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sildenafil citrate (HCP 1207 / Pahtension / HGP 1207)

✓ Approved

Hanmi Pharmaceutical · PDE5A · 小分子

什么是 sildenafil citrate?

sildenafil citrate 是一种小分子,由Hanmi Pharmaceutical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HCP 1207, Pahtension, HGP 1207
公司Hanmi Pharmaceutical
药物类别小分子
分子靶点PDE5A
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

sildenafil citrate 作用于 1 个分子靶点:

PDE5Aphosphodiesterase 5A (PDE5, CGB-PDE)
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

sildenafil citrate 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
Respiratory, thoracic and mediastinal disordersPulmonary hypertension✓ Approved

相关研究文献

PubMedACS applied optical materials2026-08-05

Surface Chemistry-Driven Surface-Enhanced Raman Scattering Fingerprinting of Aptamers on Silver Colloids.

Pandolfi Sara S, Venuti Elisabetta E, Locatelli Erica E, Mateos Xavier X et al.

The surface-enhanced Raman scattering (SERS) spectra of nucleic acids (NAs) often vary substantially across plasmonic substrates. However, systematic comparative studies across the most commonly employed plasmonic platforms remain limited, particularly for structurally complex NAs, such as aptamers. Herein, we investigate the direct SERS fingerprinting of a thiolated aptamer across three representative silver colloidal systems widely used in nucleic-acid SERS studies: intrinsically cationic spermine-modified nanoparticles, post-synthetically spermine-modified citrate colloids, and chloride-modified citrate colloids. The results show that, under the investigated conditions, the surface chemistry appears to primarily determine the dominant adsorption regime, modulating the balance between the backbone electrostatics and nucleobase-metal interactions. Intrinsically cationic nanoparticles preserve folding-dependent spectral differences, whereas negatively charged systems exhibit pronounced coverage-dependent spectral variability, highlighting the sensitivity of the interfacial SERS response to surface coverage and preparation history. These findings highlight that the SERS fingerprint of the aptamer in colloidal suspension largely emerges from the interplay between the structural complexity of the NA and the adsorption regime imposed by the nanoparticle surface chemistry. Therefore, different colloidal substrates can provide complementary spectroscopic information.

PMID 42553731
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PubMedFrontiers in medicine2026-08-05

Case Report: Mitochondrial insufficiency underlies cholinergic failure in post-vaccination long COVID: a candidate treatment protocol.

Goulding Tom T

An 80-year-old male with severe long COVID developed acute deterioration following COVID-19 vaccination despite ongoing cholinergic therapy (Mestinon 90 mg daily). A comprehensive mitochondrial support protocol targeting NAD+ repletion, electron transport chain function, and oxidative stress was initiated, with all components delivered in fresh-squeezed orange juice. Clinical response was dramatic within 48 h, with sustained functional recovery over 6 weeks. Challenge-rechallenge testing demonstrated rapid symptom recurrence and resolution with three key observations: missed doses, wrong component sequence, and substitution of water for orange juice. This final observation suggests citric acid may function as a rate-limiting Krebs cycle substrate, consistent with impaired endogenous citrate synthesis in severe long COVID. This case suggests that cholinergic support may require concurrent metabolic foundation including direct substrate supplementation, and some long COVID manifestations may be metabolically reversible with multi-pathway intervention. As a single self-case report, these findings generate hypotheses for systematic investigation rather than establishing treatment guidelines.

PMID 42553540
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PubMedVeterinary medicine and science2026-08-05

Dose-Dependent Effects of Clinoptilolite Supplementation on Sperm Quality and Oxidative Stress During Canine Semen Cryopreservation.

