Tag: 442.2214

The effect of brimonidine and proparacaine on metabolic enzymes: Glucose-6-phosphate dehydrogenase, 6-phosphogluconate dehydrogenase, and glutathione reductase was written by Caliskan, Buesra;Oeztuerk Kesebir, Arzu;Demir, Yeliz;Akyol Salman, Ilknur. And the article was included in Biotechnology and Applied Biochemistry in 2022.Synthetic Route of C15H16BrN5O6 This article mentions the following:

Oxidative stress is to upregulate the pentose phosphate pathway (PPP). The PPP consists of two functional branches, glucose-6-phosphate dehydrogenase (G6PD) and 6-phosphogluconaste dehydrogenase (6PGD). Glutathione reductase (GR) has a significant role in catalyzing an oxidized glutathione form into a reduced form. The purpose of this study is to investigate the effects of brimonidine and proparacaine on the activity of 6PGD, G6PD, and GR enzymes purified from human erythrocytes. Brimonidine displayed considerable inhibition profile against G6PD with IC50 value and KI constant of 29.93 ± 3.56 and 48.46 ± 0.66μM, resp. On the other hand, proparacaine had no inhibitory effect against G6PD. KI values were found to be 66.06 ± 0.78 and 811.50 ± 11.13μM for brimonidine and proparacaine, resp., for 6PGD. KI values were found to be 144.10 ± 2.01 and 1,654.00 ± 26.29μM for brimonidine and proparacaine, resp., for GR. Herein, also in silico mol. docking studies were performed between drugs and enzymes. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5Synthetic Route of C15H16BrN5O6).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Quinoxaline is isomeric with other naphthyridines including quinazoline, phthalazine and cinnoline. Quinoxaline and its analogues may also be formed by reduction of amino acids substituted 1,5-difluoro-2,4-dinitrobenzene (DFDNB),One study used 2-iodoxybenzoic acid (IBX) as a catalyst in the reaction of benzil with 1,2-diaminobenzene.Synthetic Route of C15H16BrN5O6

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Development and validation of high performance liquid chromatographic method for estimation of brimonidine tartrate as bulk drug and in ophthalmic formulation was written by Rohan, Barse;Amol, Tagalpallewar;Chandrakant, Kokare;Shrivastava, Birendra. And the article was included in International Journal of PharmTech Research in 2019.COA of Formula: C15H16BrN5O6 This article mentions the following:

Glaucoma is complex disease characterized by ocular hypertension with a progressive visual loss that could resist in blindness due to damage occurred to optic nerve. Brimonidine tartrate is commonly used drug in glaucoma therapy which is selective alpha 2 adrenergic agonist. The reverse phase high performance liquid chromatog. method was developed and validated for estimation of brimonidine tartrate in bulk drug and pharmaceutical dosage form. Better separation was achieved on Kromasil C 18 ( 250 mm X 4.6 mm i.d., 5μm particle size) column using isocratic elution program with mobile phase citric acid monohydrate buffer : water: methanol (30:50:20 volume/volume/v) and pH 3 was maintained by using triethylamine. The flow rate was 1.0 mL/min. Elute was detected at 246 nm and it effectively separated at retention time of 6 min. The developed method was successfully validated according to ICH guidelines. The method was validated for linearity, accuracy, specificity, precision and robustness. The LOD and LOQ was 1.47 and 4.47μg/mL resp. The optimized and validated method can be used for estimation of brimonidine tartrate in bulk and in ophthalmic formulation. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5COA of Formula: C15H16BrN5O6).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Condensed heterocycles of quinoxalines have become attractive targets in synthetic and medicinal chemistry due to their significant biological activities. Quinoxaline and its analogues may also be formed by reduction of amino acids substituted 1,5-difluoro-2,4-dinitrobenzene (DFDNB),One study used 2-iodoxybenzoic acid (IBX) as a catalyst in the reaction of benzil with 1,2-diaminobenzene.COA of Formula: C15H16BrN5O6

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Ocular co-delivery of timolol and brimonidine from a self-assembling peptide hydrogel for the treatment of glaucoma: in vitro and ex vivo evaluation was written by Taka, Elissavet;Karavasili, Christina;Bouropoulos, Nikolaos;Moschakis, Thomas;Andreadis, Dimitrios D.;Zacharis, Constantinos K.;Fatouros, Dimitrios G.. And the article was included in Pharmaceuticals in 2020.Computed Properties of C15H16BrN5O6 This article mentions the following:

