Effects of Topically Applied Falintolol: A New Beta-Adrenergic Antagonist for Treatment of Glaucoma

Himber, Jacques; Sallee, Verney L.; Andermann, G.; Bouzoubaa, Mohamed; Leclerc, G.; Santis, Louis De

doi:10.1089/jop.1987.3.111

Cited by 14 publications

(11 citation statements)

References 16 publications

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“…This method proved to be successful in the delivery of liposome-entrapped drugs, i.e., in the intra-articular administration of hormone-based drugs totreat arthritis [ 206 ] and in the intracoronary infusion of thrombolytic enzymes to cure myocardial infarction [ 207 ]. Non-encapsulated falintolol used as a beta-blocking agent has been successfully delivered by direct application in open-angle glaucoma therapy [ 208 ]. A recent feasibility study demonstrated how topical application of metformin could help bone regeneration around dental implants in type 2 diabetic patients [ 209 ].…”

Section: Targeting Strategies and Applicationsmentioning

confidence: 99%

Targeted Delivery of Protein Drugs by Nanocarriers

2010

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Recent advances in biotechnology demonstrate that peptides and proteins are the basis of a new generation of drugs. However, the transportation of protein drugs in the body is limited by their high molecular weight, which prevents the crossing of tissue barriers, and by their short lifetime due to immuno response and enzymatic degradation. Moreover, the ability to selectively deliver drugs to target organs, tissues or cells is a major challenge in the treatment of several human diseases, including cancer. Indeed, targeted delivery can be much more efficient than systemic application, while improving bioavailability and limiting undesirable side effects. This review describes how the use of targeted nanocarriers such as nanoparticles and liposomes can improve the pharmacokinetic properties of protein drugs, thus increasing their safety and maximizing the therapeutic effect.

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Section: Targeting Strategies and Applicationsmentioning

confidence: 99%

Targeted Delivery of Protein Drugs by Nanocarriers

2010

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“…A 0.5-g sample of fumMic acid was dissolved in a minimum of EtOAc and was added to the crude base. The salt formed was induced to crystallize by scratching; two recrystallizations from EtOAc-MeOH (90:10) gave 0.84 g of 10 (0.5 fumMate), yield 15%; mp 159 ± 1 °C; NMR (CDC13) of the free base 3.95 (m, 2 ), 3.80 (m, 1 ), 2.70 (m, 2 H), 2.45 (m, 2 ), 1.45 (m, 2 ), 0.8 (m, 8 H). Anal.…”

Section: -[3-(tert -Butylamino)-2-hydroxypropyl] Dicyclopropylmentioning

confidence: 99%

“…The crude epoxide was chromatographed on silica gel with hexane-EtOAc (95:5) as eluent. The yield was 1.5 g (57%) of (R)-3: NMR (CC14) 3.80 (d, J = 5 Hz, 2 H), 2.95 (m, 1 H), 2.45 (m,…”

Section: -[3-(tert -Butylamino)-2-hydroxypropyl] Dicyclopropylmentioning

confidence: 99%

New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent .beta.-adrenergic blocking properties

Bouzoubaa¹,

Leclerc²,

Rakhit³

et al. 1985

J. Med. Chem.

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The synthesis of R-(+) and S-(-) isomers of O-[3-tert-butylamino)-2-hydroxypropyl] cyclopropyl methyl ketone oxime (falintolol) is described. The syn and anti isomers of falintolol were obtained in two different ways from cyclopropyl methyl ketoxime or from falintolol. For comparison purposes, the enantiomers of the dicyclopropyl ketone oxime derivatives were also prepared. Structure-activity relationships are described.

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“…Pharmaceutical treatment strategies such as anti-vascular endothelial growth factor (VEGF) drugs for wet-age-related macular degeneration (AMD) are becoming increasingly available. Such treatments are also becoming increasingly effective in treating glaucoma, for example, prostaglandin analogs (Tomic et al, 2013 ), beta-adrenergic receptor antagonists (Himber et al, 1987 ), alpha2-adrenergic agonists (Wheeler & Woldemussie, 2001 ), alpha agonists (Arthur & Cantor, 2011 ), carbonic anhydrase inhibitors (Gugleta, 2010 ), and physostigmine (Gburkowa & Pojda, 1965 ). Nevertheless, such approaches cannot treat conditions where the underlying cause is genetic and cannot restore lost vision.…”

Section: Introductionmentioning

confidence: 99%

Optogenetic approaches to retinal prosthesis

2014

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The concept of visual restoration via retinal prosthesis arguably started in 1992 with the discovery that some of the retinal cells were still intact in those with the retinitis pigmentosa disease. Two decades later, the first commercially available devices have the capability to allow users to identify basic shapes. Such devices are still very far from returning vision beyond the legal blindness. Thus, there is considerable continued development of electrode materials, and structures and electronic control mechanisms to increase both resolution and contrast. In parallel, the field of optogenetics—the genetic photosensitization of neural tissue holds particular promise for new approaches. Given that the eye is transparent, photosensitizing remaining neural layers of the eye and illuminating from the outside could prove to be less invasive, cheaper, and more effective than present approaches. As we move toward human trials in the coming years, this review explores the core technological and biological challenges related to the gene therapy and the high radiance optical stimulation requirement.

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Effects of Topically Applied Falintolol: A New Beta-Adrenergic Antagonist for Treatment of Glaucoma

Cited by 14 publications

References 16 publications

Targeted Delivery of Protein Drugs by Nanocarriers

Targeted Delivery of Protein Drugs by Nanocarriers

New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent .beta.-adrenergic blocking properties

Optogenetic approaches to retinal prosthesis

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