Alexander Shulgin Research Institute

Publications

Publications

ASRI scientists publish their work in the world’s leading research and medical journals.
  1. N-(4-Bromo-2,5-dimethoxyphenethyl)-6-(4-phenylbutoxy)hexan-1-amine (XOB): a novel phenylalkylamine antagonist of serotonin 2A receptors and voltage-gated sodium channels. N Denomme, CC Hernandez, HA Bock, RF Ohana, AM Sherwood, JD McCorvy, PF Daley, WB Callaway, JM Hull, A Alt LL Isom, NV Cozzi. Mol. Pharmacol., 106, 92-106 (2024). DOI: 10.1124/molpharm.123.000837
  2. Psilocybin pulse regimen reduces cluster headache attack frequency in the blinded extension phase of a randomized controlled trial. EAD Schindler, RA Sewell, CH Gottschalk, LT Flynn, Y Zhu, BP Pittman, NV Cozzi, DC D’Souza. J. Neurol. Sci., 460, 122993-12300 (2024). DOI: 10.1016/j.jns.2024.122993.
  3. The origin of 2,5-dimethoxy-4-methylamphetamine (DOM, STP). K Trout, PF Daley. Drug Test. Anal., (2024). DOI: 10.1002/dta.3667
  4. A matter of mass. KF Foley, NV Cozzi, PF Daley. J. Appl. Lab. Med., 8, 990-992 (2023). DOI: 10.1093/jalm/jfad037
  5. Exploratory investigation of a patient-informed low dose psilocybin pulse regimen in the suppression of cluster headache: Results from a randomized, double-blind, placebo-controlled trial. EAD Schindler, RA Sewell, CH Gottschalk, C Luddy, LT Flynn, Y Zhu, H Lindsey, BP Pittman, NV Cozzi, DC D’Souza. Headache, 62, 1383-1394 (2022). DOI: 10.1111/head.14420
  6. Exploratory study of the dose-related safety, tolerability, andefficacy of dimethyltryptamine (DMT) in healthy volunteers and major depressive disorder. DC D’Souza, SA Syed, LT Flynn, H Safi-Aghdam, NV Cozzi, M Ranganathan. Neuropsychopharmacology, 47, 1854-1862 (2022). DOI: 10.1038/s41386-022-01344-y
  7. Psilocybin: crystal structure solutions enable phase analysis of prior art and recently patented examples. AM Sherwood, RB Kargbo, KW Kaylo, NV Cozzi, P Meisenheimer, JA Kaduk.  Acta Crystallogr., Sect. C: Cryst. Struct. Commun., 78, 36-55 (2022). DOI: 10.1107/S2053229621013164
  8. N,N-Dimethyltryptamine attenuates spreading depolarization and restrains neurodegeneration by sigma-1 receptor activation in the ischemic rat brain. Í Szabó, VÉ Varga, S Dvorácskó, AE Farkas, T Körmöczi, R Berkecz, S. Kecskés, Á Menyhárt, R Frank, D Hantosi, NV Cozzi, E Frecska, C Tömböly, IA Krizbai, F Bari, E Farkas. Neuropharmacology, 192, 108612 (2021). DOI: 10.1016/j.neuropharm.2021.108612
  9. Exploratory controlled study of the migraine-suppressing effects of psilocybin. EAD Schindler, RA Sewell, CH Gottschalk, C Luddy, LT Flynn, H Lindsey, BP Pittman, NV Cozzi, DC D’Souza. Neurotherapeutics, 18, 534-543 (2021). DOI:10.1007/s13311-020-00962-y
  10. Synthesis and characterization of high-purity DMT hemifumarate for human clinical trials. NV Cozzi, PF Daley. Drug Test. Anal., 12, 1483-1493 (2020). DOI:10.1002/dta.2889
