ReviewBritish journal of clinical pharmacology2016
Cell membranes… and how long drugs may exert beneficial pharmacological activity in vivo.
Review in British journal of clinical pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
25 citing papers in PubMed, 42 citations in OpenAlex.
- Detergent Conjugation Decouples Chlorpromazine Solubility from Antibacterial Activity against Bacteria Relevant for Gut Microbiota.Bioconjugate chemistry · 2026Article
- Bitopic AJournal of medicinal chemistry · 2025Article
- Cell-Based Drug Delivery Systems: Innovative Drug Transporters for Targeted Therapy.International journal of molecular sciences · 2025Review
- Review
- Article
- Novel Cannabinoid Receptor 2 (CB2) Low Lipophilicity Agonists Produce Distinct cAMP and Arrestin Signalling Kinetics without Bias.International journal of molecular sciences · 2023Article
- Exploring the kinetic selectivity of drugs targeting the βPharmacology research & perspectives · 2022Article
- Inhibition of NMDA receptors through a membrane-to-channel path.Nature communications · 2022Article
- Interaction With the Lipid Membrane Influences Fentanyl Pharmacology.Advances in drug and alcohol research · 2022Article
- Mechanistic Understanding from Molecular Dynamics in Pharmaceutical Research 2: Lipid Membrane in Drug Design.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Membrane-Facilitated Receptor Access and Binding Mechanisms of Long-ActingMolecular pharmacology · 2021Article
- Cholesterol as a modulator of cannabinoid receptor CBScientific reports · 2021Article
- An Advanced Automated Patch Clamp Protocol Design to Investigate Drug-Ion Channel Binding Dynamics.Frontiers in pharmacology · 2021Article
- On the Rational Drug Design for Hypertension through NMR Spectroscopy.Molecules (Basel, Switzerland) · 2020Review
- Slow-binding reversible inhibitor of acetylcholinesterase with long-lasting action for prophylaxis of organophosphate poisoning.Scientific reports · 2020Article
- Does the Lipid Bilayer Orchestrate Access and Binding of Ligands to Transmembrane Orthosteric/Allosteric Sites of G Protein-Coupled Receptors?Molecular pharmacology · 2019Review
- Agonist-induced membrane nanodomain clustering drives GLP-1 receptor responses in pancreatic beta cells.PLoS biology · 2019Article
- Biological Obstacles for IdentifyingPharmaceutics · 2019Review
- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine APurinergic signalling · 2019Article
- Link between a highMedChemComm · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The time course of the beneficial pharmacological effect of a drug has long been considered to depend merely on the temporal fluctuation of its free concentration. Only in the last decade has it become widely accepted that target-binding kinetics can also affect in vivo pharmacological activity. Although current reviews still essentially focus on genuine dissociation rates, evidence is accumulating that additional micro-pharmacokinetic (PK) and -pharmacodynamic (PD) mechanisms, in which the cell membrane plays a central role, may also increase the residence time of a drug on its target. The present review provides a compilation of otherwise widely dispersed information on this topic. The cell membrane can intervene in drug binding via the following three major mechanisms: (i) by acting as a sink/repository for the drug; (ii) by modulating the conformation of the drug and even by participating in the binding process; and (iii) by facilitating the approach (and rebinding) of the drug to the target. To highlight these mechanisms, we focus on drugs that are currently used in clinical therapy, such as the antihypertensive angiotensin II type 1 receptor antagonist candesartan, the atypical antipsychotic agent clozapine and the bronchodilator salmeterol. Although the role of cell membranes in PK-PD modelling is gaining increasing interest, many issues remain unresolved. It is likely that novel biophysical and computational approaches will provide improved insights in the near future.
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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.