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James A. Golen

21 papers in the library · 268 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 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...

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;...

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...

The fumarate salts of the N-isopropyl-N-methyl derivatives of DMT and psilocin

Acta Crystallographica Section E Crystallographic Communications August 15, 2019 Andrew R Chadeayne, Duyen N. K. Pham, James A. Golen et al. 10 citations

The solid-state structures of the salts of two substituted tryptamines, namely N -isopropyl- N -methyltryptaminium (MiPT) fumarate {systematic name: [2-(1 H -indol-3-yl)ethyl](methyl)propan-2-ylazanium 3-carboxyprop-2-enoate}, C 14 H 21 N 2 + ·C 4 H 3 O 4 − , and 4-hydroxy- N -isopropyl- N -methyltryptaminium (4-HO-MiPT) fumarate monohydrate {systematic name: [2-(4-hydroxy-1 H...

Bis(4-acetoxy-N,N-dimethyltryptammonium) fumarate: a new crystalline form of psilacetin, an alternative to psilocybin as a psilocin prodrug

Acta Crystallographica Section E Crystallographic Communications May 31, 2019 Andrew R Chadeayne, James A. Golen, David R. Manke 20 citations

The title compound (systematic name: bis{2-[4-(acetyloxy)-1 H -indol-3-yl]ethan-1-aminium} but-2-enedioate), 2C 14 H 19 N 2 O 2 + ·C 4 H 2 O 4 2− , has a single protonated psilacetin cation and one half of a fumarate dianion in the asymmetric unit. There are N—H...O hydrogen bonds between the ammonium H atoms and the fumarate O atoms, as well as N—H...O hydrogen bonds between the indole H atoms...