  11. Direct phosphorylation of psilocin enables optimized cGMP kilogram-scale manufacture of psilocybin. R Kargbo, A Sherwood, A Walker, NV Cozzi, RE Dagger, J Sable, K O’Hern, K Kaylo, T Patterson, G Tarpley, P Meisenheimer. ACS Omega, 5, 16959-16966 (2020). DOI:10.1021/acsomega.0c02387
  12. para-Trifluoromethyl-methcathinone is an allosteric modulator of the serotonin transporter. M Niello, D Cintulova, E Hellsberg, K Jäntsch, M Holy, LH Ayatollahi, NV Cozzi, M Freissmuth, W Sandtner, GF Ecker, MD Mihovilovic, HH Sitte. Neuropharmacology, 161, 107615-107626 (2019). DOI:10.1016/j.neuropharm.2019.04.021
  13. High dose psilocybin is associated with positive subjective effects. CR Nicholas, KM Henriquez, MC Gassman, KM Cooper, D Muller, S Hetzel, RT Brown, NV Cozzi, C Thomas, PR Hutson. J. Psychopharmacol., 32, 770-778 (2018). DOI:10.1177/0269881118780713
  14. Receptor binding profiles and behavioral pharmacology of ring-substituted N,N-diallyltryptamine analogs. LM Klein, NV Cozzi, PF Daley, SD Brandt, AL Halberstadt. Neuropharmacology, 142, 231-239 (2018). DOI:10.1016/j.neuropharm.2018.02.028
  15. Pharmacokinetics of ecalating doses of oral psilocybin in healthy adults. RT Brown, CR Nicholas, NV Cozzi, MC Gassman, KM Cooper, D Muller, CD Thomas, SJ Hetzel, KM Henriquez, AS Ribaudo, PR Hutson. Clin. Pharmacokinet., 56, 1543-1554 (2017). DOI:10.1007/s40262-017-0540-6
  16. Atypical dopamine efflux caused by 3,4-methylenedioxypyrovalerone (MDPV) via the human dopamine transporter. A Shekar, JI Aguilar, G Galli, NV Cozzi, SD Brandt, AE Ruoho, MH Baumann, HJG Matthies, A Galli. J. Chem. Neuroanat., 83-84, 69-74 (2017). DOI:10.1016/j.jchemneu.2017.01.004
  17. Combined simulation and mutation studies to elucidate selectivity of unsubstituted amphetamine-like cathinones at the dopamine transporter. A Seddik, DP Geerke, T Stockner, M Holy, O Kudlacek, NV Cozzi, AE Ruoho, HH Sitte, GF Ecker. Mol. Inform., 36, 5-6, (2017). DOI:10.1002/minf.201600094
  18. Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. NV Cozzi, PF Daley. Bioorg. Med. Chem. Lett., 26, 959-964 (2016). DOI:10.1016/j.bmcl.2015.12.053
  19. Reinforcing and neurochemical effects of the “bath salts” constituents 3,4-methylenedioxypyrovalerone (MDPV) and 3,4-methylenedioxy-N-methylcathinone (methylone) in male rats. CW Schindler, EB Thorndike, S Goldberg, KR Lehner, NV Cozzi, SD Brandt, MH Baumann. Psychopharmacology, 233, 1981-1990 (2016). DOI:10.1007/s00213-015-4057-0
  20. Quantitative structure-activity relationship analysis of the pharmacology of para-substituted methcathinone analogues. JS Bonano, ML Banks, R Kolanos, F Sakloth, M Barnier, RA Glennon, NV Cozzi, JS Partilla, MH Baumann, SS Negus. Brit. J. Pharmacol., 172, 2433-2444 (2015). DOI:10.1111/bph.13030
  21. Noncompetitive inhibition of indolethylamine-N-methyltransferase by N,N-dimethyltryptamine and N,N-dimethylaminopropyltryptamine. UB Chu, S Vorperian, K Satyshur, K Eickstaedt, NV Cozzi, AR Hajipour, AE Ruoho. Biochemistry, 53, 2956-2965 (2014). DOI:10.1021/bi500175p
