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Потенциал репродукции клемастина для поощрения воспоминаний.

Белая материя в центральной нервной системе включает в себя связанные нервные волокна, миелинированные олигодендроцитами. Увечье белого тела, характеризующееся потерей олигодендроцитов и миелина, часто встречается после ишемической травмы мозга, подстрекательских демиелинизирующих заболеваний, включая множественный склероз, и таких травм, как повреждение спинного мозга. В настоящее время не было установлено никаких методов лечения, которые способствовали бы воспоминанию об этих заболеваниях. За последнее десятилетие в различных докладах говорилось о том, что антимукаринский наркотик может стим

Совпадение в аннотации оригинала
White matter in the central nervous system comprises bundled nerve fibers myelinated by oligodendrocytes. White matter injury, characterized … these diseases. Over the past decade, various reports have suggested that the anti-muscarinic drug clemastine can stimulate remyelination by oligodendrocytes. Consequently, the repurposing of clemastine as a potential treatment for a variety of neurological disorders has gained significant attention. The therapeutic effects of clemastine have been demonstra …

Clemastine effects in rat models of a myelination disorder.

BackgroundPelizaeus Merzbacher disease (PMD) is a dysmyelinating disorder of the central nervous system caused by impaired differentiation of oligodendrocytes. This study was prompted by findings that antimuscarinic compounds enhance oligodendrocyte differentiation and remyelination in vitro. One of these compounds, clemastine fumarate, is licensed for treatment of allergic conditions. We tested whether clemastine fumarate can promote myelination in two rodent PMD models, the myelin-deficient and the PLP transgenic rat.MethodsPups were treated with daily injections of clemastine (10-30 mg/kg/d…

Effects of clemastine, ketotifen and prednisolone on chloroquine-induced pruritus.

The effects of single doses of placebo, clemastine, ketotifen and prednisolone on chloroquine-induced pruritus were investigated in healthy black African volunteers using a visual analogue scale. There was no significant differences between the mean percentage degrees of pruritus recorded with placebo, clemastine and ketotifen. By contrast, the mean percentage degree of pruritus recorded with prednisolone was significantly lower than those with the other three treatments. If these results are confirmed in patients with malaria, it might be more rational to administer a single prophylactic dose…

Clemastine/tamoxifen hybrids as easily accessible antileishmanial drug leads.

A library of hybrid molecules is developed based on the common chemical features shared by clemastine and tamoxifen both of which are well known for their antileishmanial activities. In the initial screening against Leishmania major and L. amazonensis promastigotes, as well as cytotoxicity assays using HepG2 cells, several hybrids showed submicromolar activity against the parasite and no toxicity against human cells. The compounds with an EC50 < 2 μM against promastigotes of both species and a selectivity index >10 were further characterized against intracellular amastigotes as well as promast…

The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations.

Studies were conducted in healthy male volunteers (n = 171; age range, 19-49 years; 22-27 subjects per study) to examine the following: pharmacokinetics and dose proportionality of the antihistamine clemastine; the effect of coadministration of phenylpropanolamine and clemastine on the pharmacokinetics of the two drugs; and the bioavailability of clemastine tablets and combination tablets of clemastine and sustained-release phenyl-propanolamine under fasted and fed conditions after single-dose administration and at steady state. All studies used crossover designs, with randomized drug treatmen…

Clemastine enhances exercise-induced motor improvement in hypoxic ischemic rats.

Neonatal hypoxic ischemia (HI) occurs owing to reduced cerebral oxygen levels and perfusion during the perinatal period. Brain injury after … p. We further evaluated the effect of myelination promotion on rotarod performance by administering clemastine, a myelination-promoting drug, via daily intraperitoneal injections. Clemastine did not enhance motor improvement in untrained-HI rats. However, clemastine-administered trained-HI rats (n = 7) exhibited significantly improved motor performance compa …

Появляющееся терапевтическое применение клемастина: обзор последних обновлений патентов.

Клемастин, антигистамин первого поколения, традиционно используемый для лечения аллергического ринита и уртикарии, недавно вызвал интерес в связи с его потенциальным терапевтическим применением, выходящим за пределы его антигистаминергических свойств. В настоящем обзоре рассматриваются недавние патентные заявки (2015 - 2024 годы), с тем чтобы прояснить формирующийся терапевтический ландшафт для этого комплекса. Анализ показывает различные потенциальные виды применения, включая нейродегенеративные расстройства, сердечно-сосудистые заболевания и лечение рака. В частности, в ряде исследований осн

Совпадение в аннотации оригинала
Clemastine, a first-generation antihistamine traditionally used for treating allergic rhinitis and urticaria, has recently gathered interest due to its potential therapeutic applications beyond its antihistaminergic properties. This review examines recent patent filings (2015-2024) to elucidate the emerging therapeutic landscape for this compound. The analys…

Clemastine protects against sepsis-induced myocardial injury in vivo and in vitro.

