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Article ; Online: Synthetic Strategies toward Lysergic Acid Diethylamide: Ergoline Synthesis via α-Arylation, Borrowing Hydrogen Alkylation, and C-H Insertion.

Tuck, Jeremy R / Dunlap, Lee E / Olson, David E

2023 Volume 88, Issue 19, Page(s) 13712–13719

Abstract: Lysergic acid diethylamide (LSD), a semisynthetic ergoline alkaloid analogue and hallucinogen, is a potent psychoplastogen with promising therapeutic potential. While a variety of synthetic strategies for accessing ergoline alkaloids have emerged, the ... ...

Abstract	Lysergic acid diethylamide (LSD), a semisynthetic ergoline alkaloid analogue and hallucinogen, is a potent psychoplastogen with promising therapeutic potential. While a variety of synthetic strategies for accessing ergoline alkaloids have emerged, the complexity of the tetracyclic ring system results in distinct challenges in preparing analogues with novel substitution patterns. Methods of modulating the hallucinogenic activity of LSD by functionalization at previously inaccessible positions are of continued interest, and efficient syntheses of the ergoline scaffold are integral toward this purpose. Here, we report novel C-C bond forming strategies for preparing the ergoline tetracyclic core, focusing on the relatively unexplored strategy of bridging the B- and D-ring systems last. Following cross-coupling to first join the A- and D-rings, we explored a variety of methods for establishing the C-ring, including intramolecular α-arylation, borrowing hydrogen alkylation, and rhodium-catalyzed C-H insertion. Our results led to a seven-step formal synthesis of LSD and the first methods for readily introducing substitution on the C-ring. These strategies are efficient for forming ergoline-like tetracyclic compounds and analogues, though they each face unique challenges associated with elaboration to ergoline natural products. Taken together, these studies provide important insights that will guide future synthetic strategies toward ergolines.
MeSH term(s)	Ergolines ; Lysergic Acid Diethylamide ; Hydrogen/chemistry ; Alkaloids ; Alkylation
Chemical Substances	Ergolines ; Lysergic Acid Diethylamide (8NA5SWF92O) ; Hydrogen (7YNJ3PO35Z) ; Alkaloids
Language	English
Publishing date	2023-09-11
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S.
ZDB-ID	123490-0
ISSN	1520-6904 ; 0022-3263
ISSN (online)	1520-6904
ISSN	0022-3263
DOI	10.1021/acs.joc.3c01363
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 4473: Show issues

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Article: Reaction of

Dunlap, Lee E / Olson, David E

ACS omega

2018 Volume 3, Issue 5, Page(s) 4968–4973

Abstract: A large number of clinically used drugs and experimental pharmaceuticals possess ... ...

Abstract	A large number of clinically used drugs and experimental pharmaceuticals possess the
Language	English
Publishing date	2018-05-07
Publishing country	United States
Document type	Journal Article
ISSN	2470-1343
ISSN	2470-1343
DOI	10.1021/acsomega.8b00507
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Article ; Online: Developmental Neurotoxicity Screen of Psychedelics and Other Drugs of Abuse in Larval Zebrafish (

Tombari, Robert J / Mundy, Paige C / Morales, Kelly M / Dunlap, Lee E / Olson, David E / Lein, Pamela J

ACS chemical neuroscience

2023 Volume 14, Issue 5, Page(s) 875–884

Abstract: In recent years, psychedelics have garnered significant interest as therapeutic agents for treating diverse neuropsychiatric disorders. However, the potential for these compounds to produce developmental neurotoxicity has not been rigorously assessed, ... ...

Abstract	In recent years, psychedelics have garnered significant interest as therapeutic agents for treating diverse neuropsychiatric disorders. However, the potential for these compounds to produce developmental neurotoxicity has not been rigorously assessed, and much of the available safety data is based on epidemiological studies with limited experimental testing in laboratory animal models. Moreover, the experimental safety data available thus far have focused on adult organisms, and the few studies conducted using developing organisms have tested a limited number of compounds, precluding direct comparisons between various chemical scaffolds. In the present study, 13 psychoactive compounds of different chemical or pharmacological classes were screened in a larval zebrafish model for teratological and behavioral abnormalities following acute and chronic developmental exposures. We found that the psychedelic tryptamines and ketamine were less neurotoxic to larval zebrafish than LSD and psychostimulants. Our work, which leverages the advantage of using zebrafish for higher throughput toxicity screening, provides a robust reference database for comparing the neurotoxicity profiles of novel psychedelics currently under development for therapeutic applications.
MeSH term(s)	Animals ; Hallucinogens/toxicity ; Zebrafish ; Larva ; Ketamine ; Models, Animal
Chemical Substances	Hallucinogens ; Ketamine (690G0D6V8H)
Language	English
Publishing date	2023-02-08
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.2c00642
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: A mouse model of Zhu-Tokita-Takenouchi-Kim syndrome reveals indispensable SON functions in organ development and hematopoiesis.

