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zolpidem tartrate (Intermezzo / zolpidem, TransOral)

✓ Approved

Transcept Pharmaceuticals · GABRA1 · 小分子

什么是 zolpidem tartrate？

zolpidem tartrate 是一种小分子，由Transcept Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)、Sublingual (SL)/Oral Transmucosal。

药物档案

商品名Intermezzo, zolpidem, TransOral
公司Transcept Pharmaceuticals
药物类别小分子
分子靶点GABRA1
给药途径Oral (PO), Sublingual (SL)/Oral Transmucosal
状态Approved
来源： ClinicalTrials.gov, Transcept Pharmaceuticals

作用机制

分子靶点

zolpidem tartrate 作用于 1 个分子靶点：

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

zolpidem tartrate 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersInsomnia✓ Approved

相关研究文献

PubMedJournal of dental sciences2026-10-25

Runt-related transcription factor 2 transcriptionally represses sirtuin 1 to regulate osteoclastogenesis and tooth eruption.

Li Jie J, Yan Changqing C, Sun Xinyi X, Zhang Chenying C et al.

Cleidocranial dysplasia (CCD), caused by Runt-related transcription factor 2 (RUNX2) haploinsufficiency, features delayed tooth eruption. Although impaired osteoclastogenesis contributes to eruption failure, the direct molecular mechanisms linking RUNX2 deficiency to osteoclast dysfunction remain elusive. Sirtuin 1 (SIRT1) is a critical regulator of osteoclastogenesis; however, whether it serves as a downstream effector of RUNX2 remains unexplored. This study aimed to elucidate the mechanistic link between RUNX2 and SIRT1 in regulating osteoclast differentiation and tooth eruption. Tooth eruption and osteoclast differentiation were assessed by microcomputed tomography and histological analysis in Runx2 +/- mice. Chromatin immunoprecipitation quantitative polymerase chain reaction and luciferase reporter assays confirmed RUNX2 binding to the Sirt1 promoter. Osteoclast marker expression was evaluated by reverse transcription quantitative polymerase chain reaction and western blotting. Bone marrow-derived macrophages from Runx2 +/- mice were transfected with small interfering RNA targeting SIRT1 for rescue experiments. Osteoclast differentiation and function were assessed by tartrate-resistant acid phosphatase (TRAP) staining and bone resorption assays. Runx2 +/- mice showed significantly reduced mandibular first molar eruption and decreased TRAP-positive osteoclasts, accompanied by SIRT1 upregulation. RUNX2 directly bound to the Sirt1 promoter and repressed its transcription. SIRT1 knockdown increased expression levels of osteoclast markers and elevated acetylation of NF-κB p65 at lysine 310. Importantly, SIRT1 knockdown rescued osteoclast formation and resorption to wild-type levels in Runx2 +/- cells. RUNX2 haploinsufficiency impairs tooth eruption through transcriptional derepression of SIRT1, which inhibits osteoclastogenesis via NF-κB p65 deacetylation, highlighting the RUNX2-SIRT1 axis as a novel therapeutic target for CCD.

PMID 42924197
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PubMedFrontiers in cell and developmental biology2026-10-25

Potential anti-osteoporotic and anti-inflammatory potential of plant derived extracts and column semi-purified fractions of Epimedium brevicornum.

