Substances tested

What has been given to the oligodendrocyte, and what the cell did. Research reference, not medical advice.

All substances 30

Clemastine fumarate antihistamine with antimuscarinic action

acts on muscarinic receptors (M1 and M3)

Promotes oligodendrocyte precursor differentiation and remyelination. In the ReBUILD crossover trial the primary endpoint was met: visual evoked potential latency delay reduced by 1.7 ms per eye (95% CI 0.5 to 2.9, p = 0.0048); fatigue was associated, no serious adverse events.

dose: trial dose not stated in the abstract · human, 50 patients with multiple sclerosis · randomised double-blind placebo-controlled crossover trial, 150 days · Green AJ, Gelfand JM, Cree BA, Bevan C, Boscardin WJ, Mei F et al. Clemastine fumarate as a remyelinating therapy for multiple sclerosis (ReBUILD): a randomised, controlled, double-blind, crossover trial. Lancet. 2017;390:2481-2489. PMID: 29029896. · source

Clemastine antihistamine with antimuscarinic action

acts on muscarinic receptors, ERK1/2, Myrf and Olig2

Promotes OPC differentiation through muscarinic receptors and ERK1/2 activation with increased Myrf and Olig2; blocked by ERK inhibition (U0126) and reduced by the muscarinic agonist cevimeline.

dose: not stated in the abstract · rat, spinal cord injury · in vivo pharmacology · Tong LY, Deng YB, Du WH, Zhou WZ, Liao XY, Jiang X. Clemastine Promotes Differentiation of Oligodendrocyte Progenitor Cells Through the Activation of ERK1/2 via Muscarinic Receptors After Spinal Cord Injury. Front Pharmacol. 2022;13:914153. PMID: 35865954. · source

Antimuscarinic compounds (screen) muscarinic antagonists

acts on muscarinic receptors

Screening 1,000 bioactive molecules on micropillar arrays identified a cluster of antimuscarinic compounds that enhance oligodendrocyte differentiation and remyelination.

dose: screen concentrations not stated in the abstract · rodent OPCs in vitro (species not stated in the abstract) · high-throughput micropillar screen · Mei F, Fancy SPJ, Shen YA, Niu J, Zhao C, Presley B et al. Micropillar arrays as a high-throughput screening platform for therapeutics in multiple sclerosis. Nat Med. 2014;20:954-960. PMID: 24997607. · source

Benztropine anticholinergic

acts on direct antagonism of M1 and/or M3 muscarinic receptors

Among the most effective compounds in an image-based screen for myelin basic protein expression; decreases clinical severity in EAE alone or with approved immunosuppressants; efficacy from enhanced remyelination, not immune suppression (cuprizone model, T-cell assays).

dose: not stated in the abstract · rat optic nerve OPCs in vitro; mouse EAE and cuprizone models · screen plus in vivo models · Deshmukh VA, Tardif V, Lyssiotis CA, Green CC, Kerman B, Kim HJ et al. A regenerative approach to the treatment of multiple sclerosis. Nature. 2013;502:327-332. PMID: 24107995. · source

Miconazole antifungal

acts on mitogen-activated protein kinase signalling in OPCs

Increases new oligodendrocytes and enhances remyelination in lysolecithin lesions; reverses disease severity at the peak of EAE; acts directly as a remyelinating drug with no immune effect; enhances human oligodendrocyte generation from human OPCs in vitro.

dose: not stated in the abstract · mouse; human cells in vitro · in vivo lesion models and in vitro · Najm FJ, Madhavan M, Zaremba A, Shick E, Karl RT, Factor DC et al. Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo. Nature. 2015;522:216-220. PMID: 25896324. · source

Clobetasol glucocorticoid

acts on glucocorticoid receptor signalling in OPCs

Same remyelinating effects as miconazole in lysolecithin and EAE models, and a potent immunosuppressant as well; enhances human oligodendrocyte generation in vitro.

