Yong Sup Lee - The Consciousness Library

Enhanced dopamine transporter binding is associated with species-specific 2C-B-induced reinforcement in marmosets, but not in mice

Biomedicine & Pharmacotherapy July 29, 2026 Yong-Qing Zhang, Hyeokjun Kwon, Taeyun Yoo et al.

Hallucinogens have been prescribed for the treatment of mental illnesses; however, reports on the dependence potential of hallucinogens across species remain inconsistent. Non-human primate (NHP) self-administration model are suitable for evaluating species-specific reinforcement behavior induced by hallucinogens. In this study, we demonstrated that 4-bromo-2,5-dimethoxyphenethylamine (2C-B)...

DOI: 10.1016/j.biopha.2026.119773

Serotonin 2C receptors are also important in head-twitch responses in male mice.

Psychopharmacology July 1, 2025 Raly James Perez Custodio, Darlene Mae Ortiz, Hyun Jun Lee et al. 8 citations

Serotonergic psychedelics exert their effects via their high affinity for serotonin (5-HT) receptors, particularly through activating 5-HT2A receptors (5-HT2AR), employing the frontal cortex-dependent head-twitch response (HTR). Although universally believed to be so, studies have not yet fully ascertained whether 5-HT2AR activation is the sole initiator of these psychedelic effects. This is...

DOI: 10.1007/s00213-023-06482-9 Full text Mescaline Bod Head-twitch response Inflammation +3

Deletion of Cryab increases the vulnerability of mice to the addiction-like effects of the cannabinoid JWH-018 via upregulation of striatal NF-κB expression

Frontiers in Pharmacology March 16, 2023 Leandro Val Sayson, Darlene Mae Ortiz, Hyun Jun Lee et al. 4 citations

Synthetic cannabinoids have exhibited unpredictable abuse liabilities, especially self-administration (SA) responses in normal rodent models, despite seemingly inducing addiction-like effects in humans. Thus, an efficient pre-clinical model must be developed to determine cannabinoid abuse potential in animals and describe the mechanism that may mediate cannabinoid sensitivity. The Cryab...

DOI: 10.3389/fphar.2023.1135929 Addiction Synaptic plasticity Conditioned place preference Neuroinflammation +11

4-F-PCP, a Novel PCP Analog Ameliorates the Depressive-Like Behavior of Chronic Social Defeat Stress Mice via NMDA Receptor Antagonism

Biomolecules & Therapeutics February 15, 2023 Darlene Mae Ortiz, Mikyung Kim, Hyun Jun Lee et al. 3 citations

Major depressive disorder is a leading cause of disability in more than 280 million people worldwide. Monoamine-based antidepressants are currently used to treat depression, but delays in treatment effects and lack of responses are major reasons for the need to develop faster and more efficient antidepressants. Studies show that ketamine (KET), a PCP analog, produces antidepressant effects...

DOI: 10.4062/biomolther.2022.159 Serotonin Antidepressant Nmda receptor Monoamine neurotransmitter +3

Structure–Activity Relationship and Evaluation of Phenethylamine and Tryptamine Derivatives for Affinity towards 5-Hydroxytryptamine Type 2A Receptor

Biomolecules & Therapeutics October 13, 2022 Shujie Wang, Anlin Zhu, Suresh Paudel et al. 3 citations

Among 14 subtypes of serotonin receptors (5-HTRs), 5-HT2AR plays important roles in drug addiction and various psychiatric disorders. Agonists for 5-HT2AR have been classified into three structural groups: phenethylamines, tryptamines, and ergolines. In this study, the structure-activity relationship (SAR) of phenethylamine and tryptamine derivatives for binding 5-HT2AR was determined. In...

DOI: 10.4062/biomolther.2022.096 Phenethylamines Tryptamines Stereochemistry Pharmacology

Methoxphenidine (MXP) induced abnormalities: Addictive and schizophrenia-related behaviours based on an imbalance of neurochemicals in the brain.

British Journal of Pharmacology October 1, 2021 Kwang-Hyun Hur, Seong-Eon Kim, Shi-Xun Ma et al.

Methoxphenidine is a dissociative-based novel psychoactive designer drug. Although fatal accidents from methoxphenidine abuse have been reported, recreational use of the drug continues. We aim to provide scientific supportfor legal regulation of recreational abuse of methoxphenidine by demonstrating its the pharmacological action. Addictive potential of methoxphenidine was examined using...

DOI: 10.1111/bph.15528 Full text Addiction Mxp Nmda receptor antagonist Dissociative drug +2

R (-)-methoxetamine exerts rapid and sustained antidepressant effects and fewer behavioral side effects relative to S (+)-methoxetamine.

Neuropharmacology August 1, 2021 Chrislean Jun Botanas, Raly James Perez Custodio, Hee Jin Kim et al. 13 citations

The newfound antidepressant efficacy of ketamine has provided opportunities for the development of new-generation, rapid-acting, glutamate-based antidepressants. We previously identified that methoxetamine (MXE), a ketamine analog, and an N-Methyl-d-aspartate (NMDA) receptor antagonist, produced rapid and sustained antidepressant effects in mice. MXE (R, S (±)-MXE) is a racemic mixture...

DOI: 10.1016/j.neuropharm.2021.108619 Full text Depression Antidepressant Enantiomers Methoxetamine +1

Two newly-emerging substituted phenethylamines MAL and BOD induce differential psychopharmacological effects in rodents

Journal of Psychopharmacology July 10, 2020 Raly James Perez Custodio, Leandro Val Sayson, Chrislean Jun Botanas et al. 15 citations

Background: Recently, the recreational use of substituted phenethylamines has grown rapidly. Among these are 2-(3,5-dimethoxy-4-((2-methylallyl)oxy)phenyl)ethanamine (MAL) and 2-(2,5-dimethoxy-4-methylphenyl)-2-methoxyethan-1-amine (BOD). However, studies characterizing their abuse potential are still lacking. Aim: The purpose of this study was to investigate the abuse potential of MAL and BOD....

