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Andrew R Chadeayne

27 papers in the library · 321 citations · publishing 2019-2026

Papers

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Syntheses and structures of two norpsilocin derivatives: N-ethyl-4-hy-droxy-tryptamine (4-HO-NET) and 4-hy-droxy-N-propyl-tryptamine (4-HO-NPT).

Acta crystallographica. Section E, Crystallographic communications September 1, 2026 Marilyn Naeem, Andrew R Chadeayne, James A Golen et al.

The solid-state structures of N-ethyl-4-hy-droxy-tryptamine (4-HO-NET) {systematic name: 3-[2-(ethyl-amino)-eth-yl]-1H-indol-4-ol}, C12H16N2O, and 4-hy-droxy-N-propyl-tryptamine (4-HO-NPT) {systematic name: 3-[2-(propyl-amino)-eth-yl]-1H-indol-4-ol}, C13H18N2O, are reported. Both compounds possess a single tryptamine mol-ecule in the asymmetric unit that exhibits an inter-nal O-H⋯N hydrogen...

Serotonin Transporter Blockade Reduces the Psychedelic-Like Effects of 4-Methoxy- N -methyl- N -isopropyltryptamine and Related Analogs

ACS Chemical Neuroscience May 27, 2026 Grant C. Glatfelter, Serena S. Schalk, Donna Walther et al.

High Resolution Image Download MS PowerPoint Slide Tryptamine psychedelics induce psychoactive effects via agonist actions at serotonin 2A receptors (5-HT 2A ), but the compounds are generally nonselective. 4-Methoxy- N -methyl- N -isopropyltryptamine (4-MeO-MiPT) is a 5-HT 2A agonist which also blocks the 5-HT transporter (SERT) and has blunted visual and other psychedelic effects in humans....

Specific and Multi‐Product Clade I and Clade IV Sesquiterpene Synthases Contribute to the Psilocybe cubensis Volatilome

ChemBioChem April 1, 2026 Sebastian Schober, Lisa Dorfmann, Karl Walther et al.

Apart from the psychedelic psilocybin, the metabolite spectrum of Psilocybe "magic mushrooms" comprises sesquiterpenes, a class of natural products known to exhibit receptor-modulating bioactivities. However, the composition of the sesquiterpene profile has largely remained an open question. Here, we report the characterization of five Psilocybe cubensis sesquiterpene synthases, both in vitro...

Development and validation of an analytical method for the determination of select 4-position ring-substituted tryptamines in plasma by liquid chromatography–tandem mass spectrometry

Journal of Analytical Toxicology May 26, 2025 Malik Schoffner, Vamshikrishna Reddy Sammeta, Marilyn Naeem et al. 2 citations

Abstract 4-Phosporyloxy-N, N-dimethyltryptamine (psilocybin) is a psychedelic tryptamine found in certain mushroom species that has shown efficacy in the treatment of various psychiatric disorders. In conjunction with the renewed interest in therapeutic effects of psychedelics, there has been an increase in psilocybin-like designer tryptamines appearing in non-medical drug markets. The present...

Clade III Synthases Add Cyclic and Linear Terpenoids to the Psilocybe Metabolome

ChemBioChem May 3, 2025 Nick Zschoche, Markus Gressler, Stefan Bartram et al. 1 citation

Psilocybe “magic mushrooms” are best known for their indolethylamine psilocybin, yet they encode enzymes for a much more diverse arsenal of small and potentially bioactive molecules. Herein, four Psilocybe cubensis clade III sesquiterpene synthases, CubB‐CubE, whose genes are differently expressed in fruiting bodies compared to vegetative mycelium are reported. CubB‐CubE were functionally...

Serotonin 1A Receptors Modulate Serotonin 2A Receptor-Mediated Behavioral Effects of 5-Methoxy-N,N-dimethyltryptamine Analogs in Mice.

