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diazepam (Stesolid / diazepam, Alpharma)

✓ Approved

Pfizer, Inc. · GABRA1 · 小分子

什么是 diazepam？

diazepam 是一种小分子，由Pfizer, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Rectal。

药物档案

商品名Stesolid, diazepam, Alpharma
公司Pfizer, Inc.
药物类别小分子
分子靶点GABRA1, GABRA2, GABRA3, GABRA5
给药途径Rectal
状态Approved
来源： ClinicalTrials.gov, Pfizer, Inc.

作用机制

分子靶点

diazepam 作用于 4 个分子靶点：

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
GABRA2gamma-aminobutyric acid type A receptor alpha2 subunit (DEE78, EIEE78)
GABRA3gamma-aminobutyric acid type A receptor alpha3 subunit (EPILX2)
GABRA5gamma-aminobutyric acid type A receptor alpha5 subunit (EIEE79, DEE79)
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

diazepam 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAnxiety✓ Approved
Nervous system disordersEpilepsy✓ Approved

相关研究文献

PubMedNeuroscience letters2026-07-26

Diazepam, a positive allosteric modulator of the GABAA receptor induces strain-specific responses in object recognition, ultrasonic vocalizations and monoaminergic profiles in the Wistar Kyoto rat model of endogenous depression.

Inavally Akshata T AT, Sadananda Monika M

Major depressive disorder (MDD) involves cognitive impairment, altered affective states and dysregulation of neurotransmitter homeostasis. The Wistar Kyoto (WKY) rat is characterized by inherent depressive-like behaviour, anxiety, cognitive deficits and dysregulated monoaminergic/GABAergic neurotransmission. This study investigated strain-specific differences in learning and memory, affective states and neurochemical responses to Diazepam (DZP), a positive allosteric modulator of the GABAA receptor, in Wistar and WKY rats. Learning and memory were assessed using the novel object recognition (NOR) paradigm, affective states through ultrasonic vocalizations (USVs) emitted, and monoaminergic levels in implicated brain areas using HPLC. DZPs significantly impaired NOR in Wistar, evidenced by reduced discrimination and recognition index (p < 0.05). DZP also increased contacts and approaches to familiar objects in Wistar (p < 0.05) and reduced approaches to novel objects in both Wistar (p < 0.01) and WKY (p < 0.001). DZP lowered bandwidth of 50-kHz USVs across both strains, though no DZP × strain interactions were observed on all acoustic and spectral parameters analyzed. WKYs displayed significantly lower baseline dopamine (DA) and serotonin (5-HT) in both PFC (DA: p < 0.001; 5-HT: p < 0.01) and hippocampus (DA: p < 0.01; 5-HT: p < 0.05). DZP reduced prefrontal (p < 0.001) and hippocampal DA (p < 0.001) levels in Wistar, with no effect in WKY, though DZP × strain interaction indicated differential effects on DA levels. Prefrontal 5-HT (p < 0.05) was also reduced in DZP-treated Wistars. Thus, strain-specific differences of the dopaminergic response to DZP and the finding that DZP's affected more cognitive measures in Wistar than in WKY underscores the importance of strain and individual variability in translational research.

PMID 42501815
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PubMedEnvironmental toxicology and pharmacology2026-07-25

Perfluorohexane sulfonate (PFHxS) modulates conformational transitions, ligand-binding functions and aggregation of human serum albumin.

Suramya Suramya S, Muthu Shivani A SA, Chauhan Chanchal C, Qureshi Afnaan A et al.

Perfluorohexane sulfonate (PFHxS), a persistent short-chain member of perfluoroalkyl substances (PFAS) family, exhibits a long biological half-life and widespread human exposure, raising toxicological concerns. Human serum albumin (HSA), the most abundant plasma protein, regulates transport of xenobiotics, including PFAS, yet the effects of PFHxS binding remain unclear. This study examined PFHxS-HSA interactions across pH-dependent isomeric states using an integrated approach. PFHxS preferentially bound to hydrophobic cavities, particularly Sudlow's site I, via hydrophobic and electrostatic interactions, supported by docking, molecular dynamics, and molecular mechanics/Poisson-Boltzmann surface area (MM-PBSA) analyses. Spectroscopic data revealed isomer-specific conformational changes, reduced α-helical content, and stabilization of partially unfolded intermediates. At physiological pH, PFHxS displaced diazepam, indicating impaired drug-binding capacity. PFHxS also remodeled the aggregation pathway of HSA, promoting smaller oligomeric species rather than amyloid-like aggregates. Conclusively, PFHxS acts as an active modulator of HSA structure and function, influencing ligand transport, bioavailability, and pharmacokinetics, underscoring potential risks of persistent environmental PFAS exposure to human health.