Metformin antidiabetic

acts on aged OPCs (mechanism beyond the abstract not claimed here)

Restores CNS remyelination capacity by rejuvenating aged OPCs, which had become unresponsive to pro-differentiation signals.

dose: not stated in the abstract · aged rodents · in vivo · Neumann B, Baror R, Zhao C, Segel M, Dietmann S, Rawji KS et al. Metformin Restores CNS Remyelination Capacity by Rejuvenating Aged Stem Cells. Cell Stem Cell. 2019;25:473-485. PMID: 31585093. · source

Opicinumab anti-LINGO-1 monoclonal antibody

acts on LINGO-1

In acute optic neuritis (RENEW), the visual evoked potential latency benefit over placebo was greatest in participants aged 33 or older (-14.17 ms, p = 0.01) and absent below 33 (-0.89 ms, p = 0.87); latency recovery associated with less retinal ganglion cell layer thinning.

dose: not stated in the abstract · human, 33 treated and 36 placebo · randomised trial, per-protocol analysis · Cadavid D, Balcer L, Galetta S, Aktas O, Ziemssen T, Vanopdenbosch LJ et al. Predictors of response to opicinumab in acute optic neuritis. Ann Clin Transl Neurol. 2018;5:1154-1162. PMID: 30349850. · source

Adenosine neuron-glial transmitter

acts on adenosine receptors on OPCs

Released in response to action potential firing; inhibits OPC proliferation, stimulates differentiation and promotes myelin formation.

dose: not stated in the abstract · not stated in the abstract · in vitro co-culture and electrophysiology · Stevens B, Porta S, Haak LL, Gallo V, Fields RD. Adenosine: a neuron-glial transmitter promoting myelination in the CNS in response to action potentials. Neuron. 2002;36:855-868. PMID: 12467589. · source

Nicotine nicotinic agonist

acts on neuronal nicotinic acetylcholine receptors (alpha3, alpha4, alpha5, alpha7, beta2, beta4 subunits) on OPCs

About 65 percent of O2A/OPCs raise intracellular calcium on nicotine; 37 percent show calcium oscillations at 20 to 30 s intervals over 2 to 3 min, blocked by the alpha4 beta2 antagonist dihydro-beta-erythroidine or nifedipine.

dose: not stated in the abstract · rat corpus callosum OPCs · RT-PCR, immunocytochemistry, FURA-2 calcium imaging · Rogers SW, Gregori NZ, Carlson N, Gahring LC, Noble M. Neuronal nicotinic acetylcholine receptor expression by O2A/oligodendrocyte progenitor cells. Glia. 2001;33:306-313. PMID: 11246229. · source

Dopamine (quinpirole, D3 agonist) dopaminergic

acts on dopamine D3 receptor, expressed in differentiating oligodendrocytes but not mature ones

20 uM quinpirole decreased the number of O1-positive oligodendrocytes with myelin-like membranes and increased precursors at 14 days in vitro; prevented by haloperidol.

dose: 20 uM quinpirole · not stated in the abstract (cultured oligodendrocyte precursors) · culture, immunocytochemistry, confocal microscopy · Bongarzone ER, Howard SG, Schonmann V, Campagnoni AT. Identification of the dopamine D3 receptor in oligodendrocyte precursors: potential role in regulating differentiation and myelin formation. J Neurosci. 1998;18:5344-5353. PMID: 9651217. · source

Acetylcholine (muscarinic M3 signalling) endogenous transmitter

acts on muscarinic M3 receptor on OPCs

M3R signalling delays differentiation and remyelination in human OPCs; conditional M3R ablation in adult NG2 OPCs increased oligodendrocyte differentiation and improved spontaneous remyelination.

dose: genetic ablation, no dose · human OPCs and mouse · genetics, in vivo · Welliver RR, Polanco JJ, Seidman RA, Sinha AK, O'Bara MA, Khaku ZM et al. Muscarinic Receptor M3R Signaling Prevents Efficient Remyelination by Human and Mouse Oligodendrocyte Progenitor Cells. J Neurosci. 2018;38:6921-6932. PMID: 29959237. · source

Glutamate endogenous transmitter

acts on AMPA-type glutamate receptors at neuron-to-OPC synapses

Neurons form glutamatergic synapses onto OPCs in the hippocampus.

dose: synaptic · rat · electrophysiology and electron microscopy · Bergles DE, Roberts JD, Somogyi P, Jahr CE. Glutamatergic synapses on oligodendrocyte precursor cells in the hippocampus. Nature. 2000;405:187-191. PMID: 10821275. · source

GABA endogenous transmitter

acts on GABA-A receptors at interneuron-to-OPC synapses

Interneurons form GABAergic synapses onto OPCs in the hippocampus.