  22. Radiotracers for cardiac sympathetic innervation: transport kinetics and binding affinities for the human norepinephrine transporter. DM Raffel, W Chen, Y-W Jung, K-S Jang, G Gua, NV Cozzi. Nucl. Med. Biol., 40, 331-337 (2013). DOI:10.1016/j.nucmedbio.2012.11.014
  23. Pharmacological examination of trifluoromethyl ring-substituted methcathinone analogs. NV Cozzi, SD Brandt, PF Daley, JS Partilla, RB Rothman, A Tulzer, HH Sitte, MH Baumann. Eur. J. Pharmacol., 699, 180-187 (2013). DOI:10.1016/j.ejphar.2012.11.008
  24. Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive “bath salts” products. MH Baumann, JS Partilla, KR Lehner, EB Thorndike, AF Hoffman, M Holy, RB Rothman, SR Goldberg, CR Lupica, HH Sitte, SD Brandt, SR Tella, NV Cozzi, CW Schindler. Neuropsychopharmacology, 38, 552-562 (2013). DOI:10.1038/npp.2012.204
  25. Analytical characterization of three trifluoromethyl-substituted methcathinone isomers. SD Brandt, PF Daley, NV Cozzi. Drug Test. Anal., 4, 525-529 (2012). DOI:10.1002/dta.382
  26. Synthesis and characterization of 5-methoxy-2-methyl-N,N-dialkylated tryptamines. SD Brandt, R Tearavarich, N Dempster, NV Cozzi, PF Daley. Drug Test. Anal., 4, 24-32 (2012). DOI:10.1002/dta.398
  27. The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissue. MH Baumann, MA Ayestas, JS Partilla, JL Sink, AT Shulgin, PF Daley, SD Brandt, RB Rothman, AE Ruoho, NV Cozzi. Neuropsychopharmacology, 37, 1192-1203 (2012). DOI:10.1038/npp.2011.304
  28. Microwave-accelerated preparation and analytical characterization of 5-ethoxy-N,N-dialkyl-[α,α,β,β-H4]- and [α,α,β,β-D4]-tryptamines. R Tearavarich, V Hahnvajanawong, N Dempster, PF Daley, NV Cozzi, SD Brandt. Drug Test. Anal., 3, 597‑608 (2011). DOI:10.1002/dta.223
  29. Clinal geographic variation in mescaline concentration among Texas populations of Lophophora williamsii (Cactaceae). D Hulsey, MA Kalam, PF Daley, N Fowler, M Terry. J. Bot. Res. Inst. Texas 5, 677-683 (2011)
  30. New mescaline concentrations from 14 taxa-cultivars of Echinopsis spp. (Cactaceae)(‘San Pedro’) and their relevance to shamanic practice. O Ogunbodede, D McCombs, K Trout, PF Daley,  M Terry. J. Ethnopharmacology, 131, 356-362 (2010). DOI:10.1016/j.jep.2010.07.021
  31. Dimethyltryptamine and other hallucinogenic tryptamines exhibit substrate behavior at the serotonin uptake transporter and the vesicle monoamine transporter. NV Cozzi, A Gopalakrishnan, LL Anderson, JT Feih, AT Shulgin, PF Daley, AE Ruoho. J. Neural Transm., 116, 1591-1599 (2009). DOI:10.1007/s00702-009-0308-8
  32. The hallucinogen N,N-dimethyltryptamine (DMT) is an endogenous sigma-1 receptor regulator. D Fontanilla, M Johannessen, AR Hajipour, NV Cozzi, MB Jackson, AE Ruoho. Science, 323, 934-937 (2009). DOI:10.1126/science.1166127