Vukadin, Lana / Park, Bohye / Mohamed, Mostafa / Li, Huashi / Elkholy, Amr / Torrelli-Diljohn, Alex / Kim, Jung-Hyun / Jeong, Kyuho / Murphy, James M / Harvey, Caitlin A / Dunlap, Sophia / Gehrs, Leah / Lee, Hanna / Kim, Hyung-Gyoon / Sah, Jay Prakash / Lee, Seth N / Stanford, Denise / Barrington, Robert A / Foote, Jeremy B /

Sorace, Anna G / Welner, Robert S / Hildreth, Blake E / Lim, Ssang-Taek Steve / Ahn, Eun-Young Erin

JCI insight

2024 Volume 9, Issue 5

Abstract: Rare diseases are underrepresented in biomedical research, leading to insufficient awareness. Zhu-Tokita-Takenouchi-Kim (ZTTK) syndrome is a rare disease caused by genetic alterations that result in heterozygous loss of function of SON. While patients ... ...

Abstract	Rare diseases are underrepresented in biomedical research, leading to insufficient awareness. Zhu-Tokita-Takenouchi-Kim (ZTTK) syndrome is a rare disease caused by genetic alterations that result in heterozygous loss of function of SON. While patients with ZTTK syndrome live with numerous symptoms, the lack of model organisms hampers our understanding of SON and this complex syndrome. Here, we developed Son haploinsufficiency (Son+/-) mice as a model of ZTTK syndrome and identified the indispensable roles of Son in organ development and hematopoiesis. Son+/- mice recapitulated clinical symptoms of ZTTK syndrome, including growth retardation, cognitive impairment, skeletal abnormalities, and kidney agenesis. Furthermore, we identified hematopoietic abnormalities in Son+/- mice, including leukopenia and immunoglobulin deficiency, similar to those observed in human patients. Surface marker analyses and single-cell transcriptome profiling of hematopoietic stem and progenitor cells revealed that Son haploinsufficiency shifted cell fate more toward the myeloid lineage but compromised lymphoid lineage development by reducing genes required for lymphoid and B cell lineage specification. Additionally, Son haploinsufficiency caused inappropriate activation of erythroid genes and impaired erythropoiesis. These findings highlight the importance of the full gene expression of Son in multiple organs. Our model serves as an invaluable research tool for this rare disease and related disorders associated with SON dysfunction.
MeSH term(s)	Animals ; Humans ; Mice ; Gene Expression Profiling ; Hematopoiesis/genetics ; Mutation ; Rare Diseases
Chemical Substances	Son protein, mouse
Language	English
Publishing date	2024-03-08
Publishing country	United States
Document type	Journal Article
ISSN	2379-3708
ISSN (online)	2379-3708
DOI	10.1172/jci.insight.175053
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Two-Year Tumor Outcomes of a Phase 2B, Randomized, Double-Blind Trial of Avasopasem Manganese (GC4419) Versus Placebo to Reduce Severe Oral Mucositis Owing to Concurrent Radiation Therapy and Cisplatin for Head and Neck Cancer.

Anderson, Carryn M / Lee, Christopher M / Saunders, Deborah / Curtis, Amarinthia E / Dunlap, Neal E / Nangia, Chaitali / Lee, Arielle S / Kovoor, Philip / Bar-Ad, Voichita / Pedadda, Abhinand V / Holmlund, Jon / Downs, Matt / Sonis, Stephen T

International journal of radiation oncology, biology, physics

2022 Volume 114, Issue 3, Page(s) 416–421

Abstract: Purpose: Avasopasem manganese (GC4419), an investigational selective dismutase mimetic radioprotector, reduced duration, incidence, and severity of severe oral mucositis (World Health Organization grade 3-4) in a phase 2b, randomized, double-blind trial ...