ACS Chemical Neuroscience December 18, 2024 Grant C. Glatfelter, Allison A Clark, Natalie G. Cavalco et al. 14 citations

5-methoxy-N,N-dimethyltrytpamine (5-MeO-DMT) analogs are used as recreational drugs, but they are also being developed as potential medicines, warranting further investigation into their pharmacology. Here, we investigated the neuropharmacology of 5-MeO-DMT and several of its N-alkyl, N-allyl, and 2-methyl analogs, with three major aims: 1) to determine in vitro receptor profiles for the...

Bis(4-acetoxy-N-ethyl-N-n-propyltryptammonium) fumarate–fumaric acid (1/1)

IUCrData September 7, 2023 Duyen N. K. Pham, Nathan Sackett, Andrew R Chadeayne et al. 1 citation

The solid-state structure of the title salt/adduct (systemic name: bis{[2-(4-acetyloxy-1 H -indol-3-yl)ethyl](ethyl)propylazanium} but-2-enedioate–( E )-butenedioic acid (1/1)), 2C 17 H 25 N 2 O 2 + ·C 4 H 2 O 4 2− ·C 4 H 4 O 4 , was determined by single-crystal X-ray diffraction. The asymmetric unit consists of a singly protonated tryptammonium cation, one half of a fumarate dianion and one...

A „Magic Mushroom“ Multi‐Product Sesquiterpene Synthase

ChemBioChem August 24, 2023 Eike Schäfer, Stefan Bartram, Felix Trottmann et al. 7 citations

Abstract Psilocybe “magic mushrooms” are chemically well understood for their psychotropic tryptamines. However, the diversity of their other specialized metabolites, in particular terpenoids, has largely remained an open question. Yet, knowledge on the natural product background is critical to understand if other compounds modulate the psychotropic pharmacological effects. CubA, the single...

Receptor Binding Profiles for Tryptamine Psychedelics and Effects of 4-Propionoxy-N,N-dimethyltryptamine in Mice

ACS Pharmacology & Translational Science March 10, 2023 Marilyn Naeem, Grant C. Glatfelter, Duyen N. K. Pham et al. 25 citations

Analogues of 4-phosphoryloxy-N,N-dimethyltryptamine (psilocybin) are being sold on recreational drug markets and developed as potential medications for psychedelic-assisted therapies. Many of these tryptamine-based psilocybin analogues produce psychedelic-like effects in rodents and humans primarily by agonist activity at serotonin 2A receptors (5-HT2A). However, the comprehensive...

Synthesis and structure of 4-hydroxy-N-isopropyltryptamine (4-HO-NiPT) and its precursors

Acta Crystallographica Section E Crystallographic Communications March 10, 2023 U. Laban, Marilyn Naeem, Andrew R Chadeayne et al. 2 citations

The title compound, 4-hydroxy- N -isopropyltryptamine ( 4 ) or 4-HO-NiPT (systematic name: 3-{2-[(propan-2-yl)amino]ethyl}-1 H -indol-4-ol), C 13 H 18 N 2 O, was synthesized in three steps from 4-benzyloxyindole ( 1 ) (systematic name: 4-phenoxy-1 H -indole), C 15 H 13 NO. ( 1 ) was treated with oxalyl chloride and isopropylamine to produce N -isopropyl-4-benzyloxy-3-indoleglyoxylamide ( 2 )...

Structure–Activity Relationships for Psilocybin, Baeocystin, Aeruginascin, and Related Analogues to Produce Pharmacological Effects in Mice

ACS Pharmacology & Translational Science November 2, 2022 Eline Pottie, Marilyn Naeem, Vamshikrishna Reddy Sammeta et al. 91 citations

4-Phosphoryloxy-N,N-dimethyltryptamine (psilocybin) is a naturally occurring tertiary amine found in many mushroom species. Psilocybin is a prodrug for 4-hydroxy-N,N-dimethyltryptamine (psilocin), which induces psychedelic effects via agonist activity at the serotonin (5-HT) 2A receptor (5-HT2A). Several other 4-position ring-substituted tryptamines are present in psilocybin-containing...

The methanol and ethanol solvates of 4-glutarato-N,N-diisopropyltryptamine

Acta Crystallographica Section E: Crystallographic Communications September 22, 2022 Maria Naeem, Barbara E. Bauer, Andrew R Chadeayne et al.