Coşkun Nurdan N, Karaca Fikret F

Cryopreservation induces oxidative stress, leading to reduced semen quality in canine semen. Clinoptilolite (CLP), a natural zeolite, has potential antioxidant properties that may improve post-thaw sperm parameters. This study aimed to evaluate the dose-dependent effects of CLP supplementation in semen extenders on sperm quality and oxidative stress in dogs. Semen was collected from four adult dogs by manual manipulation, divided into five equal aliquots, and diluted at a ratio of 1:3 (v/v) with a Tris-citrate extender containing 0% (control), 1%, 2%, 3%, or 4% CLP. Samples were cooled to 5°C within 45 min, equilibrated for 2 h in 0.25 mL straws, frozen in liquid nitrogen vapour, and stored in liquid nitrogen. Samples were thawed at 37°C for 30 s. Post-thaw sperm quality was evaluated together with oxidative stress markers, including total antioxidant status (TAS), total oxidant status (TOS), and oxidative stress index (OSI). The 2% CLP group showed the highest post-thaw sperm quality, whereas the lowest performance was observed in the 4% CLP group. Additionally, the 2% CLP group exhibited a more favourable oxidative profile, with higher TAS and lower TOS and OSI values than all other groups. CLP supplementation exerted dose-dependent effects on sperm quality and oxidative balance in canine semen cryopreservation. A 2% CLP concentration appears to be the most effective for improving post-thaw sperm quality.

PMID 42554047
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PubMedMethods (San Diego, Calif.)2026-08-04

Europium(III)-driven red photoluminescent sensor for ultra-sensitive and reliable assay of sildenafil citrate in pure form, pharmaceutical formulations and Bio-fluids.

Ali Hazim M HM, Essawy Abd El-Naby I AEI, Elnasr Tarek Ahmed Seaf TAS, Essawy Amr A AA

Lanthanide complexes, particularly Eu3+ β-diketonates, offer narrow-band, long-lived red emission ideally suited to sensitive fluorescence assays in complex media. The Eu(TTA)3(H2O)2 chelate combines efficient near-UV excitation, robust emission and labile coordination sites, making its signal highly responsive to molecular binding events. Sildenafil citrate is a widely used PDE-5 inhibitor whose misuse, counterfeiting and potential drug interactions demand reliable monitoring in pharmaceuticals and biological fluids. However, current chromatographic techniques are costly and labor-intensive, creating a pressing need for a simple, robust, low-cost, green, field-deployable optical method for sildenafil quantification. Near-UV excitation around 350 nm efficiently promotes ligand-to-metal energy transfer to the Eu3+ 5D0 level, producing line-narrowed 5D0→7F2 emission at ∼ 614 nm whose intensity is selectively quenched by sildenafil without disturbing its spectral fingerprint. The interaction between the Eu-TTA chemosensor and sildenafil involves a mixed mechanism of dynamic fluorescence deactivation and static "antenna" shelving, governed by photo-induced electron transfer and triplet-triplet energy transfer. Under optimized experimental conditions, the sensing protocol exhibits excellent linear Stern-Volmer behavior for sildenafil concentrations from 0.2 to 8.0 µg mL-1 (r ≈ 0.999), with a limit of detection of 0.036 µg mL-1 and a limit of quantification of 0.121 µg mL-1. Fluorimetric method coupled with SupelcleanTM LC-Florisil SPE cartridge with 2-propanol elution solvent was used for the selective determination of sildenafil in human serum and urine avoiding the presence of interference. Analysis of sildenafil in pharmaceutical formulations, spiked human urine and serum affords high overall accuracy and precision, with recoveries of 95.26-99.12 %, 97.5-102.4 % and 93.7-102.3 % and RSD values of 1.29-1.35 %, 1.16-2.01 and 1.21-2.71, respectively, while AGREE and BAGI metrics confirm the method's strong greenness and practical applicability. Consequently, the Eu-TTA-based fluorimetric probe provides a simple, sensitive, and low-cost analytical platform for sildenafil determination in pharmaceutical formulations and biological matrices, with satisfactory accuracy, precision, and practical applicability. Moreover, the system probing performance surpasses existing spectrophotometric methods and rivals chromatographic techniques in sensitivity while offering significant operational simplicity, high throughput, and cost efficiency, thus providing a green and clinically relevant alternative platform.

