ArticleBioorganic & medicinal chemistry2014
Identification of a new selective dopamine D4 receptor ligand.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 29 citations in OpenAlex.
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- Design, synthesis, and cytotoxicity of ibuprofen-appended benzoxazole analogues against human breast adenocarcinoma.RSC medicinal chemistry · 2024Article
- Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.Journal of medicinal chemistry · 2023Article
- Dopamine Receptor Ligand Selectivity-An In Silico/In Vitro Insight.Biomedicines · 2023Article
- Highly Potent and Selective Dopamine DJournal of medicinal chemistry · 2022Article
- New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry · 2021Article
- A study of the structure-affinity relationship in SYA16263; is a DBioorganic & medicinal chemistry · 2021Article
- Dopamine D3 receptor: A neglected participant in Parkinson Disease pathogenesis and treatment?Ageing research reviews · 2020Review
- New analogs of SYA013 as sigma-2 ligands with anticancer activity.Bioorganic & medicinal chemistry · 2019Article
- SYA 013 analogs as moderately selective sigma-2 (σBioorganic & medicinal chemistry · 2019Article
- Dopamine DJournal of medicinal chemistry · 2019Article
- A Complete Assessment of Dopamine Receptor- Ligand Interactions through Computational Methods.Molecules (Basel, Switzerland) · 2019Article
- Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.Bioorganic & medicinal chemistry · 2016Article
- Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.Bioorganic & medicinal chemistry · 2016Article
- Homology modeling, molecular dynamic simulation, and docking based binding site analysis of human dopamine (D4) receptor.Journal of molecular modeling · 2015Article
- Expression of a Novel D4 Dopamine Receptor in the Lamprey Brain. Evolutionary Considerations about Dopamine Receptors.Frontiers in neuroanatomy · 2015Article
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
The dopamine D4 receptor has been shown to play key roles in certain CNS pathologies including addiction to cigarette smoking. Thus, selective D4 ligands may be useful in treating some of these conditions. Previous studies in our laboratory have indicated that the piperazine analog of haloperidol exhibits selective and increased affinity to the DAD4 receptor subtype, in comparison to its piperidine analog. This led to further exploration of the piperazine moiety to identify new agents that are selective at the D4 receptor. Compound 27 (KiD4=0.84 nM) was the most potent of the compounds tested. However, it only had moderate selectivity for the D4 receptor. Compound 28 (KiD4=3.9 nM) while not as potent, was more discriminatory for the D4 receptor subtype. In fact, compound 28 has little or no binding affinity to any of the other four DA receptor subtypes. In addition, of the 23 CNS receptors evaluated, only two, 5HT1AR and 5HT2BR, have binding affinity constants better than 100 nM (Ki <100 nM). Compound 28 is a potentially useful D4-selective ligand for probing disease treatments involving the D4 receptor, such as assisting smoking cessation, reversing cognitive deficits in schizophrenia and treating erectile dysfunction. Thus, further optimization, functional characterization and evaluation in animal models may be warranted.
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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.