dose: synaptic · rat · electrophysiology · Lin SC, Bergles DE. Synaptic signaling between GABAergic interneurons and oligodendrocyte precursor cells in the hippocampus. Nat Neurosci. 2004;7:24-32. PMID: 14661022. · source

Thyroid hormone (T3, triiodothyronine) thyroid hormone

acts on thyroid hormone receptors (TRalpha, TRbeta) on OPCs

T3 is the primary driver of OPC differentiation to mature myelinating oligodendrocytes. In Mct8/Oatp1c1 double-knockout mice (a model of MCT8 deficiency), CNS thyroid hormone deficiency causes persistent hypomyelination associated with a reduction in Olig2-positive oligodendroglial cells across all developmental stages studied (P12, P30, P120).

dose: endogenous; genetic model · mouse (Mct8/Oatp1c1 double knockout vs wild-type) · multi-marker immunostaining and confocal microscopy at postnatal days P12, P30, P120 · Mayerl S, Heuer H. Thyroid hormone transporter Mct8/Oatp1c1 deficiency compromises proper oligodendrocyte maturation in the mouse CNS. Neurobiol Dis. 2023;184:106195. PMID: 37307933. · source

Thyroid hormone receptor-beta synthetic agonists (IS25, TG68) TRbeta1 selective agonists

acts on thyroid hormone receptor beta-1 on OPCs

TG68 (a TRbeta1 pro-drug) induces OPC differentiation and maturation in a neural stem cell-derived OPC model comparable to the natural ligand T3 and the reference TRbeta1 agonist; maintains efficacy under inflammatory challenge conditions.

dose: not stated in the abstract · rat neural stem cell-derived OPCs in vitro · in vitro OPC differentiation assay with and without inflammatory challenge · Baldassarro VA, Quadalti C, Runfola M, Manera C, Rapposelli S, Calza L. Synthetic Thyroid Hormone Receptor-beta Agonists Promote Oligodendrocyte Precursor Cell Differentiation in the Presence of Inflammatory Challenges. Pharmaceuticals (Basel). 2023;16. PMID: 37765015. · source

IRX4204 (selective RXR agonist) retinoid X receptor agonist

acts on retinoid X receptor (RXR)

IRX4204 blocked progressive loss of knee and ankle movement and reversed movement deficits in EAE mice; promoted functional recovery and myelin repair. Unlike bexarotene, which activates multiple nuclear receptor subtypes and causes hyperlipidemia, IRX4204 selectively activates RXR without this side effect.

dose: not stated in the abstract · mouse (EAE model) · treadmill gait analysis with machine learning, histology · Kasheke GDS, Hendy BAM, Dorighello GG, Uccelli NA, Gothie JM, Novorolsky RJ et al. Selective retinoid X receptor agonism promotes functional recovery and myelin repair in experimental autoimmune encephalomyelitis. Acta Neuropathol Commun. 2024;12:197. PMID: 39707547. · source

Quetiapine atypical antipsychotic

acts on mechanism in OPCs not stated in the abstract; associated with downregulation of Olig2 during maturation

Quetiapine (10 mg/kg/day orally) during the recovery period after cuprizone-induced demyelination significantly improved spatial working memory and increased myelin restoration; enhanced repopulation of mature oligodendrocytes in demyelinated lesions associated with Olig2 downregulation.

dose: 10 mg/kg/day oral · mouse (C57BL/6, cuprizone model) · behavioral testing (locomotor, Y-maze), immunohistochemistry · Zhang Y, Zhang H, Wang L, Jiang W, Xu H, Xiao L et al. Quetiapine enhances oligodendrocyte regeneration and myelin repair after cuprizone-induced demyelination. Schizophr Res. 2012;138:8-17. PMID: 22555017. · source

Agomelatine melatonin receptor agonist and 5-HT2C antagonist

acts on LRP1 / PPARgamma signalling in OPCs

Agomelatine treatment after transient middle cerebral artery occlusion reduced white matter lesion volume, attenuated long-term sensorimotor and cognitive deficits, promoted OPC differentiation and enhanced remyelination in vitro, ex vivo and in vivo via LRP1/PPARgamma; did not affect OPC proliferation.

