Cocaine inhibits 5-HT3 receptor function in neurons from transgenic mice overexpressing the receptor.
Studies have shown that cocaine alters the function of recombinant 5-HT(3) receptors and that behavioral responses to cocaine are affected by 5-HT(3) receptor ligands. However, the actions of cocaine on brain 5-HT(3) receptors have not been characterized because these receptors are not abundantly expressed in most neuronal populations. We examined the effect of cocaine on 5-HT(3) receptor function in cultured hippocampal neurons from transgenic mice overexpressing the receptor. Cocaine competitively inhibited 5-HT(3) receptors with an IC(50) of approximately 4 microM, indicating that brain 5-HT(3) receptors are important targets for the actions of this commonly abused substance.
Carta
Mario
M
Department of Neurosciences, University of New Mexico Health Sciences Center, Basic Medical Sciences Building, Room 145, Albuquerque, NM 87131-5223, USA.
Allan
Andrea M
AM
Partridge
L Donald
LD
Valenzuela
C Fernando
CF
D000818:Animals; D002478:Cells, Cultured; D003042:Cocaine / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005786:Gene Expression Regulation / Q000187:drug effects / Q000502:physiology; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008822:Mice, Transgenic; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000096:biosynthesis* / Q000235:genetics; D044406:Receptors, Serotonin, 5-HT3; D012701:Serotonin / Q000494:pharmacology
D011985:Receptors, Serotonin; D044406:Receptors, Serotonin, 5-HT3; D012701:Serotonin; D003042:Cocaine