Abstract	Purpose: Avasopasem manganese (GC4419), an investigational selective dismutase mimetic radioprotector, reduced duration, incidence, and severity of severe oral mucositis (World Health Organization grade 3-4) in a phase 2b, randomized, double-blind trial of patients receiving concurrent cisplatin (cis) and radiation therapy (RT) for head and neck cancer. We report the secondary endpoints of final 1- and 2-year tumor outcomes and exploratory data on trismus and xerostomia. Methods and materials: Patients with locally advanced oral cavity or oropharynx cancer to be treated with definitive or postop cis and RT were randomized to 1 of 3 arms: 30 mg avasopasem, 90 mg avasopasem, or placebo. Pairwise comparisons of Kaplan-Meier estimates (each active arm separately vs placebo) were made for overall survival, progression-free survival, locoregional control, and distant metastasis-free survival. Xerostomia and trismus data were collected at each follow-up visit and analyzed for trends by post-RT timepoint and treatment group. Results: At a median follow-up for the entire cohort of 25.5 months (25th-75th percentile, 24.6-26.2 months; range, 0.2-31.9 months), Kaplan-Meier estimates of 1- and 2-year overall survival, progression-free survival, locoregional control, and distant metastasis-free survival were not statistically different. No trends were apparent in xerostomia or trismus data. Conclusions: Avasopasem does not lead to statistically different tumor control outcomes when used concurrently with cis and RT for head and neck cancer. There was no detectable effect on trismus or xerostomia.
MeSH term(s)	Cisplatin/adverse effects ; Head and Neck Neoplasms/drug therapy ; Head and Neck Neoplasms/radiotherapy ; Humans ; Organometallic Compounds ; Stomatitis/etiology ; Stomatitis/prevention & control ; Trismus/etiology ; Trismus/prevention & control ; Xerostomia/etiology ; Xerostomia/prevention & control
Chemical Substances	Organometallic Compounds ; avasopasem manganese (EY1WA413UL) ; Cisplatin (Q20Q21Q62J)
Language	English
Publishing date	2022-06-17
Publishing country	United States
Document type	Journal Article ; Randomized Controlled Trial ; Research Support, Non-U.S. Gov't
ZDB-ID	197614-x
ISSN	1879-355X ; 0360-3016
ISSN (online)	1879-355X
ISSN	0360-3016
DOI	10.1016/j.ijrobp.2022.06.063
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Zs.A 1218: Show issues

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ab Jg. 2022: Lesesaal (EG)

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Article ; Online: Dark Classics in Chemical Neuroscience: 3,4-Methylenedioxymethamphetamine.

Dunlap, Lee E / Andrews, Anne M / Olson, David E

ACS chemical neuroscience

2018 Volume 9, Issue 10, Page(s) 2408–2427

Abstract: Better known as "ecstasy", 3,4-methylenedioxymethamphetamine (MDMA) is a small molecule that has played a prominent role in defining the ethos of today's teenagers and young adults, much like lysergic acid diethylamide (LSD) did in the 1960s. Though MDMA ...

Abstract	Better known as "ecstasy", 3,4-methylenedioxymethamphetamine (MDMA) is a small molecule that has played a prominent role in defining the ethos of today's teenagers and young adults, much like lysergic acid diethylamide (LSD) did in the 1960s. Though MDMA possesses structural similarities to compounds like amphetamine and mescaline, it produces subjective effects that are unlike any of the classical psychostimulants or hallucinogens and is one of the few compounds capable of reliably producing prosocial behavioral states. As a result, MDMA has captured the attention of recreational users, the media, artists, psychiatrists, and neuropharmacologists alike. Here, we detail the synthesis of MDMA as well as its pharmacology, metabolism, adverse effects, and potential use in medicine. Finally, we discuss its history and why it is perhaps the most important compound for the future of psychedelic science-having the potential to either facilitate new psychedelic research initiatives, or to usher in a second Dark Age for the field.
MeSH term(s)	Hallucinogens/chemistry ; Hallucinogens/history ; Hallucinogens/pharmacology ; Hallucinogens/therapeutic use ; History, 20th Century ; History, 21st Century ; Humans ; N-Methyl-3,4-methylenedioxyamphetamine/chemistry ; N-Methyl-3,4-methylenedioxyamphetamine/history ; N-Methyl-3,4-methylenedioxyamphetamine/pharmacology ; N-Methyl-3,4-methylenedioxyamphetamine/therapeutic use
Chemical Substances	Hallucinogens ; N-Methyl-3,4-methylenedioxyamphetamine (KE1SEN21RM)
Language	English
Publishing date	2018-07-12
Publishing country	United States
Document type	Historical Article ; Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Review
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.8b00155
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Medical Societies Must Choose Professional Meeting Locations Responsibly in a Post-

