Monoamine transporter and receptor interaction profiles of a new series of designer cathinones

  title={Monoamine transporter and receptor interaction profiles of a new series of designer cathinones},
  author={Linda D. Simmler and Anna Rickli and Marius C. Hoener and Matthias E. Liechti},

Monoamine Transporter and Receptor Interaction Profiles of Synthetic Cathinones

There are considerable differences among cathinones with respect to potencies and relative activity at monoaminergic targets, and in vitro screening and pharmacological classification are essential in providing translationally valuable information promptly after new cathinone derivatives emerge among drug users.

Para-Halogenation Affects Monoamine Transporter Inhibition Properties and Hepatocellular Toxicity of Amphetamines and Methcathinones

Para-halogenation of stimulants increases the risk for serotonergic neurotoxicity and may increase hepatic toxicity mediated by mitochondrial impairment in susceptible users.

Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens

Effects of the new psychoactive substances diclofensine, diphenidine, and methoxphenidine on monoaminergic systems

2-Aminoindan and its ring-substituted derivatives interact with plasma membrane monoamine transporters and α2-adrenergic receptors

2-AI is predicted to have (+)-amphetamine-like effects and abuse potential whereas the ring-substituted derivatives may produce 3,4-methylenedioxymethamphetamine (MDMA)-like effects but with less abuse liability.

Interactions of Cathinone NPS with Human Transporters and Receptors in Transfected Cells.

Cathinones with a nitrogen-containing pyrrolidine ring emerged as NPS that are extremely potent transporter inhibitors but not monoamine releasers, suggesting more stimulant and reinforcing properties.

Hazard Characterization of Synthetic Cathinones Using Viability, Monoamine Reuptake, and Neuronal Activity Assays

The combination of integrated measurements (MEA recordings of neuronal activity) with single target assays (monoamine reuptake transporter inhibition) indicates inhibition of hDAT and hNET as the primary mode of action of these synthetic cathinones.



Pharmacological profile of antidepressants and related compounds at human monoamine transporters.

Powerful Cocaine-Like Actions of 3,4-Methylenedioxypyrovalerone (MDPV), a Principal Constituent of Psychoactive ‘Bath Salts’ Products

The data show that MDPV is a monoamine transporter blocker with increased potency and selectivity for catecholamines when compared with cocaine, and may provide a mechanism to explain the adverse effects observed in humans taking high doses of ‘bath salts’ preparations.

MDMA (Ecstasy) and human dopamine, norepinephrine, and serotonin transporters: implications for MDMA-induced neurotoxicity and treatment

The affinity of ecstasy for the human SERT in transfected cells does not clarify the apparent selective toxicity of MDMA for serotonin neurons, although conceivably, its higher efficacy for stimulating 5-HT release may be a distinguishing factor.

Serotonin 5-HT2B Receptors Are Required for 3,4-Methylenedioxymethamphetamine-Induced Hyperlocomotion and 5-HT Release In Vivo and In Vitro

These findings reveal a novel regulatory component in the actions of MDMA and represent the first demonstration that 5-HT2B receptors play an important role in the brain, i.e., modulation of 5- HT release, and may serve as promising therapeutic drugs for MDMA abuse.

Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters.

Relationship between the Serotonergic Activity and Reinforcing Effects of a Series of Amphetamine Analogs

The results suggest that the mechanism for this effect involves a decrease in reinforcing potency and efficacy among monoamine releasing agents when 5-HT releasing potency is increased relative to DA.

p-methylthioamphetamine is a potent new non-neurotoxic serotonin-releasing agent.