ArticleScientific reports2018
Blocking drug activation as a therapeutic strategy to attenuate acute toxicity and physiological effects of heroin.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 16 citations in OpenAlex.
- Pleiotropic prodrugs for both symptomatic and disease-modifying treatment of Alzheimer's disease.Acta pharmaceutica Sinica. B · 2025Article
- Identification of Potent and Selective Acetylcholinesterase/Butyrylcholinesterase Inhibitors by Virtual Screening.Journal of chemical information and modeling · 2023Article
- Systematic Structure-Based Virtual Screening Approach to Antibody Selection and Design of a Humanized Antibody against Multiple Addictive Opioids without Affecting Treatment Agents Naloxone and Naltrexone.ACS chemical neuroscience · 2021Article
- Cebranopadol reduces cocaine self-administration in male rats: Dose, treatment and safety consideration.Neuropharmacology · 2020Article
- Discovery of potent and selective butyrylcholinesterase inhibitors through the use of pharmacophore-based screening.Bioorganic & medicinal chemistry letters · 2019Article
- Structure-based virtual screening leading to discovery of highly selective butyrylcholinesterase inhibitors with solanaceous alkaloid scaffolds.Chemico-biological interactions · 2019Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Heroin is a growing national crisis in America. There is an increasing frequency of heroin overdoses. All of the currently used therapeutic approaches to treatment of heroin abuse and other opioid drugs of abuse focus on antagonizing a brain receptor (particularly µ-opiate receptors). However, it has been known that the therapeutic use of certain µ-opiate receptor antagonist may actually increase heroin overdose. Once overdosed, heroin addicts may continue to get overdosed again and again until fatal. Here we report our design and validation of a novel therapeutic strategy targeting heroin activation based on our analysis of the chemical transformation and functional change of heroin in the body. An effective blocker of heroin activation, such as ethopropazine tested in this study, may be used as a standalone therapy or in combination with a currently available, traditional medications targeting µ-opiate receptors (e.g. naltrexone or its extended-release formulation Vivitrol). The combination therapy would be ideal for heroin abuse treatment as the effects of two therapeutic agents targeting two independent mechanisms are cooperative.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.