ArticleThe Journal of pharmacology and experimental therapeutics2010
Dopamine transporter-dependent and -independent striatal binding of the benztropine analog JHW 007, a cocaine antagonist with low abuse liability.
Article in The Journal of pharmacology and experimental therapeutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 36 citations in OpenAlex.
- Repurposing drugs for the human dopamine transporter through WHALES descriptors-based virtual screening and bioactivity evaluation.Journal of pharmaceutical analysis · 2025Article
- Novel Ways of Targeting the Dopamine Transporter.Advances in neurobiology · 2025Review
- Unlocking the Potential of High-Quality Dopamine Transporter Pharmacological Data: Advancing Robust Machine Learning-Based QSAR Modeling.Advances in neurobiology · 2025Review
- Cryo-EM structure of the dopamine transporter with a novel atypical non-competitive inhibitor bound to the orthosteric site.Journal of neurochemistry · 2024Article
- Article
- Interactions of calmodulin kinase II with the dopamine transporter facilitate cocaine-induced enhancement of evoked dopamine release.Translational psychiatry · 2023Article
- Dopamine Transporter Dynamics ofThe Journal of pharmacology and experimental therapeutics · 2018Article
- Behavioral economic analysis of the effects of N-substituted benztropine analogs on cocaine self-administration in rats.Psychopharmacology · 2018Article
- Atypical dopamine transporter inhibitors R-modafinil and JHW 007 differentially affect D2 autoreceptor neurotransmission and the firing rate of midbrain dopamine neurons.Neuropharmacology · 2017Article
- σ Receptor Effects of N-Substituted Benztropine Analogs: Implications for Antagonism of Cocaine Self-Administration.The Journal of pharmacology and experimental therapeutics · 2017Article
- Cocaine Antagonists; Studies on Cocaine Self-Administration.Journal of alcoholism and drug dependence · 2015Article
- Thermal Stability of Dopamine Transporters.The Journal of membrane biology · 2015Article
- Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporter.Drug and alcohol dependence · 2015Review
- Preference for distinct functional conformations of the dopamine transporter alters the relationship between subjective effects of cocaine and stimulation of mesolimbic dopamine.Biological psychiatry · 2014Article
- Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist.The Journal of pharmacology and experimental therapeutics · 2014Article
- Preclinical efficacy of N-substituted benztropine analogs as antagonists of methamphetamine self-administration in rats.The Journal of pharmacology and experimental therapeutics · 2014Article
- Relations between stimulation of mesolimbic dopamine and place conditioning in rats produced by cocaine or drugs that are tolerant to dopamine transporter conformational change.Psychopharmacology · 2013Article
- Nonclassical pharmacology of the dopamine transporter: atypical inhibitors, allosteric modulators, and partial substrates.The Journal of pharmacology and experimental therapeutics · 2013Review
- Sex-specific brain deficits in auditory processing in an animal model of cocaine-related schizophrenic disorders.Brain sciences · 2013Article
- N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects.The Journal of pharmacology and experimental therapeutics · 2011Article
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
The benztropine analog N-(n-butyl)-3α-[bis(4'-fluorophenyl)methoxy]-tropane (JHW 007) displays high affinity for the dopamine transporter (DAT), but unlike typical DAT ligands, has relatively low abuse liability and blocks the effects of cocaine, including its self-administration. To determine sites responsible for the cocaine antagonist effects of JHW 007, its in vitro binding was compared with that of methyl (1R,2S,3S,5S)-3-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate (WIN 35428) in rats, mice, and human DAT (hDAT)-transfected cells. A one-site model, with K(d) values of 4.21 (rat) and 8.99 nM (mouse) best fit the [(3)H]WIN 35428 data. [(3)H]JHW 007 binding best fit a two-site model (rat, 7.40/4400 nM; mouse, 8.18/2750 nM), although a one-site fit was observed with hDAT membranes (43.7 nM). Drugs selective for the norepinephrine and serotonin transporters had relatively low affinity in competition with [(3)H]JHW 007 binding, as did drugs selective for other sites identified previously as potential JHW 007 binding sites. The association of [(3)H]WIN 35428 best fit a one-phase model, whereas the association of [(3)H]JHW 007 best fit a two-phase model in all tissues. Because cocaine antagonist effects of JHW 007 have been observed previously soon after injection, its rapid association observed here may contribute to those effects. Multiple [(3)H]JHW 007 binding sites were obtained in tissue from mice lacking the DAT, suggesting these as yet unidentified sites as potential contributors to the cocaine antagonist effects of JHW 007. Unlike WIN 35428, the binding of JHW 007 was Na(+)-independent. This feature of JHW 007 has been linked to the conformational status of the DAT, which in turn may contribute to the antagonism of cocaine.
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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.