Lee, Alison G / Maley, Jason / Hibbert, Kathryn / Akgün, Kathleen M / Hauschildt, Katrina E / Law, Anica / Kaminski, Naftali / Hayes, Margaret / Gesthalter, Yaron / Bosslet, Gabriel T / Santhosh, Lekshmi / Witkin, Alison / Hills-Dunlap, Kelsey / Çoruh, Başak / Gershengorn, Hayley B / Hardin, C Corey

Annals of the American Thoracic Society

2023 Volume 20, Issue 6, Page(s) 781–784

MeSH term(s)	Humans ; Societies, Medical/ethics ; Supreme Court Decisions ; Congresses as Topic/ethics
Language	English
Publishing date	2023-02-24
Publishing country	United States
Document type	Journal Article
ZDB-ID	2717461-X
ISSN	2325-6621 ; 1943-5665 ; 2325-6621
ISSN (online)	2325-6621 ; 1943-5665
ISSN	2325-6621
DOI	10.1513/AnnalsATS.202211-928IP
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Zs.A 5828: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

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Article ; Online: Reaction of N,N‑Dimethyltryptamine with Dichloromethane Under Common Experimental Conditions

Lee E. Dunlap / David E. Olson

ACS Omega, Vol 3, Iss 5, Pp 4968-

2018 Volume 4973

Keywords	Chemistry ; QD1-999
Language	English
Publishing date	2018-05-01T00:00:00Z
Publisher	American Chemical Society
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: A mouse model of ZTTK syndrome reveals indispensable SON functions in organ development and hematopoiesis.

bioRxiv : the preprint server for biology

2023

Abstract	Rare diseases are underrepresented in biomedical research, leading to insufficient awareness. Zhu-Tokita-Takenouchi-Kim (ZTTK) syndrome is a rare disease caused by genetic alterations that result in heterozygous loss-of-function of SON. While ZTTK syndrome patients suffer from numerous symptoms, the lack of model organisms hamper our understanding of both SON and this complex syndrome. Here, we developed
Language	English
Publishing date	2023-11-19
Publishing country	United States
Document type	Preprint
DOI	10.1101/2023.11.19.567732
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Effects of N, N-Dimethyltryptamine on Rat Behaviors Relevant to Anxiety and Depression.

Cameron, Lindsay P / Benson, Charlie J / Dunlap, Lee E / Olson, David E

ACS chemical neuroscience

2018 Volume 9, Issue 7, Page(s) 1582–1590

Abstract: Depression and anxiety disorders are debilitating diseases resulting in substantial economic costs to society. Traditional antidepressants often take weeks to months to positively affect mood and are ineffective for about 30% of the population. ... ...

Abstract	Depression and anxiety disorders are debilitating diseases resulting in substantial economic costs to society. Traditional antidepressants often take weeks to months to positively affect mood and are ineffective for about 30% of the population. Alternatives, such as ketamine, a dissociative anesthetic capable of producing hallucinations, and the psychoactive tisane ayahuasca, have shown great promise due to their fast-acting nature and effectiveness in treatment-resistant populations. Here, we investigate the effects of N, N-dimethyltryptamine (DMT), the principle hallucinogenic component of ayahuasca, in rodent behavioral assays relevant to anxiety and depression using adult, male, Sprague-Dawley rats. We find that while DMT elicits initial anxiogenic responses in several of these paradigms, its long-lasting effects tend to reduce anxiety by facilitating the extinction of cued fear memory. Furthermore, DMT reduces immobility in the forced swim test, which is a characteristic behavioral response induced by many antidepressants. Our results demonstrate that DMT produces antidepressant and anxiolytic behavioral effects in rodents, warranting further investigation of ayahuasca and classical psychedelics as treatments for depression and post-traumatic stress disorder.
MeSH term(s)	Animals ; Anti-Anxiety Agents/pharmacology ; Antidepressive Agents/pharmacology ; Anxiety Disorders/drug therapy ; Conditioning, Psychological/drug effects ; Depressive Disorder/drug therapy ; Disease Models, Animal ; Exploratory Behavior/drug effects ; Fear/drug effects ; Feeding Behavior/drug effects ; Male ; Motor Activity/drug effects ; N,N-Dimethyltryptamine/pharmacology ; Rats, Inbred SHR
Chemical Substances	Anti-Anxiety Agents ; Antidepressive Agents ; N,N-Dimethyltryptamine (WUB601BHAA)
Language	English
Publishing date	2018-04-24
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.8b00134
Database	MEDical Literature Analysis and Retrieval System OnLINE

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