Sepsis-induced myocardial dysfunction (SIMD) is associated with high morbidity and mortality rates; however, it lacks targeted therapies. Modulating cardiomyocyte autophagy maintains intracellular homeostasis during SIMD. Clemastine, a histamine receptor inhibitor, promotes autophagy and other effective biological functions. Nevertheless, the effect of clemastine on SIMD remains unclear. This study aimed to explore the underlying mechanism of clemastine in cardiomyocyte injury in cecum ligation and perforation (CLP)-induced rats and lipopolysaccharide (LPS)-stimulated H9c2 cells. Clemastine (1…

Systematic Analysis of Clemastine, a Candidate Apicomplexan Parasite-Selective Tubulin-Targeting Agent.

Apicomplexan parasites, such as Toxoplasma gondii, Plasmodium spp., Babesia spp., and Cryptosporidium spp., cause significant morbidity and mortality. Existing treatments are problematic due to toxicity and the emergence of drug-resistant parasites. Because protozoan tubulin can be selectively disrupted by small molecules to inhibit parasite growth, we assembled an in vitro testing cascade to fully delineate effects of candidate tubulin-targeting drugs on Toxoplasma gondii and vertebrate host cells. Using this analysis, we evaluated clemastine, an antihistamine that has been previously shown t…

Clemastine rescues myelination defects and promotes functional recovery in hypoxic brain injury.

Hypoxia can injure brain white matter tracts, comprised of axons and myelinating oligodendrocytes, leading to cerebral palsy in neonates and … eloped the rare condition DPHL and made a nearly complete recovery in the setting of treatment with clemastine, a widely available antihistamine that in preclinical models promotes oligodendrocyte precursor cell differentiation. This suggested possible therapeutic benefit in the more clinically prevalent hypoxic injury of newborns, and we demonstrate in muri …

Effectiveness of clemastine fumarate for treatment of rhinorrhea and sneezing associated with the common cold.

Limited data support the use of first-generation antihistamines for treatment of the common cold. The purpose of this study was to test the effectiveness of clemastine fumarate, a first-generation antihistamine, for treatment of sneezing and rhinorrhea associated with naturally occurring common colds. Four hundred three subjects (202 clemastine fumarate recipients and 201 placebo recipients) who reported new onset (< 24 hours) of cold symptoms that included rhinorrhea or sneezing were studied. At baseline (day 1), the mean symptom-severity scores +/- SEM for the clemastine fumarate and placebo…

Randomized controlled trial of clemastine fumarate for treatment of experimental rhinovirus colds.

We used a rhinovirus challenge model to test the therapeutic efficacy of clemastine fumarate for reducing sneezing and nasal secretion in a double-blind, randomized clinical trial. Clemastine fumarate (1.34 mg) or placebo was administered at 8 A.M. and 8 P.M. for 4 days, beginning 24 hours, 36 hours, 48 hours, and 60 hours after viral challenge. Infected evaluable subjects who received clemastine (n = 75) had reduced sneeze-severity scores compared with those who received placebo (n = 75) on illness days 2 (0.3 vs. 0.5; P = .003), 3 (0.4 vs. 0.8; P = .0003), 4 (0.3 vs. 0.5; P = .025), and 5 (0…

Remyelination-oriented clemastine treatment attenuates neuropathies of optic nerve and retina in glaucoma.

As one of the top causes of blindness worldwide, glaucoma leads to diverse optic neuropathies such as degeneration of retinal ganglion cells … ligodendroglial lineage cells were responsible for the subsequent neuropathology. By treatment with clemastine, an Food and Drug Administration (FDA)-approved first-generation antihistamine medicine, we demonstrate that the optic nerve and retina damages were attenuated via promoting oligodendrocyte precursor cell (OPC) differentiation and enhancing remyelin …

Клемастин фумарат ускоряет аккумуляцию инвалидности в прогрессивном множественном склерозе, усиливая пироптоз.

Множественный склероз (MS) — иммунопосредованное демиелинизирующее заболевание центральной нервной системы (CNS). Клемастин фумарат, внезапный антигистамин и мускариновый блокатор рецепторов, обладает ремиелионирующим потенциалом в MS. Климастичная рука была добавлена в текущее клиническое испытание платформы TRAP-MS ( &quot; TRP-MS &quot; )NCT03109288) для выявления сигнатуры ремиелинирования цереброспиновой жидкости (CSF) и для сбора данных о безопасности клемастина у пациентов независимо от рецидива (PIRA). Клемастинская рука была остановлена в соответствии с определенными протоколом критер

Совпадение в аннотации оригинала
Multiple sclerosis (MS) is an immune-mediated demyelinating disease of the central nervous system (CNS). Clemastine fumarate, the over-the-counter antihistamine and muscarinic receptor blocker, has remyelinating potential in MS. A clemastine arm was added to an ongoing platform clinical trial TRAP-MS (NCT03109288) to identify a cerebrospinal fluid (CSF) remy…

Effects on mouse melanoma and immune cells of P2X7 receptor positive allosterism by clemastine.