PMID 42498051
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PubMedFrontiers in immunology2026-07-25

Immunological mechanisms and prevention strategies for febrile seizures in children.

Chen Binbin B, Tao Enfu E

Febrile seizures (FS) affect 2-5% of children globally, causing significant caregiver anxiety and healthcare utilization. Emerging evidence implicates neuroinflammation and T-cell-mediated immunity in FS pathogenesis, suggesting potential targets for future investigation. This Review synthesizes current evidence on FS prevention, emphasizing a paradigm shift from universal pharmacological approaches toward risk-stratified, personalized strategies. The COVID-19 pandemic provided unique insights: non-pharmaceutical interventions reduced FS incidence by 54-70%, while the Omicron variant emerged as a novel trigger associated with complex FS features. Prevention is conceptualized within a three-level framework: primary prevention targets all children through vaccination (MMR, PCV13, COVID-19 vaccines) and infection control; secondary prevention focuses on high-risk children with prior FS, where risk stratification integrates clinical predictors (complex features, young age, low fever), biomarkers (hyponatremia, zinc/vitamin D deficiency, inflammatory indices), and pathogen-specific risks (influenza A, Omicron); tertiary prevention addresses complications and epileptogenesis in children with complex FS or genetic predisposition (SCN1A, PCDH19). Key immunological mechanisms include HMGB1-NLRP3 inflammasome activation, TRPV1-mediated Th17 differentiation, and IL-1β/IL-10 dysregulation. Antipyretics do not prevent FS recurrence during distant febrile episodes, while intermittent benzodiazepines (diazepam, intranasal midazolam) effectively reduce early recurrence in high-risk children (NNT = 6.8), albeit with adverse effects in up to 36%. Emerging frontiers include novel therapeutic targets (HMGB1 inhibitors, TRP channel modulators, TSP-1 pathway inhibitors) and non-pharmacological innovations (wearable sensors, chronotherapy). Crucially, caregiver education underpins all prevention levels, addressing high rates of parental anxiety (58.2%). This integrated framework guides clinical practice toward more individualized, risk-based management.

PMID 42500652
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PubMedFrontiers in neurology2026-07-25

Potential neuroprotective and anticonvulsant effects of Ganoderma lucidum ethanol extract and its impact on affective comorbidities associated with pentylenetetrazol kindling model of epilepsy: behavioral, biochemical and histological studies.

Abdessamad Itto Rahou IR, Leila Bikjdaouene B, Youssef Bahbiti B, Youssef Sqalli Houssaini SH et al.

