bioRxiv (Cold Spring Harbor Laboratory)
June 30, 2026
Blake A Fordyce, Yi-Ting Chiu, Nicholas A. Wright et al.
Abstract Activation of mGluR2 (metabotropic glutamate receptor 2), the primary presynaptic autoreceptor for glutamate in the brain, is well established to attenuate the psychedelics-mediated behavioral and electrophysiological effects. However, the mechanisms responsible for these actions are controversial. The two competing mechanistic hypotheses have been proposed to explain this phenomenon...
PLoS One
June 14, 2016
Bryan L. Roth, Simon Gibbons, Warunya Arunotayanun et al.
153 citations
In this paper we determined the pharmacological profiles of novel ketamine and phencyclidine analogues currently used as 'designer drugs' and compared them to the parent substances via the resources of the National Institute of Mental Health Psychoactive Drug Screening Program. The ketamine analogues methoxetamine ((RS)-2-(ethylamino)-2-(3-methoxyphenyl)cyclohexanone) and 3-MeO-PCE...
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...
Bioorganic & Medicinal Chemistry Letters
June 1, 2013
Warunya Arunotayanun, Jeffrey W Dalley, Xi-Ping Huang et al.
41 citations
Novel Psychoactive Drugs (NPD) can be sold without restriction and are often synthetic analogues of controlled drugs. The tryptamines are an important class of NPD as they bind to the various serotonin (5-HT) receptor subtypes and cause psychosis and hallucinations that can lead to injury or death through misadventure. Here we report on the structure elucidation and receptor binding profiles of...
Planta Medica
August 1, 2011
JK Zjawiony, PR Polepally, B.l. Roth et al.
10 citations
Psychoactive natural products play an important role in the discovery and development of new drugs for the treatment of central nervous system (CNS) disorders. Our studies are focusing on identification of plant metabolites responsible for CNS activity and designing new ligands with high affinity to CNS receptors. Salvinorin A, the most potent naturally occurring hallucinogen isolated from the...
Journal of Neuroscience
March 12, 2008
Stéphane Doly, Emmanuel Valjent, Vincent Setola et al.
140 citations
The “club drug” 3,4-methylenedioxymethamphetamine (MDMA; also known as ecstasy) binds preferentially to and reverses the activity of the serotonin transporter, causing release of serotonin [5-hydroxytryptamine (5-HT)] stores from nerve terminals. Subsequent activation of postsynaptic 5-HT receptors by released 5-HT has been shown to be critical for the unique psychostimulatory effects of MDMA....