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European journal of medicinal chemistry

ISSN 1768-3254

3 papers in the library · 38 citations · publishing 2014-2025

Papers

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Structural insights into tryptamine psychedelics: The role of hydroxyl indole ring site in 5-HT2A receptor activation and psychedelic-like activity.

European journal of medicinal chemistry January 5, 2025 Miyuan Zhang, Yuefeng Yang, Zhishuai Yang et al. 10 citations

Recent advancements in the study of mushroom-derived tryptamines, particularly psilocybin and its metabolite psilocin, highlight their unique psychedelic properties and potential therapeutic applications, especially for mental health conditions like depression. This study examines how the position of the hydroxyl group on the indole ring affects the 5-HT2A receptor activity and psychedelic-like...

Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.

European journal of medicinal chemistry October 6, 2014 Prabhakar R Polepally, Krzysztof Huben, Eyal Vardy et al. 28 citations

The neoclerodane diterpenoid salvinorin A is a major secondary metabolite isolated from the psychoactive plant Salvia divinorum. Salvinorin A has been shown to have high affinity and selectivity for the κ-opioid receptor (KOR). To study the ligand-receptor interactions that occur between salvinorin A and the KOR, a new series of salvinorin A derivatives bearing potentially reactive Michael...

Molecular basis of the selective binding of MDMA enantiomers to the alpha4beta2 nicotinic receptor subtype: synthesis, pharmacological evaluation and mechanistic studies.

European journal of medicinal chemistry June 23, 2014 Salomé Llabrés, Sara Garcia-Ratés, Edgar Cristóbal-Lecina et al.

The α4β2 nicotinic acetylcholine receptor (nAChR) is a molecular target of 3,4-methylenedioxymethamphetamine (MDMA), a synthetic drug also known as ecstasy, and it modulates the MDMA-mediated reinforcing properties. However, the enantioselective preference of the α4β2 nAChR subtype still remains unknown. Since the two enantiomers exhibit different pharmacological profiles and stereoselective...

DOI: 10.1016/j.ejmech.2014.04.044 (opens in new tab) Full text (opens in new tab) MDMA Alpha4beta2 nicotinic receptor Enantioselective binding Molecular modelling +2