Epilepsy is a chronic neurological disorder that is strongly influenced by oxidative stress and neuronal death, two major pathophysiological factors. According to various recent studies, Ganoderma lucidum extract (GLE) may have antioxidant properties. However, there is little evidence to support its effectiveness in treating epilepsy. Here, we examined the neuroprotective qualities of GLE (300 mg/kg) against seizures induced by pentylenetetrazol (35 mg/kg). Four groups of eight male Wistar rats per group were randomly assigned: control, Pentylenetetrazol (PTZ), GLE-300 and Diazepam. The animals received an intraperitoneal dose of PTZ (35 mg/kg) every 48 h (11 injections in total) for 21 days to create an epilepsy model. The Racine five-point score was used to assess seizure severity. Anxious behavior, locomotor and exploratory activity were assessed using the open field test (OFT) and the elevated plus maze test (EPM), while the forced swim test (FST) was used to assess depressive behavior. Markers of oxidative stress, including malondialdehyde (MDA), nitric oxide (NO), and the enzymatic activities of superoxide dismutase (SOD) and catalase, were measured using the 2-thiobarbituric acid method (TBA), Griess reagent, nitro blue tetrazolium (NBT) reduction, and hydrogen peroxide decomposition. We performed a histological study of the prefrontal cortex (PFC) to quantify neuronal loss in the cortical layers using Nissl staining. All in all, our results showed that GLE reduces the severity of convulsive seizures during the induction of epilepsy (p < 0.001) and alleviates anxious (p = 0.005) and depressive (p = 0.008) behaviors while reducing neuronal damage. As well as significantly reduce NO and MDA levels (p < 0.001), and restore catalase (p = 0.005) and SOD (p = 0.010) enzyme activities in biochemical evaluation. Histologically, the GLE reduces neurodegeneration in the PFC due to its antioxidant and neuroprotective properties (p = 0.003). In conclusion, the experimental results indicate that GLE significantly attenuates the behavioral, biochemical, and histological alterations induced by PTZ, thus supporting its neurotherapeutic potential in the PTZ-Kindling model of epilepsy.

PMID 42500387
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PubMedNeuroscience2026-07-24

Diazepam reduces hippocampal and behavioral plasticity, blunting environmental impact on emotional responses.

Poggini Silvia S, Veleanu Maxime M, Albanese Naomi Ciano NC, Bronnec Martin M et al.

Plasticity is essential for mental health, as it enables individuals to adapt to environmental changes. However, its effects are highly context-dependent. While increased plasticity can be beneficial in supportive environments, as treatments that enhance plasticity have proved more effective when paired with favorable experiences, it may promote maladaptive responses under adverse conditions. Accordingly, a reduction in plasticity is expected to be beneficial in adverse circumstances, as it can limit harmful influences on mental well-being. To test this hypothesis, we investigated whether diazepam, a benzodiazepine that reduces neural plasticity, thereby attenuates the impact of environmental conditions on behavioral and physiological endophenotypes of depression. In a first experiment, we treated C57BL/6 adult male and female mice with diazepam or vehicle, delivered either orally or intraperitoneally, and found a consistent impairment in synaptic plasticity, as indicated by reduced hippocampal long-term potentiation. In a second experiment, after inducing a depression-like phenotype, we treated C57BL/6 adult male mice for three weeks with diazepam or vehicle in either enriched or stressful conditions. The treatment had opposite effects depending on the environmental conditions. In enrichment, it was associated with no significant recovery from anhedonia, whereas under stress, it prevented a further worsening, relative to the control groups. Diazepam also affected anxiety-related behavioral outcomes and hypothalamic-pituitary-adrenal axis activation in an environment-dependent manner. Overall, we demonstrate that diazepam, impairing hippocampal plasticity, blunts the impact of environmental factors on the behavioral outcome. These findings underscore the potential of tailoring neural plasticity to environmental quality as a strategy in precision psychiatry.

PMID 42492890
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PubMedFrontiers in medicine2026-07-22

Intranasal Dexmedetomidine as a rescue strategy for established postoperative delirium following loss of intravenous access: a case report.

Peng Yingao Y, Liu Mingjin M, Wang Jiafang J

The clinical management of established postoperative delirium (POD) is particularly challenging in patients who exhibit agitated behavior and self-remove intravenous (IV) access. A 70-year-old man with prior cerebral infarction developed POD following urologic surgery under general anesthesia. Two doses of IV diazepam failed to provide sustained relief, and the patient subsequently self-removed his IV catheter. Intranasal (IN) dexmedetomidine was administered in a stepwise titration protocol (total dose: 100 μg). The patient transitioned from agitation to calm and entered sustained sleep within 1 h. The only hemodynamic alteration observed was mild bradycardia (heart rate: 58-65 beats/min), with no clinically significant respiratory depression occurring throughout the observation period. The Confusion Assessment Method (CAM) test result was negative on postoperative day 2, and the patient was discharged uneventfully on postoperative day 4. This case suggests that IN dexmedetomidine may offer a safe, non-invasive rescue option for established POD when IV access is unavailable.

PMID 42482906
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