dose: not stated in the abstract · rat (tMCAO ischemic stroke model); OPCs in vitro · in vivo stroke model, MRI, immunohistochemistry, in vitro differentiation assay · Wang S, Li C, Kang X, Su X, Liu Y, Wang Y et al. Agomelatine promotes differentiation of oligodendrocyte precursor cells and preserves white matter integrity after cerebral ischemic stroke. J Cereb Blood Flow Metab. 2024;44:1487-1500. PMID: 38853430. · source

Progesterone steroid hormone

acts on progesterone receptor on oligodendrocyte lineage cells

Progesterone promotes myelination and remyelination through the progesterone receptor and also decreases neuroinflammation to indirectly support OPC differentiation; acts both directly on the oligodendrocyte lineage and indirectly by reducing the inflammatory environment.

dose: not stated in the abstract (review) · rodent (review of in vivo studies) · review of mechanisms in vivo and in vitro · Jure I, De Nicola AF, Labombarda F. Progesterone effects on the oligodendrocyte linage: all roads lead to the progesterone receptor. Neural Regen Res. 2019;14:2029-2034. PMID: 31397329. · source

PDGF-AA (platelet-derived growth factor AA) growth factor

acts on PDGF receptor alpha (PDGFRalpha) on OPCs

PDGF-AA is expressed in B104 neuroblastoma conditioned medium and acts as a potent mitogen for OPC proliferation; blockade with PDGFR inhibitor AG1295 markedly decreased B104CM-stimulated OPC proliferation, confirming PDGF-AA as a major OPC mitogenic signal.

dose: not stated in the abstract · rat OPCs in vitro · conditioned medium experiments, receptor inhibitor assays · Hu JG, Wu XJ, Feng YF, Xi GM, Wang ZH, Zhou JS et al. PDGF-AA and bFGF mediate B104CM-induced proliferation of oligodendrocyte precursor cells. Int J Mol Med. 2012;30:1113-1118. PMID: 22922759. · source

Paroxetine selective serotonin reuptake inhibitor (SSRI)

acts on serotonin reuptake transporter; downstream OPC proliferation and differentiation

Paroxetine ameliorated corticosterone-induced myelin damage in the prefrontal cortex by promoting both the proliferation and differentiation of OPCs; associated with improved remyelination and reduced depressive-like behavioral deficits.

dose: not stated in the abstract · mouse (corticosterone-induced depression model) · behavioral assays, immunohistochemistry, western blot · Bu J, Liu Y, Zhao Y, Liu L, Shen J, Li Y. Paroxetine ameliorates corticosterone-induced myelin damage by promoting the proliferation and differentiation of oligodendrocyte precursor cells. Neuroscience. 2025;573:344-354. PMID: 40164278. · source

Fingolimod (FTY720) sphingosine 1-phosphate receptor modulator

acts on S1P receptors; regulates Bdnf expression via lncRNAs Hotair and Malat1

Fingolimod treatment enhanced OPC myelination three times compared to control in rat primary glial culture; coordinated the role of lncRNAs Hotair and Malat1 on Bdnf expression; Malat1 implicated in the final stages of intrinsic oligodendrocyte myelination.

dose: not stated in the abstract · rat primary glial culture and isolated OPCs · DNAzyme knockdown of lncRNAs, immunostaining, RT-qPCR · Khani-Habibabadi F, Zare L, Sahraian MA, Javan M, Behmanesh M. Hotair and Malat1 Long Noncoding RNAs Regulate Bdnf Expression and Oligodendrocyte Precursor Cell Differentiation. Mol Neurobiol. 2022;59:4209-4222. PMID: 35499794. · source

Estradiol (17beta-estradiol) estrogen

acts on estrogen receptor alpha (ERalpha) and beta (ERbeta) on oligodendroglial cells

Estradiol activates both ERalpha and ERbeta through ERE- and AP-1-driven promoters in the N20.1 mouse oligodendrocyte/astrocyte cell line; selective ER modulators raloxifene analog LY117018 and 4-hydroxytamoxifen also show activity, suggesting ER-mediated neuroprotection pathways in oligodendroglia.

dose: 100 nM (in vitro) · mouse N20.1 oligodendroglial cell line · transient cotransfection assay with ERE- and AP-1-driven reporter, luciferase readout · Guzman CB, Deighton-Collins S, Martinez A, Kleerekoper M, Zhao C, Benjamins JA et al. Activity of estradiol and selective estrogen receptor modulators in the mouse N20.1 oligodendrocyte/astrocytes cell line. Neuro Endocrinol Lett. 2005;26:526-532. PMID: 16264406. · source

