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Literature DB >> 31977208

Identification of Psychoplastogenic N,N-Dimethylaminoisotryptamine (isoDMT) Analogues through Structure-Activity Relationship Studies.

Lee E Dunlap¹, Arya Azinfar¹, Calvin Ly¹, Lindsay P Cameron², Jayashri Viswanathan¹, Robert J Tombari¹, Douglas Myers-Turnbull, Jack C Taylor, Ana Cristina Grodzki³, Pamela J Lein³, David Kokel⁴, David E Olson^1,5,6.

Abstract

Ketamine, N,N-dimethyltryptamine (DMT), and other psychoplastogens possess enormous potential as neurotherapeutics due to their ability to potently promote neuronal growth. Here, we report the first-ever structure-activity relationship study with the explicit goal of identifying novel psychoplastogens. We have discovered several key features of the psychoplastogenic pharmacophore and used this information to develop N,N-dimethylaminoisotryptamine (isoDMT) psychoplastogens that are easier to synthesize, have improved physicochemical properties, and possess reduced hallucinogenic potential as compared to their DMT counterparts.

Entities: Chemical

Mesh：

Substances：

Year: 2020 PMID： 31977208 PMCID： PMC7075704 DOI： 10.1021/acs.jmedchem.9b01404

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

36 in total

1. mTOR-dependent synapse formation underlies the rapid antidepressant effects of NMDA antagonists.

Authors: Nanxin Li; Boyoung Lee; Rong-Jian Liu; Mounira Banasr; Jason M Dwyer; Masaaki Iwata; Xiao-Yuan Li; George Aghajanian; Ronald S Duman
Journal: Science Date: 2010-08-20 Impact factor: 47.728

Review 2. Thinking inside the box. To cope with an increasing disease burden, drug discovery needs biologically relevant and predictive testing systems.

Authors: Lars E Sundstrom
Journal: EMBO Rep Date: 2007-07 Impact factor: 8.807

3. The epidemiology of 5-methoxy- N, N-dimethyltryptamine (5-MeO-DMT) use: Benefits, consequences, patterns of use, subjective effects, and reasons for consumption.

Authors: Alan K Davis; Joseph P Barsuglia; Rafael Lancelotta; Robert M Grant; Elise Renn
Journal: J Psychopharmacol Date: 2018-04-30 Impact factor: 4.153

Review 4. How were new medicines discovered?

Authors: David C Swinney; Jason Anthony
Journal: Nat Rev Drug Discov Date: 2011-06-24 Impact factor: 84.694

5. Ex Vivo Analysis of Tryptophan Metabolism Using ¹⁹F NMR.

Authors: Robert J Tombari; Carla M Saunders; Chun-Yi Wu; Lee E Dunlap; Dean J Tantillo; David E Olson
Journal: ACS Chem Biol Date: 2019-08-26 Impact factor: 5.100

6. Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.

Authors: J B Blair; D Kurrasch-Orbaugh; D Marona-Lewicka; M G Cumbay; V J Watts; E L Barker; D E Nichols
Journal: J Med Chem Date: 2000-11-30 Impact factor: 7.446

7. Effects of N, N-Dimethyltryptamine on Rat Behaviors Relevant to Anxiety and Depression.

Authors: Lindsay P Cameron; Charlie J Benson; Lee E Dunlap; David E Olson
Journal: ACS Chem Neurosci Date: 2018-04-24 Impact factor: 4.418

8. Crystal Structure of an LSD-Bound Human Serotonin Receptor.

Authors: Daniel Wacker; Sheng Wang; John D McCorvy; Robin M Betz; A J Venkatakrishnan; Anat Levit; Katherine Lansu; Zachary L Schools; Tao Che; David E Nichols; Brian K Shoichet; Ron O Dror; Bryan L Roth
Journal: Cell Date: 2017-01-26 Impact factor: 41.582

Review 9. Synaptic dysfunction in depression: potential therapeutic targets.

Authors: Ronald S Duman; George K Aghajanian
Journal: Science Date: 2012-10-05 Impact factor: 47.728

10. Sustained rescue of prefrontal circuit dysfunction by antidepressant-induced spine formation.

Authors: R N Moda-Sava; M H Murdock; P K Parekh; R N Fetcho; B S Huang; T N Huynh; J Witztum; D C Shaver; D L Rosenthal; E J Alway; K Lopez; Y Meng; L Nellissen; L Grosenick; T A Milner; K Deisseroth; H Bito; H Kasai; C Liston
Journal: Science Date: 2019-04-12 Impact factor: 63.714

16 in total

1. Bryostatin 1 Promotes Synaptogenesis and Reduces Dendritic Spine Density in Cortical Cultures through a PKC-Dependent Mechanism.

Authors: Calvin Ly; Akira J Shimizu; Maxemiliano V Vargas; Whitney C Duim; Paul A Wender; David E Olson
Journal: ACS Chem Neurosci Date: 2020-05-21 Impact factor: 4.418

2. Taking the tripping out of psychedelic medicine.

Authors: Elie Dolgin
Journal: Nature Date: 2022-09 Impact factor: 69.504

3. Automated Computer Software Assessment of 5-Hydroxytryptamine 2A Receptor-Mediated Head Twitch Responses from Video Recordings of Mice.

Authors: Grant C Glatfelter; Michael R Chojnacki; Shelby A McGriff; Tianpeng Wang; Michael H Baumann
Journal: ACS Pharmacol Transl Sci Date: 2022-04-08

Identification of Psychoplastogenic N,N-Dimethylaminoisotryptamine (isoDMT) Analogues through Structure-Activity Relationship Studies.

1. mTOR-dependent synapse formation underlies the rapid antidepressant effects of NMDA antagonists.

Review 2. Thinking inside the box. To cope with an increasing disease burden, drug discovery needs biologically relevant and predictive testing systems.

3. The epidemiology of 5-methoxy- N, N-dimethyltryptamine (5-MeO-DMT) use: Benefits, consequences, patterns of use, subjective effects, and reasons for consumption.

Review 4. How were new medicines discovered?

5. Ex Vivo Analysis of Tryptophan Metabolism Using ¹⁹F NMR.

6. Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.

7. Effects of N, N-Dimethyltryptamine on Rat Behaviors Relevant to Anxiety and Depression.

8. Crystal Structure of an LSD-Bound Human Serotonin Receptor.

Review 9. Synaptic dysfunction in depression: potential therapeutic targets.

10. Sustained rescue of prefrontal circuit dysfunction by antidepressant-induced spine formation.

1. Bryostatin 1 Promotes Synaptogenesis and Reduces Dendritic Spine Density in Cortical Cultures through a PKC-Dependent Mechanism.

2. Taking the tripping out of psychedelic medicine.

3. Automated Computer Software Assessment of 5-Hydroxytryptamine 2A Receptor-Mediated Head Twitch Responses from Video Recordings of Mice.

Review 4. Psychedelic-inspired approaches for treating neurodegenerative disorders.

5. Transient Stimulation with Psychoplastogens Is Sufficient to Initiate Neuronal Growth.

6. The Promise of Psychedelic Science.

7. Psychedelic-inspired drug discovery using an engineered biosensor.

Review 8. Biochemical Mechanisms Underlying Psychedelic-Induced Neuroplasticity.

Review 9. The role of serotonin neurotransmission in rapid antidepressant actions.

10. Engineering Safer Psychedelics for Treating Addiction.