  33. Psychoactive N,N-dialkyltryptamines modulate serotonin transport by at least two mechanisms. NV Cozzi, AT Shulgin, PF Daley, A Gopalakrishnan, LL Anderson, JT Feih, AE Ruoho. Soc. Neurosci. Abs., 34, 536.17 (2008)
  34. Microwave-accelerated synthesis of psychoactive deuterated N,N-dialkylated-[α,α,β,β-D4]-tryptamines. SD Brandt, SS Tirunarayanapuram, S Freeman, N Dempster, SA Barker, PF Daley, NV Cozzi, CPB Martins. J. Label. Compd. Radiopharm., 51, 423-429 (2008). DOI:10.1002/jlcr.1557
  35. Synthesis and biological evaluation of 2-(4-fluorophenoxy)-2-phenyl-ethyl piperazines as serotonin-selective reuptake inhibitors with a potentially improved adverse reaction profile. JM Dorsey, MG Miranda, NV Cozzi, KG Pinney. Bioorg. Med. Chem., 12, 1483-1491 (2004). DOI:10.1016/j.bmc.2003.12.021
  36. Methcathinone is a substrate for the serotonin uptake transporter. NV Cozzi, KF Foley. Pharmacol. Toxicol., 93, 219-225 (2003). DOI:10.1046/j.1600-0773.2003.pto930504.x
  37. Novel aminopropiophenones as potential antidepressants. KF Foley, NV Cozzi. Drug Dev. Res., 60, 252-260 (2003). DOI:10.1002/ddr.10297
  38. Stereospecific inhibition of monoamine uptake transporters by meta-hydroxyephedrine isomers. KF Foley, ME Van Dort, MK Sievert, AE Ruoho, NV Cozzi. J. Neural Transm., 109, 1229-1240 (2002). DOI:10.1007/s00702-002-0695-6
  39. Inhibition of transport function and desipramine binding at the human noradrenaline transporter by N-ethylmaleimide and protection by substrate analogs. KF Foley, NV Cozzi. Naunyn-Schmiedeberg’s Arch. Pharmacol., 365, 457-461 (2002). DOI:10.1007/s00210-002-0532-3
  40. Rapid and efficient method for suspending cells for neurotransmitter uptake assays. NV Cozzi, KF Foley. Biotechniques, 32, 486-492 (2002). DOI:10.2144/02323bm03
  41. Inhibition of plasma membrane monoamine transporters by β-ketoamphetamines. NV Cozzi, MK Sievert, AT Shulgin, P Jacob III, AE Ruoho. Eur. J. Pharmacol., 381, 63-69 (1999). DOI:10.1016/S0014-2999(99)00538-5
  42. Methcathinone and 2-methylamino-1-(3,4-methylenedioxyphenyl)propan-1-one (methylone) selectively inhibit plasma membrane catecholamine reuptake transporters. NV Cozzi, MK Sievert, AT Shulgin, P Jacob III, AE Ruoho. Soc. Neurosci. Abs., 24, 341.8 (1998)
  43. Methcathinone (MCAT) and 2-methylamino-1-(3,4-methylenedioxy-phenyl)propan-1-one (MDMCAT) inhibit [3H]serotonin uptake into human platelets. NV Cozzi, AT Shulgin, AE Ruoho. Amer. Chem. Soc. Div. Med. Chem. Abs., 215, 152 (1998)
  44. Conformationally restricted tetrahydro-1-benzoxepin analogs of hallucinogenic phenethylamines. AP Monte, D Marona-Lewicka, NV Cozzi, DL Nelson, DE Nichols.  Med. Chem. Res. 5, 651-663 (1995). DOI:10.1002/chin.199621182.
  45. Synthesis and pharmacological examination of benzofuran, indan, and tetralin analogs of 3,4‑(methylenedioxy)amphetamine. AP Monte, D Marona-Lewika, NV Cozzi, DE Nichols.  J. Med. Chem., 36, 3700-3706 (1993). DOI:10.1021/jm00075a027.
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