The solid-state structures of two solvated forms of 4-glutarato- N , N -diisopropyltryptamine were determined by single-crystal X-ray diffraction, namely, 5-[(3-{2-[bis(propan-2-yl)azaniumyl]ethyl}-1 H -indol-4-yl)oxy]-5-oxopentanoate methanol monosolvate, C 21 H 30 N 2 O 4 ·CH 3 OH, and the analogous ethanol monosolvate, C 21 H 30 N 2 O 4 ·C 2 H 6 O. In both compounds, the 4-glutarato- N , N...

Synthesis, Structural Characterization, and Pharmacological Activity of Novel Quaternary Salts of 4-Substituted Tryptamines

ACS Omega July 5, 2022 Grant C. Glatfelter, Duyen N. K. Pham, Donna Walther et al. 14 citations

Aeruginascin (4-phosphoryloxy-N,N,N-trimethyltryptammonium) is an analogue of psilocybin (4-phosphoryloxy-N,N-dimethyltryptamine) that has been identified in several species of psilocybin-containing mushrooms. Our team previously reported the synthesis, structural characterization, and biological activity of the putative metabolite of aeruginascin (4-hydroxy-N,N,N-trimethyltryptammonium;...

Genetic Survey of Psilocybe Natural Products

ChemBioChem May 18, 2022 Sebastian Dörner, Kai Rogge, Janis Fricke et al. 43 citations

Abstract Psilocybe magic mushrooms are best known for their main natural product, psilocybin, and its dephosphorylated congener, the psychedelic metabolite psilocin. Beyond tryptamines, the secondary metabolome of these fungi is poorly understood. The genomes of five species ( P. azurescens , P. cubensis , P. cyanescens , P. mexicana , and P. serbica ) were browsed to understand more profoundly...

The crystal structure of baeocystin

Acta Crystallographica Section E Crystallographic Communications May 6, 2022 Marilyn Naeem, Alexander M. Sherwood, Andrew R Chadeayne et al. 5 citations

The title compound, baeocystin or 4-phosphoryloxy- N -methyltryptamine {systematic name: 3-[2-(methylazaniumyl)ethyl]-1 H -indol-4-yl hydrogen phosphate}, C 11 H 15 N 2 O 4 P, has a single zwitterionic molecule in the asymmetric unit. The molecule has an intramolecular N—H...O hydrogen bond between the ammonium cation and the hydrophosphate anion. In the crystal, the molecules are linked by...

5-Methoxy-N,N-di-n-propyltryptamine (5-MeO-DPT): freebase and fumarate

Acta Crystallographica Section E Crystallographic Communications April 13, 2021 Duyen N. K. Pham, Andrew R Chadeayne, James A. Golen et al. 3 citations

The solid-state structures of the synthetic psychedelic 5-methoxy- N , N -di- n -propyltryptamine (5-MeO-DPT) {systematic name: N -[2-(5-methoxy-1 H -indol-3-yl)ethyl]- N -propylpropan-1-amine}, C 17 H 25 N 2 O, and its fumarate salt, bis(5-methoxy- N , N -di- n -propyltryptammonium) fumarate (systematic name: bis{ N -[2-(5-methoxy-1 H -indol-3-yl)ethyl]- N -propylpropan-1-aminium}...

2,5-Dimethylbufotenine and 2,5-dimethylbufotenidine: novel derivatives of natural tryptamines found in Bufo alvarius toads

Acta Crystallographica Section E Crystallographic Communications January 29, 2021 Duyen N. K. Pham, Andrew R Chadeayne, James A. Golen et al. 7 citations

The solid-state structure of the bufotenine derivative bis(5-methoxy-2, N , N -trimethyltryptammonium) (5-MeO-2-Me-DMT) fumarate (systematic name: bis{[2-(5-methoxy-2-methyl-1 H -indol-3-yl)ethyl]dimethylazanium} (2 E )-but-2-enedioate), 2C 14 H 21 N 2 O + ·C 4 H 2 O 4 2− , the bufotenidine derivative 5-methoxy-2, N , N , N -tetramethyltryptammonium (5-MeO-2-Me-TMT) iodide {systematic name:...

