USA.
Jenschke
Monica
M
Dillon
Glenn H
GH
Machu
Tina K
TK
D000818:Animals; D002460:Cell Line; D002492:Central Nervous System Depressants / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004558:Electric Stimulation / Q000379:methods; D000431:Ethanol / Q000494:pharmacology*; D005023:Ethylene Chlorohydrin / Q000031:analogs & derivatives / Q000494:pharmacology; D015870:Gene Expression / Q000187:drug effects*; D006801:Humans; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology / Q000528:radiation effects; D051379:Mice; D018408:Patch-Clamp Techniques / Q000379:methods; D021122:Protein Subunits / Q000235:genetics / Q000378:metabolism; D044406:Receptors, Serotonin, 5-HT3 / Q000235:genetics / Q000378:metabolism*; D012701:Serotonin / Q000494:pharmacology; D014162:Transfection / Q000379:methods
D002492:Central Nervous System Depressants; D021122:Protein Subunits; D044406:Receptors, Serotonin, 5-HT3; D012701:Serotonin; D000431:Ethanol; D005023:Ethylene Chlorohydrin; C005849:2,2,2-trichloroethanol