Ding Nan N, Wang Baohui B

Osteoporosis is characterized by excessive bone resorption and impaired bone remodeling, often accompanied by inflammatory processes that exacerbate skeletal deterioration. Natural products with multi-target potential have gained attention as alternative therapeutic strategies. The present study aimed to investigate the in-vitro anti-osteoporotic and anti-inflammatory potential of extracts obtained from different parts of Epimedium brevicornum, including leaves, stem, and roots, as well as isolated column semi-purified fractions (E-B-1 C, E-B-2 C, E-B-3 C, and E-B-4 C) derived from the leaf extract. Crude methanolic extracts and leaf-derived semi-purified fractions were prepared using column chromatography and evaluated for inhibitory activity against key enzymes involved in bone resorption and remodeling, including tartrate-resistant acid phosphatase (TRAP), cathepsin K, matrix metalloproteinase-9 (MMP-9), and matrix metalloproteinase-13 (MMP-13). Anti-inflammatory activity was assessed through inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). Enzyme inhibition assays were conducted at varying concentrations to determine percentage inhibition and IC50. All tested extracts and fractions demonstrated concentration-dependent inhibition across the evaluated targets. Among the semi-purified fractions, E-B-2 C and E-B-3 C generally showed stronger inhibitory activities against bone resorption-related enzymes, whereas E-B-1 C exhibited the strongest inhibition of 5-LOX. The IC50 values ranged from 95.22 to 462.37 μg/mL across the six enzymatic targets. Overall, the semi-purified fractions showed greater inhibitory potency than the crude extracts. The findings suggest that Epimedium brevicornum may serve as a promising natural source of bioactive compounds with dual anti-osteoporotic and anti-inflammatory properties. Further investigations focusing on isolation, structural characterization, and in-vivo validation are warranted to confirm therapeutic potential.

PMID 42923117
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PubMedActa ophthalmologica2026-10-24

Therapeutic efficacy and systemic pharmacokinetics of a dual-drug hydrogel contact lens for sustained glaucoma therapy.

Varshitha Vangol V, Sankararajan Umadevi U

Conventional topical therapy for glaucoma is limited by poor ocular bioavailability, rapid precorneal drug loss, frequent dosing and systemic absorption through the nasolacrimal pathway, which may reduce therapeutic efficacy and increase the risk of adverse effects. Drug-eluting hydrogel contact lenses have emerged as a promising strategy to overcome these limitations by enabling sustained ocular drug delivery. This study aimed to evaluate the therapeutic efficacy, ocular biocompatibility and systemic pharmacokinetic profile of an optimized dual-drug-loaded HEMA-based hydrogel contact lens delivering timolol maleate (TM) and brimonidine tartrate (BT) for sustained glaucoma management. Optimized hydrogel contact lenses composed of 2-hydroxyethyl methacrylate (HEMA), N, N-dimethylacrylamide (DMA), N-vinylpyrrolidone (NVP) and ethylene glycol dimethacrylate (EGDMA) were fabricated by UV photopolymerization and loaded with TM and BT (4 mg/mL each). Ocular biocompatibility was assessed using the modified Draize irritation test. Therapeutic efficacy was evaluated in a steroid-induced ocular hypertension New Zealand White rabbit model by monitoring intraocular pressure (IOP) for 24 h. Systemic drug exposure was determined by validated high-performance liquid chromatography (HPLC) analysis of plasma samples, while ocular safety was further confirmed through histopathological examination. The optimized hydrogel lens exhibited excellent ocular biocompatibility, with a maximum Draize score of 0.33 ± 0.12 that resolved completely within 48 h and no histopathological evidence of ocular tissue damage. In hypertensive rabbits, the dual-drug hydrogel lens maintained normotensive IOP (16.1 ± 0.8 mmHg) for 24 h, representing a 43.5% reduction from baseline and significantly outperforming conventional eye drops beyond 4 h (p < 0.01). Plasma concentrations of both TM and BT remained below the limit of quantification (<2.0 ng/mL) throughout the study, whereas conventional eye drops produced measurable systemic exposure (TM: 18.4 ± 2.1 ng/mL; BT: 8.2 ± 1.2 ng/mL), demonstrating effective minimization of systemic drug absorption. The optimized dual-drug-loaded hydrogel contact lens provided sustained intraocular pressure reduction, excellent ocular biocompatibility and negligible systemic drug exposure compared with conventional topical therapy. These findings highlight its potential as a sustained ocular drug-delivery platform capable of improving therapeutic efficacy, reducing systemic adverse effects and enhancing long-term treatment adherence in glaucoma management. Further long-term preclinical investigations and clinical studies are warranted to support clinical translation.

PMID 42920388
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PubMedInorganic chemistry2026-10-23

Structural Characterization of the Forensic Sodium Rhodizonate Test for Lead.

