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hyoscyamine sulfate

✓ Approved

Lumara Health · CHRM1 · 小分子

什么是 hyoscyamine sulfate？

hyoscyamine sulfate 是一种小分子，由Lumara Health研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

公司Lumara Health
药物类别小分子
分子靶点CHRM1, CHRM2, CHRM3, CHRM4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Lumara Health

作用机制

分子靶点

hyoscyamine sulfate 作用于 4 个分子靶点：

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
CHRM4cholinergic receptor muscarinic 4 (HM4, M4R)
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

hyoscyamine sulfate 针对 3 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersColitis ulcerative✓ Approved
Gastrointestinal disordersIrritable bowel syndrome✓ Approved
Renal and urinary disordersUrinary tract inflammation✓ Approved

相关研究文献

PubMedGels (Basel, Switzerland)2026-07-27

Fabrication of Chondroitin Sulfate-Copper/Zinc Complexes and Antibacterial Activity Involving Hydrogel Application in Infected Wound Healing.

Shen Qingshan Q, Wu Jiarui J, Li Jiawen J, Dong Yujie Y et al.

The escalating prevalence of bacterial infections has intensified the search for innovative antimicrobial strategies, particularly for infected wound management. Chondroitin sulfate (CS), a naturally occurring glycosaminoglycan with established biocompatibility, presents an attractive scaffold for developing metal ion-functionalized biomaterials. This study reports the fabrication of chondroitin sulfate-copper complex (CSCu) and chondroitin sulfate-zinc complex (CSZn) through an ion exchange method, wherein Cu2+ and Zn2+ ions bind to the groups of carboxylate, sulfate, or N-acetyl from the CS backbone. The resulting complexes exhibited copper or zinc loading capacities of about 6.6% and demonstrated potent antibacterial activity against E. coli and S. aureus. The integration of CSCu or CSZn with sodium alginate yielded a hydrogel system with a higher apparent viscosity, possessing injectability and spreadability on the skin surface and a porous three-dimensional internal structure conducive to wound healing applications. In a murine model of S. aureus-infected full-thickness wounds, topical application of CSCu and CSZn hydrogels substantially accelerated wound closure, achieving 97.46% and 98.11% healing, respectively, by day 10. Additionally, treatment with CSCu or CSZn hydrogels significantly attenuated systemic inflammatory responses, as reflected in lowered serum TNF-α, IL-1β, and IL-6 alongside increased IL-10. Histological evaluation confirmed enhanced re-epithelialization and stratum spinosum formation in treated wounds. These findings establish CSCu and CSZn as a promising bioactive agent for addressing bacterial wound infections through a dual mechanism of direct antibacterial action and immunomodulatory effects, offering a valuable alternative to conventional antibiotic therapies.

PMID 42505315
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PubMedCells2026-07-27

Changes in Expression of Syndecans and Heparan Sulfate Biosynthesis Enzymes in Short-Term Streptozotocin-Induced Diabetic Rat Kidneys.

Čujić Tanja T, Racetin Anita A, Filipović Natalija N, Kostić Sandra S et al.

The aim of this study was to determine the temporal expression patterns of syndecan family members (SDC1, SDC2, SDC4) and heparan sulfate biosynthesis enzymes (NDST1, NDST2) in kidneys of diabetic rats and age-matched controls. Male Sprague-Dawley rats received intraperitoneal streptozotocin (55 mg/kg; DM1 group) or citrate buffer (control group). Kidney samples were harvested after 2 weeks and 2 months and processed for immunofluorescence. SDC1 showed significant temporal upregulation in controls that was abolished in diabetic animals. SDC2 exhibited high early expression in the control group with significant decline as the kidneys matured but remained elevated in diabetic kidneys at 2 months compared to controls. SDC4 showed no significant difference between groups, though an age-related decrease was observed in controls. NDST1 was significantly upregulated in diabetic rats at 2 weeks, followed by profound suppression at 2 months (p < 0.0001). NDST2 showed modest but significant early elevation in diabetic animals. Transcript-level analysis of two independent public datasets of streptozotocin-induced diabetic rat renal cortex reproduced the principal directional findings-an early increase in SDC1 and a progressive elevation of SDC2-while indicating post-transcriptional regulation of SDC4 and the early NDST response. Diabetes disrupts normal temporal expression of syndecans and heparan sulfate biosynthesis enzymes in rat kidneys. Early compensatory upregulation of NDST1 and NDST2, followed by progressive NDST1 suppression, suggests a deteriorating heparan sulfate biosynthetic capacity, potentially contributing to the progression of diabetic nephropathy.

PMID 42505386
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PubMedMarine drugs2026-07-27

Bioactive Glycosaminoglycans from Caranx crysos: A Structure-Function Study of Selective Anticoagulant Activity.

Kroumi Ranim R, Alimi Soumaya S, Esposito Fabiana F, Haffouz Asma A et al.

Glycosaminoglycans (GAGs) are the carbohydrate portion of proteoglycans (PGS), a family of complex biomacromolecules ubiquitously found in the extracellular matrix and on cell surfaces that play critical roles in a plethora of physiological and pathological processes. In the present work, chondroitin sulfate (CS) and dermatan sulfate (DS) were extracted and purified from the head (GCB) and skin (GDB) of blue runner fish (Caranx crysos) to explore their structural features and biological properties. GCB and GDB were purified by ion-exchange chromatography with yields of 0.82% and 0.61%, respectively. Chemical and structural analysis showed that GCB and GDD demonstrated quite similar sulfation degrees (4.45% and 4.24%, respectively). The molecular weight values obtained for GCB and GDB as estimated by high-performance size exclusion chromatography coupled with a triple detector array (HP-SEC-TDA) were 48.9 and 28.54 KDa, respectively. Structural features were elucidated using FT-IR and 2D NMR spectroscopy. GCB was mainly identified as chondroitin sulfate, containing 82% GlcA and minor proportions of IdoA and IdoA2S (scoring 18% dermatan-like structures). In contrast, GDB was predominantly dermatan sulfate, with a higher unsulfated IdoA content (54%) and a lower GlcA percentage (17%). In vitro anticoagulant activity, evaluated using APTT and PT assays, demonstrated that both GAGs exhibit significant anticoagulant potential. In addition, both fractions exhibited no antiplatelet activity, suggesting that the isolated glycosaminoglycans selectively target the coagulation cascade without affecting platelet aggregation. Furthermore, hemolytic assays confirmed that neither GCB nor GDB showed any hemolytic activity at the tested concentrations. Cytotoxicity assessment in HEK293 and HUVEK cell lines further confirmed the absence of detectable toxicity even at high concentration. Overall, these marine-derived GAGs present promising therapeutic potential as a source of anticoagulant drugs.

PMID 42505974
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PubMedOrganic letters2026-07-27

Site-Specific Tyrosine Sulfation of Triabin via Semi-Synthesis Enhances Thrombin Inhibition through Synergistic Multiple-Mode Interactions.

Xiao Zhenbang Z, Mo Zeyuan Z, Lin Litong L, He Chunmao C

Herein, we report the semisynthesis of site-specifically sulfated triabin─a 142-amino-acid lipocalin protein─at Tyr124. Functional assays reveal that sulfation enhances anticoagulant activity by ∼5-fold, demonstrating that even rigid scaffolds can benefit from this modification. Modeling studies uncover a synergistic mechanism wherein the sulfate group engages in a hydrogen-bond network, electrostatic bridging, and charge-complementary interactions with thrombin exosite I, while the hydrophobic core (notably Phe106 and Val126) remains the primary driving force.

PMID 42503796
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PubMedPediatric pulmonology2026-07-27

Timing of Magnesium Sulfate Cessation and Apnea of Prematurity in Late-Preterm Twin Infants.

Shinohara Satoshi S, Yasuda Genki G, Kasai Mayuko M, Katsumata Nobuyuki N et al.

To evaluate the association between the timing of maternal magnesium sulfate (MgSO4) discontinuation before delivery and the risk of apnea of prematurity (AOP) in late-preterm twin infants. This retrospective cohort study included 161 twin pregnancies (322 infants) delivered between 34 0/7 and 36 6/7 weeks at Yamanashi Prefectural Central Hospital (2017-2025). Infants with major anomalies or intrauterine fetal demise were excluded. The primary exposure was the interval between MgSO4 cessation and delivery, categorized as: no exposure, < 12, 12-24, and ≥ 24 h. Two multivariable logistic regression models were constructed. Model 1 evaluated the association between any maternal MgSO4 exposure and AOP. Model 2 further incorporated the timing of MgSO4 discontinuation as a categorical exposure, adjusting for gestational age, chorionicity, small-for-gestational-age status, sex, and 1-min Apgar score. Among the 322 infants, 112 (34.8%) developed AOP. In Model 1, maternal MgSO4 exposure itself was not significantly associated with AOP. However, in Model 2, delivery within 12 h after cessation of MgSO4 was independently associated with AOP (adjusted odds ratio, 7.44; 95% confidence interval, 1.48-37.4), whereas longer discontinuation intervals (12-24 or ≥ 24 h) were not. Among late-preterm twin infants, maternal MgSO4 exposure itself was not independently associated with AOP; however, delivery soon after MgSO4 discontinuation was associated with an increased risk of AOP. These findings support consideration of MgSO4 discontinuation timing in perinatal risk assessment and neonatal respiratory monitoring and may help guide future studies.

PMID 42504155
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PubMedChemistryOpen2026-07-27

In Vivo Evaluation of Psoralen in a Copper Sulfate-Induced Chick (Gallus gallus domesticus) Emesis Model and In Silico Analysis of Its Interaction With D2, 5-HT3 A, and Muscarinic Receptors.

Chandra Kishor K, Bahar Sharif Uddin SU, Akter Khadija K, Khatun Mst Muslima MM et al.

Psoralen (PSN), a naturally occurring furocoumarin, was evaluated for its antiemetic potential using integrated in vivo and in silico approaches, considering the limitations of currently available antiemetic agents. The antiemetic activity of PSN was investigated in a copper sulfate-induced emesis model using 2-day-old chicks (Gallus gallus domesticus). A dose-dependent experimental design was employed with PSN (5, 10, and 20 mg/kg), alongside standard antiemetics (domperidone 6 mg/kg, ondansetron (OND) 5 mg/kg, and hyoscine 21 mg/kg) and combination treatments. Latency to first retch and total retching episodes were recorded, and percentage inhibition was calculated. Molecular docking was performed against D2, D3, 5-HT3A, and muscarinic (M1-M5) receptors. ADMET and toxicity profiles were predicted using SwissADME and ProTox-3.0. PSN produced a significant, dose-dependent reduction in retching. The 20 mg/kg dose showed 65.60% inhibition of retches compared to control. Combination treatment with OND further enhanced inhibition (65.60%). Docking analysis revealed that PSN exhibited the strongest binding affinity toward the D2 receptor (-8.8 kcal/mol), followed by M5 (-8.1 kcal/mol) and 5-HT3A (-7.7 kcal/mol). Pharmacokinetic prediction indicated high gastrointestinal absorption and favorable drug-likeness properties. PSN demonstrates significant antiemetic activity in a validated chick emesis model, supported by moderate binding affinity toward key emesis-related receptors. While docking findings suggest possible receptor interactions, further mechanistic and translational studies are required to confirm the molecular basis of its activity.

PMID 42503454
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