ArticleThe Journal of pharmacology and experimental therapeutics2011
N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects.
Article in The Journal of pharmacology and experimental therapeutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 33 citations in OpenAlex.
- Effects of cannabinoid agonists and antagonists in male rats discriminating the synthetic cannabinoid AM2201.European journal of pharmacology · 2023Article
- Allosteric Modulator KM822 Attenuates Behavioral Actions of Amphetamine inMolecular pharmacology · 2022Article
- Functional Characterization of the Dopaminergic Psychostimulant Sydnocarb as an Allosteric Modulator of the Human Dopamine Transporter.Biomedicines · 2021Article
- Progress in agonist therapy for substance use disorders: Lessons learned from methadone and buprenorphine.Neuropharmacology · 2019Review
- Dopamine Transporter Dynamics ofThe Journal of pharmacology and experimental therapeutics · 2018Article
- Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.Journal of medicinal chemistry · 2017Article
- The Isomeric Preference of an Atypical Dopamine Transporter Inhibitor Contributes to Its Selection of the Transporter Conformation.ACS chemical neuroscience · 2017Article
- σ Receptor Effects of N-Substituted Benztropine Analogs: Implications for Antagonism of Cocaine Self-Administration.The Journal of pharmacology and experimental therapeutics · 2017Article
- CTDP-32476: A Promising Agonist Therapy for Treatment of Cocaine Addiction.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2017Article
- 2-Substituted 3β-Aryltropane Cocaine Analogs Produce Atypical Effects without Inducing Inward-Facing Dopamine Transporter Conformations.The Journal of pharmacology and experimental therapeutics · 2016Article
- Regulation of the Dopamine and Vesicular Monoamine Transporters: Pharmacological Targets and Implications for Disease.Pharmacological reviews · 2015Review
- Cocaine Antagonists; Studies on Cocaine Self-Administration.Journal of alcoholism and drug dependence · 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
- Antagonist-induced conformational changes in dopamine transporter extracellular loop two involve residues in a potential salt bridge.Neurochemistry international · 2014Article
- 2-isoxazol-3-phenyltropane derivatives of cocaine: molecular and atypical system effects at the dopamine transporter.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
- Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist.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
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Previous studies suggested that differences between the behavioral effects of cocaine and analogs of benztropine were related to the relatively slow onset of action of the latter compounds. Several N-substituted benztropine analogs with a relatively fast onset of effects were studied to assess whether a fast onset of effects would render the effects more similar to those of cocaine. Only one of the compounds increased locomotor activity, and the increases were modest compared with those of 10 to 20 mg/kg cocaine. In rats trained to discriminate 10 mg/kg cocaine from saline none of the compounds produced more than 40% cocaine-like responds up to 2 h after injection. None of the compounds produced place-conditioning when examined up to 90 min after injection, indicating minimal abuse liability. The compounds had 5.6 to 30 nM affinities at the dopamine transporter (DAT), with uniformly lower affinities at norepinephrine and serotonin transporters (from 490-4600 and 1420-7350 nM, respectively). Affinities at muscarinic M(1) receptors were from 100- to 300-fold lower than DAT affinities, suggesting minimal contribution of those sites to the behavioral effects of the compounds. Affinities at histaminic H(1) sites were from 11- to 43-fold lower than those for the DAT. The compounds also had affinity for sigma, 5-hydroxytryptamine(1) (5-HT(1)), and 5-HT(2) receptors that may have contributed to their behavioral effects. Together, the results indicate that a slow onset of action is not a necessary condition for reduced cocaine-like effects of atypical DAT ligands and suggest several mechanisms that may contribute to the reduced cocaine-like efficacy of these compounds.
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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.