Clemastine (CLE), an H1R antagonist widely used for the treatment of allergic rhinitis, has recently been investigated for its positive modulatory effects on P2X7, a receptor for extracellular ATP (eATP) involved in the regulation of inflammation, immune responses, and the composition of the tumor microenvironment (TME). Here, we further examined the effects of CLE on P2X7-mediated responses to clarify the pharmacological significance of P2X7 potentiation. First, in murine and human cells expressing (B16F10 WT and HEK293-hP2X7) or lacking (B16F10 P2X7-/- and HEK293 WT) the P2X7 receptor, we me…

Effect of Clemastine on Neurophysiological Outcomes in an Ovine Model of Neonatal Hypoxic-Ischemic Encephalopathy.

Originally approved by the U.S. Food and Drug Administration (FDA) for its antihistamine properties, clemastine can also promote white matter integrity and has shown promise in the treatment of demyelinating diseases such as multiple sclerosis. Here, we conducted an in-depth analysis of the feasibility, safety, and neuroprotective efficacy of clemastine administration in near-term lambs (n = 25, 141-143 days) following a global ischemic insult induced via an umbilical cord occlusion (UCO) model. Lambs were randomly assigned to receive clemastine or placebo postnatally, and outcomes were assess…

A comparison of acrivastine versus clemastine and placebo in the treatment of patients with chronic idiopathic urticaria.

Twenty patients of mean age 41.3 years, with a diagnosis of chronic idiopathic urticaria were assessed in a fully randomized, double-blind, crossover study to investigate the efficacy of acrivastine at two doses (8 mg and 4 mg) versus 1 mg clemastine and placebo, given three times per day. All active preparations were found to be effective, and significantly better than placebo, in controlling the signs and symptoms of urticaria. There was a higher incidence of sedation with clemastine than with either acrivastine or placebo, although this difference did not achieve statistical significance in…

TH1177, Clemastine, and Benzhydryl Derivatives Act as Novel Extracellular Blockers of ORAI Channels.

ORAI channels are store-operated Ca2+ channels, which play important roles in physiology and pathophysiology. ORAI channel modulators are useful for developing pharmacological interventions. Here, we aimed to investigate the benzhydryl-derived analogues as novel ORAI channel blockers. The effects of benzhydryl-derived analogues TH1177, clemastine, cloperastine, and diphenhydramine were investigated in HEK-293 cells overexpressing individual ORAI isoforms and STIM1. The ORAI currents were recorded by patch-clamp, and cytosolic Ca2+ was measured by a fluorescent Ca2+ dye. TH1177 inhibited ORAI1,…

Клемастин фумарат ускоряет аккумуляцию инвалидности в прогрессивном множественном склерозе, усиливая пироптоз.

Множественный склероз (MS) — иммунопосредованное демиелинизирующее заболевание CNS. Клемастин фумарат, внезапный антигистамин и мускариновый блокатор рецепторов, обладает ремиелионирующим потенциалом в MS. Климастичная рука была добавлена в текущее клиническое исследование платформы, нацеленное на остаточную активность на основе точности, биомаркированной комбинированной терапии множественных склерозов (TRAP-MS) (Clinical Procures.gov). NCT03109288), для выявления сигнатуры ремиелинирования цереброспиновой жидкости (CSF) и для сбора данных о безопасности клемастина у пациентов независимо от ре

Совпадение в аннотации оригинала
Multiple sclerosis (MS) is an immune-mediated demyelinating disease of the CNS. Clemastine fumarate, the over-the-counter antihistamine and muscarinic receptor blocker, has remyelinating potential in MS. A clemastine arm was added to an ongoing platform clinical trial, targeting residual activity by precision, biomarker-guided combination therapies of multip…

Antileishmanial Chemotherapy through Clemastine Fumarate Mediated Inhibition of the Leishmania Inositol Phosphorylceramide Synthase.

Current chemotherapeutics for leishmaniasis have multiple deficiencies, and there is a need for new safe, efficacious, and affordable medicines. This study describes a successful drug repurposing approach that identifies the over-the-counter antihistamine, clemastine fumarate, as a potential antileishmanial drug candidate. The screening for inhibitors of the sphingolipid synthase (inositol phosphorylceramide synthase, IPCS) afforded, following secondary screening against Leishmania major (Lmj) promastigotes, 16 active compounds. Further refinement through the dose response against LmjIPCS and …