ArticleBritish journal of pharmacology2008
High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 48 citations in OpenAlex.
- Altered cerebral protein synthesis in fragile X syndrome: studies in human subjects and knockout mice.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2013Trial
- Propofol decreases in vivo binding of 11C-PBR28 to translocator protein (18 kDa) in the human brain.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2013Trial
- Impact of propofol on gastrointestinal cancer outcomes: A review of cellular behavior, growth, and metastasis.World journal of clinical oncology · 2025Review
- Pharmacological pain and sedation interventions for the prevention of intraventricular hemorrhage in preterm infants on assisted ventilation - an overview of systematic reviews.The Cochrane database of systematic reviews · 2023Review
- Propofol inhibits the voltage-gated sodium channel NaChBac at multiple sites.The Journal of general physiology · 2018Article
- Inhibition of the cardiac Na⁺ channel α-subunit Nav1.5 by propofol and dexmedetomidine.Naunyn-Schmiedeberg's archives of pharmacology · 2016Article
- Assessment of different anesthesia depth under total intravenous anesthesia on postoperative cognitive function in laparoscopic patients.Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences · 2016Article
- Long-term action of propofol on cognitive function and hippocampal neuroapoptosis in neonatal rats.International journal of clinical and experimental medicine · 2015Article
- 4-bromopropofol decreases action potential generation in spinal neurons by inducing a glycine receptor-mediated tonic conductance.British journal of pharmacology · 2014Article
- GABA(A) receptor pi (GABRP) stimulates basal-like breast cancer cell migration through activation of extracellular-regulated kinase 1/2 (ERK1/2).The Journal of biological chemistry · 2014Article
- Effects of anesthesia with isoflurane, ketamine, or propofol on physiologic parameters in neonatal rhesus macaques (Macaca mulatta).Journal of the American Association for Laboratory Animal Science : JAALAS · 2014Article
- Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.Current medicinal chemistry · 2014Review
- Guilty, or not guilty?: a short story of propofol abuse.Korean journal of anesthesiology · 2013Article
- The comparison of preemptive effects of propofol, remifentanil and ketamine on post-operative pain scores and analgesic requirements in elective lower abdominal surgery under general anesthesia: A randomized, double-blinded study.Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences · 2013Article
- The antinociceptive and antihyperalgesic effects of topical propofol on dorsal horn neurons in the rat.Anesthesia and analgesia · 2013Article
- Potentiating action of propofol at GABAA receptors of retinal bipolar cells.Investigative ophthalmology & visual science · 2011Article
- Effects of propofol versus urapidil on perioperative hemodynamics and intraocular pressure during anesthesia and extubation in ophthalmic patients.International journal of ophthalmology · 2011Article
- Topical antiseptics for the treatment of sore throat block voltage-gated neuronal sodium channels in a local anaesthetic-like manner.Naunyn-Schmiedeberg's archives of pharmacology · 2009Article
- Catastrophic neurologic syndrome with dramatic ECG changes.Journal of electrocardiologyArticle
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeVoltage-operated sodium channels constitute major target sites for local anaesthetic-like action. The clinical use of local anaesthetics is still limited by severe side effects, in particular, arrhythmias and convulsions. These side effects render the search for new local anaesthetics a matter of high interest. EXPERIMENTAL APPROACH: We have investigated the effects of three halogenated structural analogues of propofol on voltage-operated human skeletal muscle sodium channels (Na(V)1.4) and the effect of one compound (4-chloropropofol) on neuronal sodium channels (Na(V)1.2) heterologously expressed in human embryonic kidney cell line 293. KEY
results4-Iodo-, 4-bromo- and 4-chloropropofol reversibly suppressed depolarization-induced whole-cell sodium inward currents with high potency. The IC(50) for block of resting channels at -150 mV was 2.3, 3.9 and 11.3 microM in Na(V)1.4, respectively, and 29.2 microM for 4-chloropropofol in Na(V)1.2. Membrane depolarization inducing inactivation strongly increased the blocking potency of all compounds. Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2. Recovery from fast inactivation was prolonged in the presence of drug leading to an accumulation of block during repetitive stimulation at high frequencies (100 Hz). CONCLUSIONS AND IMPLICATIONS: Halogenated propofol analogues constitute a novel class of sodium channel-blocking drugs possessing almost 100-fold higher potency compared with the local anaesthetic and anti-arrhythmic drug lidocaine. Preferential drug binding to inactivated channel states suggests that halogenated propofol analogues might be especially effective in suppressing ectopic discharges in a variety of pathological conditions.
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