ArticleBritish journal of pharmacology2007
Cyclodextrins sequester neuroactive steroids and differentiate mechanisms that rate limit steroid actions.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 37 citations in OpenAlex.
- Pregnenolone sulfate potentiates tetrodotoxin-resistant NaThe journal of headache and pain · 2025Article
- Neurosteroid Modulation of Synaptic and Extrasynaptic GABABiomolecules · 2024Article
- Synthetic neuroactive steroids as new sedatives and anaesthetics: Back to the future.Journal of neuroendocrinology · 2022Review
- Allosteric Modulation of NMDARs Reverses Patients' Autoantibody Effects in Mice.Neurology(R) neuroimmunology & neuroinflammation · 2022Article
- Main Applications of Cyclodextrins in the Food Industry as the Compounds of Choice to Form Host-Guest Complexes.International journal of molecular sciences · 2021Review
- Neurosteroids as novel antidepressants and anxiolytics: GABA-A receptors and beyond.Neurobiology of stress · 2019Article
- Behavioral and steroidogenic pharmacology of phenyl ring substituted etomidate analogs in rats.BMC pharmacology & toxicology · 2019Article
- Positive Allosteric Modulation as a Potential Therapeutic Strategy in Anti-NMDA Receptor Encephalitis.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- A Clickable Oxysterol Photolabel Retains NMDA Receptor Activity and Accumulates in Neurons.Frontiers in neuroscience · 2018Article
- A clickable neurosteroid photolabel reveals selective Golgi compartmentalization with preferential impact on proximal inhibition.Neuropharmacology · 2016Article
- During postnatal development endogenous neurosteroids influence GABA-ergic neurotransmission of mouse cortical neurons.Neuropharmacology · 2016Article
- Neurosteroids are reduced in diabetic neuropathy and may be associated with the development of neuropathic pain.F1000Research · 2016Article
- Developmentally regulated neurosteroid synthesis enhances GABAergic neurotransmission in mouse thalamocortical neurones.The Journal of physiology · 2015Article
- 11-trifluoromethyl-phenyldiazirinyl neurosteroid analogues: potent general anesthetics and photolabeling reagents for GABAA receptors.Psychopharmacology · 2014Article
- Intrathecal neurosteroids and a neurosteroid antagonist: effects on inflammation-evoked thermal hyperalgesia and tactile allodynia.Neuroscience letters · 2013Article
- Neurosteroid analogues. 17. Inverted binding orientations of androsterone enantiomers at the steroid potentiation site on γ-aminobutyric acid type A receptors.Journal of medicinal chemistry · 2012Article
- Modulation of presynaptic GABA(A) receptors by endogenous neurosteroids.British journal of pharmacology · 2011Article
- Hydrophobic anions potently and uncompetitively antagonize GABA(A) receptor function in the absence of a conventional binding site.British journal of pharmacology · 2011Article
- Midazolam inhibits hippocampal long-term potentiation and learning through dual central and peripheral benzodiazepine receptor activation and neurosteroidogenesis.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2010Article
- The sticky issue of neurosteroids and GABA(A) receptors.Trends in neurosciences · 2010Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeNeuroactive steroids are potent modulators of GABA(A) receptors and are thus of interest for their sedative, anxiolytic, anticonvulsant and anaesthetic properties. Cyclodextrins may be useful tools to manipulate neuroactive effects of steroids on GABA(A) receptors because cyclodextrins form inclusion complexes with at least some steroids that are active at the GABA(A) receptor, such as (3alpha,5alpha)-3-hydroxypregnan-20-one (3alpha5alphaP, allopregnanolone). EXPERIMENTAL APPROACH: To assess the versatility of cyclodextrins as steroid modulators, we investigated interactions between gamma-cyclodextrin and neuroactive steroids of different structural classes. KEY
resultsBoth a bioassay based on electrophysiological assessment of GABA(A) receptor function and optical measurements of cellular accumulation of a fluorescent steroid analogue suggest that gamma-cyclodextrin sequesters steroids rather than directly influencing GABA(A) receptor function. Neither a 5beta-reduced A/B ring fusion nor a sulphate group at carbon 3 affected the presumed inclusion complex formation between steroid and gamma-cyclodextrin. Apparent dissociation constants for interactions between natural steroids and gamma-cyclodexrin ranged from 10-60 microM. Although gamma-cyclodextrin accommodates a range of natural and synthetic steroids, C(11) substitutions reduced inclusion complex formation. Using gamma-cyclodextrin to remove steroid not directly bound to GABA(A) receptors, we found that cellular retention of receptor-unbound steroid rate limits potentiation by 3alpha- hydroxysteroids but not inhibition by sulphated steroids. CONCLUSIONS AND IMPLICATIONS: We conclude that gamma-cyclodextrins can be useful, albeit non-specific, tools for terminating the actions of multiple classes of naturally occurring neuroactive steroids.
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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.