PMID 42546935
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PubMedInternational journal of pharmaceutics2026-08-04

A comparative study of the oxidative degradation of poloxamer 188, polysorbate 20 and polysorbate 80 in various buffered solutions.

Bollenbach Lukas L, Weber Johanna J, Schultz-Fademrecht Torsten T, Mäder Karsten K et al.

The importance of biologics has increased over the last few decades. Since proteins in liquid formulations tend to form protein particles in response to external stress factors, surfactants are added to prevent this. Currently, polysorbates (PSs) 20 and 80 are mainly used for this purpose. However, alternatives are being investigated, as PSs have stability issues, primarily due to oxidative or enzymatic degradation. The alternative that is discussed most frequently and already used in commercial biologics is poloxamer 188 (P188). However, this triblock copolymer, which consists of a polyoxypropylene block flanked by polyoxyethylene units, may also degrade through oxidative processes. Surprisingly, there are no direct comparative stability studies for PSs and P188. Therefore, the present study compared the oxidative degradation profiles of PS20 and PS80 with those of P188 in various relevant buffer systems. To this end, the formulations were subjected to stress in the form of 50 ppb (approximately 0.9 µM) of Fe2+ and light in the visible range, in line with their exposure during pharmaceutical production. Samples that received neither an iron spike nor light served as controls. The solutions contained 0.4 mg∙mL-1 PS20, PS80, or P188, respectively. The surfactants were formulated in either a 25 mM acetate, citrate, or histidine buffer solution (all pH 5.5) or in pure water. Significant differences were observed between these buffers, with greater effects at higher temperatures. The stability of the surfactant depended greatly on the buffer and the applied stress. All surfactants exhibited high rates of oxidative degradation when formulated in acetate buffer or pure water. PSs demonstrated the highest overall stability in citrate buffer, while P188 remained most stable in histidine, as well as in citrate buffer. However, both PSs exhibited instability in the presence of iron and light in histidine buffer, a phenomenon not observed in P188.

PMID 42546993
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PubMedMolecular biology reports2026-08-04

Downregulation of circulating miR-22 and elevation of serum ATP-citrate lyase in colorectal cancer: a proof-of-concept study.

Sahraei Danalou Nazila N, Dikmen Kursat K, Konac Ece E, Canbolat Orhan O et al.

Colorectal cancer (CRC) involves metabolic reprogramming alongside genetic alteration. ATP-citrate lyase (ACLY), the rate-limiting enzyme of de novo lipogenesis, is a validated target of microRNA-22 (miR-22) in tumor tissue. We asked whether both are dysregulated in the circulation of patients with CRC and whether they carry diagnostic value. Serum ACLY (ELISA) and circulating miR-22 (RT-qPCR, normalized to U6) were measured in 32 patients with histopathologically confirmed CRC and 31 healthy controls; metabolic activity was assessed by PET/CT SUVmax. Analyses used SPSS and REST 2009. miR-22 was downregulated in patients (relative expression 0.175; p < 0.001) and serum ACLY was elevated (p = 0.009). Across the whole cohort the two markers were inversely correlated (ρ = -0.362; p = 0.004), but not within the patient group (ρ = -0.128; p = 0.485) or within controls (ρ = -0.180; p = 0.333), indicating that it reflects their opposite direction of change between groups. Serum ACLY was higher in patients with radiologically active tumor involvement on PET/CT (p = 0.047). The ACLY/miR-22 ratio separated patients from controls with an AUC of 0.984 (p < 0.001), exceeding serum ACLY alone (AUC = 0.691). In this single-center, proof-of-concept study, circulating miR-22 and serum ACLY were dysregulated in opposite directions in colorectal cancer, and their ratio discriminated patients from controls (AUC > 0.98). These estimates were obtained in a single-center discovery cohort without an independent validation set and require external validation before any diagnostic use. The data do not demonstrate a direct regulatory interaction between the two markers in the circulation, and require validation in larger, prospective cohorts.

PMID 42550354
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