ArticleMolecular informatics2010
Transporter-mediated Efflux Influences CNS Side Effects: ABCB1, from Antitarget to Target.
Article in Molecular informatics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- Solubility-Permeability Interplay in Facilitating the Prediction of Drug Disposition Routes, Extent of Absorption, Food Effects, Brain Penetration and Drug Induced Liver Injury Potential.Journal of pharmaceutical sciences · 2023Review
- 2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery.Journal of medicinal chemistry · 2023Review
- First-Line Combination Treatment with Low-Dose Bipolar Drugs for ABCB1-Overexpressing Drug-Resistant Cancer Populations.International journal of molecular sciences · 2023Review
- State of the Art and Uses for the Biopharmaceutics Drug Disposition Classification System (BDDCS): New Additions, Revisions, and Citation References.The AAPS journal · 2022Review
- ABCB1 in dermatology: roles in skin diseases and their treatment.Journal of molecular medicine (Berlin, Germany) · 2021Review
- Diphenhydramine as a selective probe to study HJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
- Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.ACS medicinal chemistry letters · 2012Article
- Improving the prediction of the brain disposition for orally administered drugs using BDDCS.Advanced drug delivery reviews · 2012Review
- Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome.Clinical pharmacology and therapeutics · 2011Article
- Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: Ranking 1654 human protein targets by assayed compounds and molecular scaffolds.Journal of cheminformatics · 2011Article
- A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.Journal of medicinal chemistry · 2011Article
- Cross-pharmacology analysis of G protein-coupled receptors.Current topics in medicinal chemistry · 2011Article
- ChemProt: a disease chemical biology database.Nucleic acids research · 2011Article
- Impact of the Recent Mouse P-Glycoprotein Structure for Structure-Based Ligand Design.Molecular informatics · 2010Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
We examined the relationship between sedation and orthostatic hypotension, two central side effects and ABCB1 transporter-mediated efflux for a set of 64 launched drugs that are documented as histamine H1 receptor antagonists. This relationship was placed in the context of passive diffusion (estimated using LogP, the octanol/water partition coefficient), receptor affinity, and the adjusted therapeutic daily dose, in order to account for side effect variability. Within this set, CNS permeability was not dependent on passive diffusion, as no significant differences were found for LogP and its pH-corrected equivalent, LogD(74). Sedation and orthostatic hypotension can be explained within the framework of ABCB1-mediated efflux and adjusted dose, while target potency has less influence. ABCB1, an antitarget for anti-cancer agents, acts in fact as a drug target for non-sedating antihistamines. An empirical set of rules, based on the incidence of these two side-effects, target affinity and dose was used to predict efflux effects for a number of drugs. Among them, azelastine and mizolastine are predicted to be effluxed via ABCB1-mediated transport, whereas aripiprazole, clozapine, cyproheptadine, iloperidone, olanzapine, and ziprasidone are likely to be non-effluxed.
Identifiers
What OpenQuestion holds
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.