Effective pharmacotherapy during glaucoma treatment depends on interventions that reduce intraocular pressure (IOP) and retain the intraocular pressure lowering effect for sufficient time so as to reduce dosing frequency and enhance patient adherence. Combination anti-glaucoma therapy and dosage forms that increase precorneal residence time could therefore constitute a promising therapeutic intervention. The in-situ gel forming self-assembling peptide ac-(RADA)₄-CONH₂ was evaluated as carrier for the ocular co-delivery of timolol maleate (TM) and brimonidine tartrate (BR). The hydrogel’s microstructure and mech. properties were assessed with at. force microscopy and rheol., resp. Drug diffusion from the hydrogel was evaluated in vitro in simulated tear fluid and ex vivo across porcine corneas and its effect on the treated corneas was assessed through physicochem. characterization and histol. anal. Results indicated that timolol maleate and brimonidine tartrate co-delivery affected hydrogel’s microstructure resulting in shorter nanofibers and a less rigid hydrogel matrix. Rapid and complete release of both drugs was achieved within 8 h, while a 2.8-fold and 5.4-fold higher corneal permeability was achieved for timolol maleate and brimonidine tartrate, resp. No significant alterations were induced in the structural integrity of the corneas treated with the hydrogel formulation, suggesting that self-assembling peptide hydrogels might serve as promising systems for combination anti-glaucoma therapy. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5Computed Properties of C15H16BrN5O6).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Compounds possessing quinoxaline derivatives were bestowed with a variety of significant biological properties such as antiviral, antimalarial, anticancer, DNA intercalation, DNA duplex stabilization, and many others. Quinoxalines are used as dyes, pharmaceuticals, and antibiotics such as echinomycin, levomycin exhibiting antitumoral properties. Quinoxalines establish also the basis of anthelmintics and receptor antagonists.Computed Properties of C15H16BrN5O6

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Histopathologic Analysis of Conjunctival Lymphoproliferative Disease After Topical Brimonidine Use was written by Hwang, Hyung Bin;Kim, Sun Young;Ohn, Kyoung;Kim, Su-Young. And the article was included in Journal of Ocular Pharmacology and Therapeutics in 2019.Name: 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate This article mentions the following:

Purpose: To describe of histopathol. findings of conjunctival lymphoproliferative disease (CLD) after topical brimonidine use. Methods: This is a retrospective medical record review study, including histopathol. description. We reviewed the medical records of 208 patients (415 eyes) who were diagnosed with glaucoma and who were treated with topical brimonidine only for a min. of 6 mo. Of these, the medical records of 19 patients with suspected CLD clin. features were reviewed in detail. When CLD was suspected due to administration of brimonidine, histopathol. anal. was performed by biopsy of these lesions. In addition, immunohistochem. staining was performed to analyze lymphocyte markers in some pathol. tissues. Results: Nineteen patients had suspected CLD without definite irritative symptoms. Diffuse elevated (11 patients) or follicular lesion (8 patients) of salmon pink appearance was observed in inferior palpebral conjunctiva. Among these patients, 5 patients who agreed to conjunctival biopsy had histopathol. findings of CLD such as reactive lymphoid hyperplasia (LH) (2 cases) or atypical LH (2 cases). The mean duration of brimonidine use was 29.00 ± 20.25 mo (6-76 mo). And follow-up period after discontinuation of brimonidine was 27.93 ± 11.87 mo (12-58 mo). At the last visit, complete resolution of the lesion was seen in 13 patients, and partial improvement was observed in 6 patients. Conclusions: We found 4 cases of CLD following long-term administration of brimonidine. However, large-scale addnl. studies should be performed to establish causality, to determine whether these novel side effects were caused by long-term brimonidine treatment. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5Name: 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Condensed heterocycles of quinoxalines have become attractive targets in synthetic and medicinal chemistry due to their significant biological activities. Quinoxaline and its analogues may also be formed by reduction of amino acids substituted 1,5-difluoro-2,4-dinitrobenzene (DFDNB),One study used 2-iodoxybenzoic acid (IBX) as a catalyst in the reaction of benzil with 1,2-diaminobenzene.Name: 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Changes in Ocular Biometric Parameters Over a 24-Hour Period in Ocular Hypertensive Patients was written by Fan, Shan;Gulati, Vikas;Neely, Donna G.;Andersen, Austin;Toris, Carol B.. And the article was included in Journal of Ocular Pharmacology and Therapeutics in 2022.HPLC of Formula: 70359-46-5 This article mentions the following:

