{"id":473,"date":"2022-09-14T07:18:00","date_gmt":"2022-09-14T14:18:00","guid":{"rendered":"https:\/\/caam.tech\/?p=473"},"modified":"2022-09-13T16:05:42","modified_gmt":"2022-09-13T23:05:42","slug":"caamtech-publishes-fundamental-research-on-aeruginascin-derivatives","status":"publish","type":"post","link":"https:\/\/caam.tech\/caamtech-publishes-fundamental-research-on-aeruginascin-derivatives\/","title":{"rendered":"CaaMTech Publishes Fundamental Research on Aeruginascin Derivatives"},"content":{"rendered":"\n<p>In collaboration with the <a href=\"https:\/\/caam.tech\/caamtech-expands-successful-next-gen-drug-research-collaboration-with-umass-dartmouth\/\">Manke Lab at UMass Dartmouth<\/a> and the <a href=\"https:\/\/caam.tech\/caamtech-collaborates-with-national-institutes-of-health-to-research-psychedelics\/\">Designer Drug Research Unit (DDRU) at the National Institute on Drug Abuse (NIDA) Intramural Research Program (IRP)<\/a>, <a href=\"https:\/\/caam.tech\/\">CaaMTech<\/a> scientists continue to pioneer new fields of \u201cmagic mushroom\u201d research with their latest published academic work, \u201c<a href=\"https:\/\/doi.org\/10.1021\/acsomega.2c03476\">Synthesis, Structural Characterization, and Pharmacological Activity of Novel Quaternary Salts of 4-Substituted Tryptamines<\/a>.\u201d Published in the American Chemical Society\u2019s journal, <em>ACS Omega <\/em>(Structural Chemistry), the multi-disciplinary peer-reviewed research paper builds on the <a href=\"https:\/\/doi.org\/10.1021\/acsomega.0c02208\">researchers\u2019 previous synthesis, structural characterization, and pharmacological screening of aeruginascin\u2019s active metabolite (4-HO-TMT) and a prospective prodrug thereof (4-AcO-TMT)<\/a>.<\/p>\n\n\n\n<p>Psilocybin is the most studied compound in \u201cmagic mushrooms.\u201d now the subject of over 100 clinical trials.&nbsp; But a growing body of evidence indicates that psilocybin is not the only biologically important compound in magic mushrooms. Recent studies have highlighted the prevalence of other, structurally similar tryptamine compounds in magic mushrooms, including baeocystin, norbaeocystin, norpsilocin, aeruginascin, and 4-HO-TMT. Improving our understanding of these lesser-known tryptamines is essential to understanding the pharmacology of magic mushrooms and how it compares to pure psilocybin.&nbsp;&nbsp;<\/p>\n\n\n\n<p>CaaMTech\u2019s latest research broadens the scientific understanding of aeruginascin and 4-HO-TMT by comparing a series of structurally similar compounds, i.e. quaternary tryptammonium compounds, aka \u201cquats,\u201d in an effort to develop a structure activity relationship.&nbsp; The current publication illustrates how small modifications in the chemical structure of these compounds correlate with significant changes in pharmacology.<\/p>\n\n\n\n<p>In the paper, CaaMTech scientists report the synthesis and crystallographic characterization of three quaternary tryptammonium compounds similar in structure to naturally occurring 4-HO-TMT: 4-HO-DMET, 4-HO-DMPT, and 4-HO-DMiPT.\u00a0 The researchers further reported the design, synthesis, and chemical characterization of novel prodrugs for each: 4-AcO-DMET, 4-AcO-DMPT, and 4-AcO-DMiPT, respectively.\u00a0 The researchers then screened the compounds for in vitro pharmacological activity at 46 receptors and transporters. For each compound having substantial binding affinity at a particular receptor, further functional assays were conducted for purposes of measuring agonist potency at 5-HT<sub>1D<\/sub> and 5-HT<sub>2B<\/sub>, as well as uptake inhibition potency at DAT and SERT receptors.<\/p>\n\n\n\n<p>The authors of the paper concluded that for the compounds studied, \u201cthe most substantial binding affinity and noteworthy SAR was observed at SERT.\u201d The data for these compounds further showed that SERT binding affinity and potency for uptake inhibition were both increased by steric bulking of the quaternary ammonium unit.\u00a0Competitive radioligand binding assays also revealed in vitro binding affinity for some of the compounds at 5-HT<sub>1D<\/sub>, 5-HT<sub>2B<\/sub>, and DAT.<\/p>\n\n\n\n<p>\u201cTwo years ago, no one appreciated that aeruginascin was present in magic mushrooms,\u201d explained CaaMTech CEO, Dr. Andrew Chadeayne. \u201cSince then, we\u2019ve found it in the most widespread species [Psilocybe cubensis], highlighting the importance of its pharmacology\u2013and how it might modulate the pharmacology of psilocybin.\u201d<\/p>\n","protected":false},"excerpt":{"rendered":"<p class=\"excerpt\">Aeruginascin is a naturally-occurring quaternary tryptammonium compound found in Magic Mushrooms<\/p>\n","protected":false},"author":5,"featured_media":474,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[5],"tags":[],"acf":[],"_links":{"self":[{"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/posts\/473"}],"collection":[{"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/users\/5"}],"replies":[{"embeddable":true,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/comments?post=473"}],"version-history":[{"count":2,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/posts\/473\/revisions"}],"predecessor-version":[{"id":476,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/posts\/473\/revisions\/476"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/media\/474"}],"wp:attachment":[{"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/media?parent=473"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/categories?post=473"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/caam.tech\/wp-json\/wp\/v2\/tags?post=473"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}