Binodenoson (an experimental drug) and adenosine (an FDA-approved drug that is currently used by doctors) are used to increase blood flow to the heart just like when a person exercises on a treadmill. Using imaging techniques, this increased blood flow can help determine if areas of the heart are not getting enough blood and oxygen during exercise. The purpose of the study is to determine if binodenoson is as good as adenosine in determining if there are areas of the heart not getting enough oxygen when blood flow to the heart is increased.

Start Date01 Feb 2004

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with Binodenoson

100 Translational Medicine associated with Binodenoson

100 Patents (Medical) associated with Binodenoson

Literatures (Medical) associated with Binodenoson

01 Jan 2021·European Journal of Pharmaceutical SciencesQ2 · MEDICINE

Improving the solubility of an antifungal thiazolyl hydrazone derivative by cyclodextrin complexation

Q2 · MEDICINE

Article

Author: César, Isabela C ; Kronenberger, Thales ; Maltarollo, Vinícius G ; Oliveira, Renata B ; Silva, Iara R ; Gomes, Elionai C L

RN104, named 2-[2-(cyclohexylmethylene)hydrazinyl)]-4-phenylthiazole, is a thiazolyl hydrazone derivative with promising antifungal activity. A HPLC-DAD method was carried out using C18 end-capped column (250 × 4.6 mm, 5 µm) and a mobile phase composed of water and acetonitrile (15:85 v/v) at a flow rate of 1.2 mL/min, injection volume 25 μL and DAD detection at 240 nm. The method showed to be selective, linear in the range of 20 to 240 µg/mL, precise, accurate and robust.Due to the low solubility of RN104 in water, the development of inclusion complexes using different cyclodextrins (β-CD, γ-CD and 2-HP-β-CD) was investigated, as well as the interaction mode between RN104 and cyclodextrins using molecular docking followed by semi-empirical calculations. Among tested cyclodextrins, the best results were obtained with 2-HP-β-CD, which promoted an 18-fold increase in RN104's aqueous solubility.

01 Jul 2020·Journal of Chromatography BQ3 · MEDICINE

Preclinical pharmacokinetic study of a new thiazolyl hydrazone derivative with antifungal activity in mice plasma by LC-MS/MS

Q3 · MEDICINE

Article

Author: Braga, Alysson Vinícius ; Gloria, Maria Beatriz de Abreu ; César, Isabela Costa ; Silva, Iara Rinco ; Oliveira, Renata Barbosa ; Machado, Renes de Resende

RN104, named 2-[2-(cyclohexylmethylene)hydrazinyl)]-4-phenylthiazole, is a thiazolyl hydrazone derivative with promising antifungal activity. Pharmacokinetic profile of the RN104 was evaluated in mice plasma using a developed and validated bioanalytical method by LC-MS/MS. Clotrimazole was used as internal standard. The analytes were extracted by a protein precipitation procedure and separated on a C18 end-capped column and mobile phase composed of acetonitrile - 0.1% formic acid (85:15, v/v), in isocratic mode. Electrospray ionization in positive ionization mode (ESI + ) and multiple reaction monitoring (MRM) were employed using the transitions m/z 286.1 → m/z 176.1 (quantifier) and m/z 286.1 → m/z 112.2 (qualifier) for RN104 and m/z 345.2 → m/z 277.1 (quantifier) and m/z 345.2 → m/z 165.2 (qualifier) for internal standard. The method was validated and proved to be linear, accurate, precise, and selective over the range 0.625 to 40.0 ng/mL. The pharmacokinetic model that best fit the data was the bicompartmental model. The maximum plasmatic concentration was reached 20 min after administration (per os and intraperitoneal) and the highest plasma concentration of RN104 was found after per os administration at a dosage of 50 mg/kg compared to i.p. administration at 10 mg/kg.

01 Jul 2018·Future Science OA

A Phenylthiazole Derivative Demonstrates Efficacy On Treatment of the Cryptococcosis & Candidiasis in Animal Models

Article

Author: Oliveira, Renata B ; Junqueira, Juliana C ; A dos Santos, Julliana R ; Fuchs, Beth B ; Costa, Marliete C ; Mylonakis, Eleftherios ; Lima, Caroline M ; Johann, Susana ; Rosa, Carlos A ; Santos, Daniel A ; Sá, Nívea P ; Vaz, Jéssica A ; de Barros, Patrícia P

Aim: In this work we test 2-(2-(cyclohexylmethylene)hydrazinyl)-4-phenylthiazole (CHT) against Cryptococcus spp. and Candida albicans. Methods: The ability of CHT to act in biofilm and also to interfere with C. albicans adhesion was evaluated, as well as the efficiency of the CHT in cryptococcosis and candidiasis invertebrate and murine models. Results & conclusion: In the present work we verified that CHT is found to inhibit Cryptococcus and C. albicans affecting biofilm in both and inhibited adhesion of Candida to human buccal cells. When we evaluated in vivo, CHT prolonged survival of Galleria mellonella after infections with Cryptococcusgattii, Cryptococcusneoformans or C. albicans and promoted a reduction in the fungal burden to the organs in the murine models. These results demonstrate CHT therapeutic potential.

100 Deals associated with Binodenoson

External Link

KEGG	Wiki	ATC	Drug Bank
D03120	-	-	DB04853

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Coronary Artery Disease	NDA/BLA	US	Pfizer Inc.	01 Mar 2011
Cardiovascular Diseases	NDA/BLA	US	King Pharmaceuticals Research & Development LLC	-

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