Purpose: To identify 24-h changes in ocular biometric parameters in subjects with ocular hypertension (OHT), and to determine if an intraocular pressure (IOP)-lowering drug alters these parameters. Methods: Thirty volunteers with OHT (58.6 ± 9.2 years of age) were enrolled in this randomized, double-masked, placebo-controlled, crossover study. Participants self-administered 0.2% brimonidine or placebo 3 times daily for 6 wk. Measurements of seated and supine IOP, central cornea thickness (CCT), anterior chamber depth (ACD), axial length (AXL), and lens thickness were made at 8 am, 3 pm, 8 pm, and 3 am. Statistical tests were Student′s 2-tailed paired t-tests or 2-way anal. of variance (ANOVA) followed by one-way ANOVA and post hoc testing. Results: Time of day had a significant effect on IOP, CCT, ACD, and AXL. In placebo-treated eyes, CCT was greater at 3 am than at any other time (P < 0.01), ACD and AXL were greater at 3 am and 8 pm than at 3 pm (P < 0.01). Daytime IOPs were higher than nighttime (seated, P = 0.007; supine, P = 0.018), and supine IOP at night was higher than seated IOP during the day (P < 0.001). Brimonidine did not lower IOP at night nor did it alter the 24-h patterns of CCT, ACD, and AXL. Conclusions: Ocular biometric parameters exhibit characteristic 24-h fluctuations in patients with OHT. At night compared with day, the supine IOP increases, the cornea thickens, the anterior chamber deepens, and the AXL increases. Brimonidine does not alter these parameters at times when it lowers IOP (day) nor when it does not (night). Clin. Trial Registration number: NCT0132419. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5HPLC of Formula: 70359-46-5).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Quinoxaline is isomeric with other naphthyridines including quinazoline, phthalazine and cinnoline. The antitumoral properties of quinoxaline compounds have been of interest. Recently, quinoxaline and its analogs have been investigated as the catalyst’s ligands.HPLC of Formula: 70359-46-5

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Metal-Organic Frameworks as Drug Delivery Platforms for Ocular Therapeutics was written by Gandara-Loe, Jesus;Ortuno-Lizaran, Isabel;Fernandez-Sanchez, Laura;Alio, Jorge L.;Cuenca, Nicolas;Vega-Estrada, Alfredo;Silvestre-Albero, Joaquin. And the article was included in ACS Applied Materials & Interfaces in 2019.Recommanded Product: 70359-46-5 This article mentions the following:

Metal-organic frameworks (MOFs) have been evaluated as potential nanocarriers for intraocular incorporation of brimonidine tartrate to treat chronic glaucoma. Exptl. results show that UiO-67 and MIL-100 (Fe) exhibit the highest loading capacity with values up to 50-60 weight %, whereas the performance is quite limited for MOFs with narrow cavities (below 0.8 nm, for example, UiO-66 and HKUST-1). The large loading capacity in UiO-67 is accompanied by an irreversible structural amorphization in aqueous and physiol. media that promotes extended release kinetics above 12 days. Compared to the traditional drawbacks associated with the sudden release of the com. drugs (e.g., ALPHAGAN), these results anticipate UiO-67 as a potential nanocarrier for drug delivery in intraocular therapeutics. These promising results are further supported by cytotoxicity tests using retinal photoreceptor cells (661W). Toxicity of these structures (including the metal nodes and organic ligands) for retinal cells is rather low for all samples evaluated, except for HKUST-1. In the experiment, the researchers used many compounds, for example, 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5Recommanded Product: 70359-46-5).

5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine (2R,3R)-2,3-dihydroxysuccinate (cas: 70359-46-5) belongs to quinoxaline derivatives. Quinoxaline derivatives are important constituents of pharmacologically active compounds, including antibacterial, antibiotic and antineoplastic, antifungal, anti-inflammatory and analgesic drugs. Modifying quinoxaline structure it is possible to obtain a wide variety of biomedical applications, namely antimicrobial activities and chronic and metabolic diseases treatment.Recommanded Product: 70359-46-5

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider