北京若生智能科技有限公司
Drug Database
TO

tolterodine (Detrol LA / Detrusitol Neo / Detrusitol Retard)

✓ Approved

Pfizer, Inc. · CHRM1 · 小分子

什么是 tolterodine？

tolterodine 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：Oral (PO)。

药物档案

商品名Detrol LA, Detrusitol Neo, Detrusitol Retard
公司Pfizer, Inc.
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, Pfizer, Inc.

作用机制

分子靶点

tolterodine 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

tolterodine 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Renal and urinary disordersHypertonic bladder✓ Approved
Renal and urinary disordersUrinary incontinence✓ Approved

相关研究文献

PubMedGels (Basel, Switzerland)2026-10-26

Stimuli-Responsive Hydrogels for Oral Probiotic Delivery: Balancing Protection and Site-Specific Release.

Jung Sungwon S, Noh Sookyung S, Lee Hyeonseung H, Park Sohyeon S

Successful oral probiotic delivery requires protection of viable cells during gastrointestinal transit followed by efficient release at the target intestinal site. Stimuli-responsive hydrogels can provide both functions, although network properties that restrict acid, bile, and enzyme transport may also delay the structural changes required for release. This review discusses how crosslink density, particle geometry, the internal microenvironment, and interfacial layers shape this protection-release relationship. pH-, enzyme/microbiota-, redox-, and multi-stimuli-responsive systems are compared with emphasis on the structural changes that allow bacterial escape. Because probiotic cells are much larger than the molecular mesh of most hydrogels, release generally requires network opening through swelling, formation or enlargement of cell-scale pores or defects, erosion, fracture, de-crosslinking, or dissolution rather than ordinary molecular diffusion. Delivery performance should therefore be evaluated using release kinetics, viability of released cells, retained cells, and total viable recovery in sequential gastrointestinal models. Strain-specific testing, storage studies, and in vivo validation will also be important. The practical goal is a reproducible protection-release window that maintains cell viability without delaying release.

PMID 42929896
阅读全文 →
PubMedGels (Basel, Switzerland)2026-10-26

Temperature-Responsive Antheraea pernyi Silk Fibroin/Poly(N-isopropylacrylamide) Hydrogels for Controlled Protein Drug Delivery.

Wang Boxiang B, Xu Hangdan H, Huang Hong H, Xie Jinyang J et al.

Temperature-responsive hydrogels provide hydrated matrices for regulating protein release near physiological temperature. Building on a previously developed p(ASF-AGE-NIPAAm) hydrogel platform, this study evaluated five formulations with ASF-AGE feed contents of 10.0-57.1 wt% as protein delivery carriers. The hydrogels exhibited lower critical solution temperatures (LCSTs) of 31.8-33.0 °C and reversible swelling-deswelling transitions during cyclic temperature switching between 20 and 40 °C. Increasing the ASF-AGE content decreased the equilibrium swelling ratio from 17.3 to 10.6 g/g, while the bovine serum albumin (BSA) encapsulation efficiency varied between 73.5% and 76.8% and the drug loading capacity decreased from 452.6 to 380.2 mg/g. BSA release was evaluated in phosphate-buffered saline (PBS, pH 7.4) and depended on both temperature and formulation: the apparent cumulative release at the end of the observation period ranged from 37.6% to 54.1% at 20 °C and from 38.4% to 61.2% at 37 °C. Release was higher at 37 °C, coinciding with thermally induced network contraction, and ASF-rich formulations generally released less BSA. These Results define a composition-property-release relationship for p(ASF-AGE-NIPAAm) hydrogels and show that the ASF content can be adjusted to balance protein loading against temperature-responsive release.

PMID 42929921
阅读全文 →
PubMedGels (Basel, Switzerland)2026-10-26

Bioinspired Suction-Cup Architecture Modulates Hydration and Pomegranate-Extract Release from NVP/HEMA/CMC Hydrogels.

Chiaoprakobkij Nadda N, Chansiriwat Wasipim W, Wisanwattana Wisanee W, Waranuch Neti N et al.

Surface architecture may tune hydrogel transport without changing formulation. Flat and suction-cup N-vinylpyrrolidone/2-hydroxyethyl methacrylate/carboxymethyl cellulose (NVP/HEMA/CMC) hydrogels prepared from the same nominal formulation were compared for hydration, equilibrium water content, pomegranate-extract uptake, and 60 min release. Suction-cup hydrogels showed greater short-term swelling (38.7 ± 0.7%) than flat hydrogels (31.4 ± 0.6%), a 23.1% increase, while equilibrium water contents remained similar. Apparent extract uptake, estimated from loading-solution depletion, was 20.45 and 15.74 mg/g hydrated hydrogel for suction-cup and flat formats, respectively. After 60 min, cumulative apparent pomegranate-extract-equivalent release was 6.976 ± 0.681 and 4.208 ± 0.354 mg, respectively, representing a 65.8% increase. These values corresponded to approximately 17.6% and 15.2% of estimated initial loadings. Indirect-extract testing showed minimum viabilities of 86.24% for HaCaT cells and 71.01% for human dermal fibroblasts, exceeding the 70% ISO 10993-5 criterion. Overall, suction-cup architecture increased early swelling, estimated uptake, and cumulative release without altering formulation. Although the individual contributions of surface area, local thickness, liquid retention, and diffusion paths could not be separated, the results demonstrate that architectural modification can enhance early hydration and extract uptake and release while preserving the hydrogel formulation.

PMID 42929895
阅读全文 →
PubMedGels (Basel, Switzerland)2026-10-26

Hydrogel-Based Delivery Systems for Targeted Probiotic Release and Colonization: From Design Principles to Health Outcomes.

Yan Wenjia W, Shi Haichuan H, Wang Hao H, Xu Shanshan S et al.

Probiotics exert profound health benefits via the modulation of the intestinal microbiota. However, the efficacy of orally administered probiotics is severely constrained by a cascade of physiological barriers, including gastric acid inactivation, suboptimal intestinal release, and inadequate mucosal colonization. In response to these challenges, hydrogel-based delivery platforms have garnered considerable interest as versatile carriers capable of providing protective encapsulation, enabling spatiotemporally controlled release, and augmenting intestinal retention. This narrative review presents recent progress in the design and application of hydrogel-based oral delivery systems tailored for targeted probiotic release and effective colonization. First, the key gastrointestinal obstacles to successful probiotic delivery are delineated. Hydrogel design parameters are then critically appraised, with particular emphasis on material selection and network design. The underlying release mechanisms are subsequently examined. These encompass pH-responsive, enzyme-triggered, and inflammation-responsive modalities. Emerging colonization-enhancing strategies are discussed in detail. These include mucoadhesive hydrogel architectures and the nascent paradigm of "living hydrogels" functioning as dynamic bioreactors. The translational potential of these systems for health management is illustrated through applications in inflammatory bowel disease, colorectal cancer, and gut-brain axis modulation. Finally, key challenges in manufacturing, viability, and translational feasibility are evaluated. These include regulatory, safety, and encapsulation-related constraints. To address these, multi-responsive platforms, machine learning-assisted design, and synbiotic hydrogels are proposed. These hydrogels synergize with probiotics to target dysbiosis and repair mucosal damage for improved gastrointestinal health management.

PMID 42929947
阅读全文 →
PubMedBiosensors2026-10-26

Diene-Extended Chalcones Enable Red Fluorescence Detection of Human Serum Albumin Through FA1 Binding.

Corbin Brian B, Mason Jessica J, Houglan Paityn P, Murphey Amanda A et al.

Fluorescent molecular probes for selective and real-time detection of human serum albumin (HSA) protein in urine and blood have important applications in clinical diagnostics for various diseases. The majority of known fluorescent HSA probes give emission in the blue-green spectral region where biological autofluorescence could interfere with the detection. In this study, a series of chalcones with extended conjugation are shown to give red-emission with a large Stokes shift (λabs ≈ 430-445 nm, λem ≈ 620-640 nm), and low fluorescence in H2O. Upon addition of HSA protein, the fluorescence of these chalcones is shown to increase significantly, by as high as 30-fold. Potential site-selective binding to HSA has been examined by competitive displacement experiments using various known site-selective drugs. In conjunction with molecular docking experiments, the study further indicates that the chalcones could selectively enter the FA1 (Fatty Acid site 1) binding pocket (Drug Site III).

PMID 42930080
阅读全文 →
PubMedGels (Basel, Switzerland)2026-10-26

Cyclodextrin-Containing Tannic Acid-Lipoic Acid Hydrogels for the Loading and Reduction-Responsive Release of Nile Red.

Zhu Yuzheng Y, Kobayashi Kazuya U KU, Hatano Akihiko A, Suzuki Manabu M et al.

Hydrophobic molecules are generally difficult to incorporate into aqueous hydrogels because of their poor water solubility. In this study, a cyclodextrin (CD)-containing tannic acid-lipoic acid (TA-LA) hydrogel was developed using lipoic acid-modified β-cyclodextrin (LACD). LACD retained the host-guest recognition ability of the cyclodextrin cavity after lipoic acid modification and was successfully incorporated into the TA-LA hydrogel without interfering with gel formation. Using Nile Red (NR) as a model hydrophobic molecule, the LACD-containing hydrogel showed higher NR encapsulation efficiency and greater cyclodextrin retention than the hydrogel containing unmodified β-cyclodextrin. The LACD-containing hydrogel also exhibited reduction-responsive NR release in the presence of dithiothreitol (DTT). These results show that LACD can be incorporated into the TA-LA hydrogel while retaining the host-guest recognition ability of the cyclodextrin cavity and can be used for reduction-responsive release of NR.

PMID 42929903
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多tolterodine