ArticleBioorganic & medicinal chemistry2012
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled it.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 43 citations in OpenAlex.
- Strategies for Switching between Oral Postsynaptic Antidopaminergic Antipsychotics in Patients with Schizophrenia: A Systematic Review.CNS drugs · 2025Pooled it
- Structure-Affinity Relationship Optimization of SYA16263 Yields New Ligands with Improved Receptor Affinity and Antipsychotic-Like Properties.ACS omega · 2026Article
- Pharmacologic targeting of the dopamine D2 receptor impacts the efficacy of immune checkpoint blockade in melanoma.Journal for immunotherapy of cancer · 2026Article
- Pridopidine, a Potent and Selective Therapeutic Sigma-1 Receptor (S1R) Agonist for Treating Neurodegenerative Diseases.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Ergotamine enhances circadian amplitude and diurnally mitigates nitroglycerin-induced mechanical hypersensitivity.The journal of headache and pain · 2025Article
- Dopamine Receptor Ligand Selectivity-An In Silico/In Vitro Insight.Biomedicines · 2023Article
- Differential Role of Active Compounds in Mitophagy and Related Neurodegenerative Diseases.Toxins · 2023Review
- Design, Synthesis and Pharmacological Evaluation of Novel Conformationally RestrictedBiomolecules · 2022Article
- Identification of Novel Dopamine DMolecules (Basel, Switzerland) · 2022Article
- Computational approaches for the design of novel dopamine DIn silico pharmacology · 2022Article
- Sinusoidal analysis reveals a non-linear and dopamine-dependent relationship between ambient illumination and motor activity in larval zebrafish.Neuroscience letters · 2021Article
- 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
- SYA 013 analogs as moderately selective sigma-2 (σBioorganic & medicinal chemistry · 2019Article
- The differential actions of clozapine and other antipsychotic drugs on the translocation of dopamine D2 receptors to the cell surface.The Journal of biological chemistry · 2019Article
- Evaluation of SYA16263 as a new potential antipsychotic agent without catalepsy.Pharmacology, biochemistry, and behavior · 2019Article
- Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.Bioorganic & medicinal chemistry letters · 2017Article
- Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.Bioorganic & medicinal chemistry · 2016Article
- Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future.Current topics in medicinal chemistry · 2016Review
- Comparing structural fingerprints using a literature-based similarity benchmark.Journal of cheminformatics · 2016Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Using haloperidol as a scaffold, new agents were designed to investigate the structural contributions of various groups to binding at CNS receptors associated with atypical antipsychotic pharmacology. It is clear that each pharmacophoric group, the butyrophenone, the piperidine and the 4-chlorophenyl moieties contributes to changes in binding to the receptors of interest. This strategy has resulted in the identification of several new agents, compounds 16, 18, 19, 23, 24 and 25, with binding profiles which satisfy our stated criteria for agents to act as potential atypical antipsychotics. This research demonstrates that haloperidol can serve as a useful lead in the identification and design of new agents that target multiple receptors associated with antipsychotic pharmacology.
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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.