Important Scientific paper about DMT

http://www.sciencemag.org/cgi/content/abstract/323/5916/934The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor RegulatorDominique Fontanilla,1 Molly Johannessen,2 Abdol R. Hajipour,3 Nicholas V. Cozzi,1 Meyer B. Jackson,2 Arnold E. Ruoho1* 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.1 Department of Pharmacology, University of Wisconsin School of Medicine and Public Health, Madison, WI 53706, USA.2 Department of Physiology, University of Wisconsin School of Medicine and Public Health, Madison, WI 53706, USA.3 Pharmaceutical Research Laboratory, Department of Chemistry, Isfahan University of Technology, Isfahan 84156, IR Iran.* To whom correspondence should be addressed. E-mail: aeruoho@wisc.edu

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