DOI: 10.1177/0269881120936458 Ventral tegmental area Nucleus accumbens Conditioned place preference Mesolimbic pathway +2

The Abuse Potential of Novel Synthetic Phencyclidine Derivative 1-(1-(4-Fluorophenyl)Cyclohexyl)Piperidine (4'-F-PCP) in Rodents.

International Journal of Molecular Sciences June 29, 2020 In Soo Ryu, Oc-Hee Kim, Young Eun Lee et al.

The dissociative anesthetic phencyclidine (PCP) and PCP derivatives, including 4'-F-PCP, are illegally sold and abused worldwide for recreational and non-medical uses. The psychopharmacological properties and abuse potential of 4'-F-PCP have not been fully characterized. In this study, we evaluated the psychomotor, rewarding, and reinforcing properties of 4'-F-PCP using the open-field test,...

DOI: 10.3390/ijms21134631 Full text Abuse potential Conditioned place preference Designer drugs Phencyclidine pcp derivatives +1

4-MeO-PCP and 3-MeO-PCMo, new dissociative drugs, produce rewarding and reinforcing effects through activation of mesolimbic dopamine pathway and alteration of accumbal CREB, deltaFosB, and BDNF levels.

Psychopharmacology March 1, 2020 Arvie Abiero, Chrislean Jun Botanas, Raly James Custodio et al.

A high number of synthetic dissociative drugs continue to be available through online stores, leading to their misuse. Recent inclusions in this category are 4-MeO-PCP and 3-MeO-PCMo, analogs of phencyclidine. Although the dissociative effects of these drugs and their recreational use have been reported, no studies have investigated their abuse potential. To examine their rewarding and...

DOI: 10.1007/s00213-019-05412-y Full text 3-meo-pcmo 4-meo-pcp Abuse potential Dopaminergic system +2

The novel methoxetamine analogs N-ethylnorketamine hydrochloride (NENK), 2-MeO-N-ethylketamine hydrochloride (2-MeO-NEK), and 4-MeO-N-ethylketamine hydrochloride (4-MeO-NEK) elicit rapid antidepressant effects via activation of AMPA and 5-HT2 receptors

Psychopharmacology March 19, 2019 L. Sayson, Chrislean Jun Botanas, Raly James Perez Custodio et al.

RationaleDepressive syndrome or depression is a debilitating brain disorder affecting numerous people worldwide. Although readily available, current antidepressants have low remission rates and late onset times. Recently, N-methyl-D-aspartate (NMDA) receptor antagonists, like ketamine and methoxetamine (MXE), were found to elicit rapid antidepressant effects. As the search for...

DOI: 10.1007/s00213-019-05219-x

5-Methoxy-α-methyltryptamine (5-MeO-AMT), a tryptamine derivative, induces head-twitch responses in mice through the activation of serotonin receptor 2a in the prefrontal cortex.

Behavioural Brain Research February 1, 2019 Arvie Abiero, Chrislean Jun Botanas, Leandro Val Sayson et al. 17 citations

5-Methoxy-α-methyltryptamine (5-MeO-AMT) is a tryptamine derivative that is used recreationally because of its reported hallucinogenic and mood elevating effects. Studies suggest that the psychopharmacological effects of tryptamines involve serotonin receptor 2a (5-HTR2a) activation in the brain. The head-twitch response (HTR) is widely used as a behavioral correlate for assessing 5-HTR2a...

DOI: 10.1016/j.bbr.2018.07.020 Full text 5-methoxy-a-methyltryptamine Conditioned place preference Head-twitch response Self-administration +1

Methoxetamine: A foe or friend?

Neurochemistry International 2019 Chrislean Jun Botanas, June Bryan De la Peña, Hee Jin Kim et al.

Methoxetamine (MXE) is an N-methyl-D-aspartate (NMDA) receptor antagonist that is chemically and pharmacologically similar to other dissociative substances, such as ketamine and phencyclidine. There are reports on the misuse of MXE, which sometimes resulted in adverse consequences and death. Studies have also shown that MXE has abuse liability and stimulates dopamine neurotransmission in the...

DOI: 10.1016/j.neuint.2018.10.020 Full text Abuse liability Antidepressant Intoxication Methoxetamine

Methoxetamine produces rapid and sustained antidepressant effects probably via glutamatergic and serotonergic mechanisms

Neuropharmacology November 1, 2017 Chrislean Jun Botanas, June Bryan De la Peña, Raly James Perez Custodio et al.

Depression afflicts around 16% of the world's population, making it one of the leading causes of disease burden worldwide. Despite a number of antidepressants available today, the delayed onset time and low remission rate of these treatments are still a major challenge. The N-methyl-D-aspartate (NMDA) receptor antagonist ketamine has shown to produce rapid and sustained antidepressant effects...

DOI: 10.1016/j.neuropharm.2017.08.038

Methoxetamine, a ketamine derivative, produced conditioned place preference and was self-administered by rats: Evidence of its abuse potential.

Pharmacology, Biochemistry and Behavior June 1, 2015 Chrislean Jun Botanas, J. B. de la Peña, I. J. D. Dela Peña et al.

Methoxetamine (MXE) is an N-methyl-d-aspartate (NMDA) receptor antagonist that is chemically and pharmacologically similar to ketamine. Recently, there have been many reports regarding its use/misuse in humans which have resulted in serious or even fatal outcomes. Despite these reports, MXE is not controlled or regulated in many countries which may be partly due to the lack of scientific...

DOI: 10.1016/j.pbb.2015.03.007

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