Psilacetin derivatives: fumarate salts of the methyl–ethyl, methyl–allyl and diallyl variants of the psilocin prodrug

Acta Crystallographica Section E Crystallographic Communications January 8, 2021 Duyen N. K. Pham, Andrew R Chadeayne, James A. Golen et al. 9 citations

The solid-state structures of the salts of three psilacetin derivatives, namely, 4-acetoxy- N -ethyl- N -methyltryptammonium (4-AcO-MET) hydrofumarate {systematic name: [2-(4-acetyloxy-1 H -indol-3-yl)ethyl](methyl)ethylazanium 3-carboxyprop-2-enoate}, C 15 H 21 N 2 O 2 + ·C 4 H 3 O 4 − , 4-acetoxy- N -allyl- N -methyltryptammonium (4-AcO-MALT) hydrofumarate {systematic name: [2-(4-acetyloxy-1...

The hydrochloride salt of 4-hydroxy-N,N-di-n-propyltryptamine (4-HO-DPT)

IUCrData November 27, 2020 Vamshikrishna Reddy Sammeta, Sivappa Rasapalli, Andrew R Chadeayne et al. 4 citations

The title compound, 4-hydroxy- N , N -di- n -propyltryptammonium (4-HO-DPT) chloride {systematic name: N -[2-(4-hydroxy-1 H -indol-3-yl)ethyl]- N -propylpropan-1-aminium chloride}, C 16 H 25 N 2 O + ·Cl − , has a singly protonated tryptammonium cation and one chloride anion in the asymmetric unit. A series of N—H...Cl and O—H...Cl hydrogen bonds connect the ions together in ladder chains along...

Active Metabolite of Aeruginascin (4-Hydroxy-N,N,N-trimethyltryptamine): Synthesis, Structure, and Serotonergic Binding Affinity

ACS Omega July 2, 2020 Andrew R Chadeayne, Duyen N. K. Pham, Brian G. Reid et al. 31 citations

The putative active metabolite of aeruginascin, a naturally occurring tryptamine of "magic mushrooms," has been synthesized and structurally characterized. Competitive radioligand binding assays demonstrate that it has a high affinity at human serotonin receptors 5-HT1A, 5-HT2A, and 5-HT2B, though it does not bind at the 5-HT3 receptor, where activity was previously predicted.

Norpsilocin: freebase and fumarate salt

Acta Crystallographica Section E Crystallographic Communications March 27, 2020 Andrew R Chadeayne, Duyen N. K. Pham, James A. Golen et al. 13 citations

The solid-state structures of the naturally occurring psychoactive tryptamine norpsilocin {4-hydroxy- N -methyltryptamine (4-HO-NMT); systematic name: 3-[2-(methylamino)ethyl]-1 H -indol-4-ol}, C 11 H 14 N 2 O, and its fumarate salt (4-hydroxy- N -methyltryptammonium fumarate; systematic name: bis{[2-(4-hydroxy-1 H -indol-3-yl)ethyl]methylazanium} but-2-enedioate), C 11 H 15 N 2 O + ·0.5C 4 H 2...

Bis(4-hydroxy-N-isopropyl-N-methyltryptammonium) fumarate: a new crystalline form of miprocin

Acta Crystallographica Section E Crystallographic Communications March 10, 2020 Andrew R Chadeayne, Duyen N. K. Pham, James A. Golen et al. 12 citations

The title compound, bis(4-hydroxy- N -isopropyl- N -methyltryptammonium) (4-HO-MiPT) fumarate (systematic name: bis{[2-(4-hydroxy-1 H -indol-3-yl)ethyl](methyl)propan-2-ylazanium} but-2-enedioate), 2C 14 H 21 N 2 O + ·C 4 H 2 O 4 2− , has a singly protonated tryptammonium cation and one half of a fumarate dianion in the asymmetric unit. The tryptammonium and fumarate ions are held together in...