Kukucka Alex A, Thrush Devin W DW, McHenry Trent A TA, Jarošová Markéta M et al.

The forensic sodium rhodizonate test is used to detect lead in gunshot debris. Areas of interest are sprayed with a sodium rhodizonate solution followed by a tartrate buffer solution of pH 2.8, producing a deep red compound indicative of lead and other metals. A confirmatory hydrochloric acid spray produces a violet color specific to lead. The associated chemical transformations of the insoluble lead rhodizonate complexes have not been specified. Lead rhodizonate, lead rhodizonate tartrate, and lead rhodizonate chloride coordination polymers were synthesized from dilute solutions of sodium rhodizonate and lead nitrate in water, tartrate buffer, and HCl buffer. Nanoparticles of the precipitates were analyzed by three-dimensional electron diffraction (3D ED). A crystal, Pb24+(C6O6)2-Cl22-·3H2O, was characterized in the space group R3̅m (a = 8.0708(3) Å, c = 16.576(3) Å), with rhodizonate layers bidentately coordinated to three lead ions, offset by ca. 0.05 Å from the rhodizonate planes. Solid-state nuclear magnetic resonance revealed the presence of a single axial lead site in the nitrate precipitate, a distribution of lead sites in the lead rhodizonate tartrate precipitate, and three distinct sites in the lead rhodizonate chloride precipitate, suggesting other Pb compounds in the bulk coexisting with the 3D ED product.

PMID 42916903
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PubMedWaste management (New York, N.Y.)2026-10-23

Simultaneous multi-element recovery from spent LiFePO4 batteries by diethyl tartrate-assisted hydrothermal leaching.

Xu Haiqing H, Cai Longhao L, Guan Qian Q, Zeng Guisheng G et al.

Sustainable recycling of spent LiFePO4 (LFP) batteries is essential for protecting both resources and environment. Conventional hydrometallurgical methods focus primarily on Li recovery, yet they depend on corrosive acids and external oxidants while generating phosphorus-rich iron residues-posing significant economic and environmental challenges. To address these issues, we propose an innovative diethyl tartrate-based hydrothermal treatment method that facilitates acid- and oxidant-free recycling of spent LFP cathode materials. By carefully controlling the leaching conditions, selective release exceeds 98% for Li and P, whereas Fe leaching remains negligible at 0.3%. Mechanistic studies confirmed that the high-efficiency leaching of Li and P is attributed to the combined effect of acetic acid and tartaric acid produced by the hydrothermal reaction of diethyl tartarate. Moreover, the high-quality Li3PO4 was prepared from leaching filtrate via purification-precipitation, and the purity of 99.08% FeC4H4O6 was obtained from leaching residue via redissolving-precipitation. This work establishes a sustainable, efficient pathway to fully recover valuable resources from spent LFP batteries.

PMID 42914664
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PubMedOrganic letters2026-10-23

Photoinduced Palladium-Catalyzed Cross-Coupling of Chloroacetamides with Alkenes and Heteroarenes.

Zhao Jun-Fei JF, Yuan Binfang B, Yang Zhi Z, Yan Qiu-Ping QP et al.

A visible light-induced palladium catalyzed intramolecular and intermolecular C(sp3)-C(sp2) cross-coupling reaction has been established. This synthetic method exhibits broad functional group tolerance and a wide substrate scope including bioactive molecules, pharmaceutical scaffolds, and peptides, enabling access to structurally novel β,γ-unsaturated amides, benzazepine derivatives as bioisosteres of sedative-hypnotic 1,4-benzodiazepine drugs, and heterocyclic acetamides. Moreover, it offers a direct route to commercially relevant pharmaceuticals such as zolpidem and alpidem. Notably, the successful synthesis of key inhibitors─including those targeting KDM5B, JNK1, and PDE10A─highlights the practical significance and broad applicability of this method. The reaction mechanism was explored using control experiments, Stern-Volmer fluorescence quenching experiments, light on/off experiments, and density functional theory (DFT) calculations.

PMID 42918069
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