Siponimod sphingosine-1-phosphate receptor modulator

acts on S1P1 and S1P5 receptors on OPCs and mature oligodendrocytes

Exerts direct pro-remyelinating effects on OPCs independent of its immunomodulatory action; accumulating evidence from in vitro, animal models and human studies supports effects on OPC recruitment and differentiation.

dose: not stated in the abstract · human and animal models · systematic review (in vitro, in vivo, clinical evidence) · Ricigliano VAG et al. 2026. Effects of sphingosine-1-phosphate receptor modulators on remyelination in multiple sclerosis: evidence from in vitro experiments, animal models and human studies. Front Immunol. 2026. PMID: 42780639. · source

Bazedoxifene selective estrogen receptor modulator

acts on estrogen receptors on oligodendrocytes

Restores myelin and oligodendrocyte-related markers in Alzheimer's disease mouse model brain and attenuates associated cognitive deficits.

dose: not stated in the abstract · mouse, Alzheimer's disease model · in vivo pharmacology; immunohistochemistry and behavioural testing · Xu MY et al. 2026. Bazedoxifene restores myelin changes and attenuates cognitive deficits in a mouse model of Alzheimer's disease. J Alzheimers Dis. 2026. PMID: 42821606. · source

Opicinumab (anti-LINGO-1) monoclonal antibody

acts on LINGO-1 (leucine-rich repeat and immunoglobulin domain-containing Nogo receptor-interacting protein 1)

Blocks LINGO-1, a membrane protein that suppresses myelination; shows robust remyelinating activity in animal models; Phase 2 clinical trial ongoing for relapsing MS. Functional activity requires engagement at a secondary binding site distinct from the primary epitope.

dose: not stated in the abstract · animal models; human Phase 2 · preclinical pharmacology; Phase 2 clinical trial · Hanf KJM et al. 2020. Functional activity of anti-LINGO-1 antibody opicinumab requires target engagement at a secondary binding site. mAbs. 2020. PMID: 31928294. · source

Clobetasol glucocorticoid / Smoothened agonist (repurposed)

acts on Smoothened (SMO) / Hedgehog pathway; RXRgamma

Identified by drug repositioning screen as a Smoothened agonist that promotes myelin gene expression (MBP, PLP) at the premyelination stage of OPC maturation; also activates RXRgamma.

dose: not stated in the abstract · mouse oligodendrocyte cell line (Oli-neu) and primary rat OPCs · drug repositioning screen; in vitro pharmacology · Porcu G et al. 2015. Clobetasol and Halcinonide Act as Smoothened Agonists to Promote Myelin Gene Expression and RXRgamma Receptor Activation. PLoS One. 2015. PMID: 26658258. · source

MCT2 substrate / ketogenic diet (MCT2 pathway) monocarboxylate transporter substrate / dietary intervention

acts on monocarboxylate transporter 2 (MCT2; SLC16A7) on myelinating oligodendrocytes

MCT2 is expressed by myelinating oligodendrocytes and is downregulated in progressive MS; deletion of MCT2 in oligodendrocytes causes myelin thinning and axonal degeneration, establishing MCT2-mediated monocarboxylate transport as essential for myelin and axonal integrity.

dose: not applicable (genetic deletion model) · mouse (conditional knockout) · conditional gene deletion; electron microscopy; electrophysiology · Izagirre-Urizar L et al. 2026. Monocarboxylate transporter 2 regulates maintenance of myelin and axonal integrity by oligodendrocytes. Nat Commun. 2026. PMID: 42315503. · source

Olesoxime cholesterol-like mitochondrial compound

acts on mitochondria / microtubule dynamics in oligodendrocytes

Favors oligodendrocyte maturation in culture and promotes myelin regeneration in rodents by a mechanism involving a functional interplay between mitochondria and microtubules.

dose: not stated in the abstract · rat (in vitro and in vivo) · cell culture; rodent demyelination model · Magalon K et al. 2016. Olesoxime favors oligodendrocyte differentiation through a functional interplay between mitochondria and microtubules. Neuropharmacology. 2016. PMID: 27618742. · source

Every row rests on a PubMed abstract read in full by golden.goose on 2026-09-12; a dose not stated in the abstract is written as such, never guessed. Research reference, not medical advice.