The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator Export

@article{citeulike:4053224, abstract = {The sigma-1 receptor is widely distributed in the central nervous system and periphery. Originally mischaracterized as an opioid receptor, the sigma-1 receptor binds a vast number of synthetic compounds but does not bind opioid peptides; it is currently considered an orphan receptor. The sigma-1 receptor pharmacophore includes an alkylamine core, also found in the endogenous compound N,N-dimethyltryptamine (DMT). DMT acts as a hallucinogen, but its receptor target has been unclear. DMT bound to sigma-1 receptors and inhibited voltage-gated sodium ion (Na+) channels in both native cardiac myocytes and heterologous cells that express sigma-1 receptors. DMT induced hypermobility in wild-type mice but not in sigma-1 receptor knockout mice. These biochemical, physiological, and behavioral experiments indicate that DMT is an endogenous agonist for the sigma-1 receptor. 10.1126/science.1166127}, author = {Fontanilla, Dominique and Johannessen, Molly and Hajipour, Abdol R. and Cozzi, Nicholas V. and Jackson, Meyer B. and Ruoho, Arnold E.}, citeulike-article-id = {4053224}, citeulike-linkout-0 = {http://dx.doi.org/10.1126/science.1166127}, citeulike-linkout-1 = {http://www.sciencemag.org/cgi/content/abstract/323/5916/934?sa_campaign=Email}, citeulike-linkout-2 = {http://view.ncbi.nlm.nih.gov/pubmed/19213917}, citeulike-linkout-3 = {http://www.hubmed.org/display.cgi?uids=19213917}, day = {13}, doi = {10.1126/science.1166127}, journal = {Science}, keywords = {dmt, sigma-1}, month = {February}, number = {5916}, pages = {934--937}, posted-at = {2009-03-03 23:42:47}, priority = {4}, title = {The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator}, url = {http://dx.doi.org/10.1126/science.1166127}, volume = {323}, year = {2009} }

TY - JOUR ID - citeulike:4053224 L3 - citeulike-article-id:4053224 N2 - The sigma-1 receptor is widely distributed in the central nervous system and periphery. Originally mischaracterized as an opioid receptor, the sigma-1 receptor binds a vast number of synthetic compounds but does not bind opioid peptides; it is currently considered an orphan receptor. The sigma-1 receptor pharmacophore includes an alkylamine core, also found in the endogenous compound N,N-dimethyltryptamine (DMT). DMT acts as a hallucinogen, but its receptor target has been unclear. DMT bound to sigma-1 receptors and inhibited voltage-gated sodium ion (Na+) channels in both native cardiac myocytes and heterologous cells that express sigma-1 receptors. DMT induced hypermobility in wild-type mice but not in sigma-1 receptor knockout mice. These biochemical, physiological, and behavioral experiments indicate that DMT is an endogenous agonist for the sigma-1 receptor. 10.1126/science.1166127 IS - 5916 JF - Science EP - 937 TI - The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator VL - 323 SP - 934 KW - dmt KW - sigma-1 AU - Fontanilla, Dominique AU - Johannessen, Molly AU - Hajipour, Abdol AU - Cozzi, Nicholas AU - Jackson, Meyer AU - Ruoho, Arnold PY - 2009/02/13/ UR - http://dx.doi.org/10.1126/science.1166127 ER -