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Nicholas Bodor – One of the best experts on this subject based on the ideXlab platform.

  • Ocular delivery of the β-adrenergic antagonist alprenolol by sequential bioactivation of its methoxime analogue
    Journal of medicinal chemistry, 1995
    Co-Authors: Laszlo Prokai, Gábor Somogyi, Nicholas Bodor

    Abstract:

    Ocular delivery of alprenolol, a beta-adrenergic antagonist, by site-specific bioactivation of its methoxime analogue results in significant and prolonged decrease of the intraocular pressure in rabbits after topical administration. Alprenolone methoxime is stable in isotonic phosphate vehicle but undergoes enzymatic hydrolysis to the corresponding ketone in the eye. The ketone is then converted to alprenolol by a carbonyl reductase present in the iris-ciliary body. The benefit of this chemical delivery system approach includes the facile release of a potential Antiglaucoma Agent only at the site of the action; thus, unwanted systemic effects of the drug can be avoided.

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  • Improved Delivery Through Biological Membranes. LVI. Pharmacological Evaluation of Alprenoxime—A New Potential Antiglaucoma Agent
    Pharmaceutical Research, 1991
    Co-Authors: Nicholas Bodor, Alaaeldin Elkoussi

    Abstract:

    A new site-specific chemical delivery system (CDS) for alprenolol was designed and investigated as a potential novel Antiglaucoma Agent. The effect of this compound, alprenoxime (AO), on the intraocular pressure (IOP) of rabbits was evaluated after its uni- and bilateral administration. AO produced significant reduction of the IOP starting at 30 min and lasting for more than 6 hr after its topical administration. Both in rats and in rabbits the i.v. bolus injection of AO (6 mg/kg) led to insignificant transient bradycardia, while no activity was found after oral or topical administration. Alprenolol (ALP) in a similar dose produced a sustained and significant bradycardia for more than 30 min. When the beta-adrenergic blocking activity was assessed against isoprenaline-tachycardia, the same results were obtained, i.e., AO led to a transient brief activity, whereas ALP produced a significant long-lasting beta blockade. These results support the potent ocular hypotensive action and the weak systemic beta-adrenergic blocking and cardiovascular activity of AO: a significant improvement in the therapeutic index. This finding recommends alprenoxime as a potent site-specific Antiglaucoma Agent with minimal systemic side effects.

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  • improved delivery through biological membranes lvi pharmacological evaluation of alprenoxime a new potential Antiglaucoma Agent
    Pharmaceutical Research, 1991
    Co-Authors: Nicholas Bodor, Alaaeldin Elkoussi

    Abstract:

    A new site-specific chemical delivery system (CDS) for alprenolol was designed and investigated as a potential novel Antiglaucoma Agent. The effect of this compound, alprenoxime (AO), on the intraocular pressure (IOP) of rabbits was evaluated after its uni- and bilateral administration. AO produced significant reduction of the IOP starting at 30 min and lasting for more than 6 hr after its topical administration. Both in rats and in rabbits the i.v. bolus injection of AO (6 mg/kg) led to insignificant transient bradycardia, while no activity was found after oral or topical administration. Alprenolol (ALP) in a similar dose produced a sustained and significant bradycardia for more than 30 min. When the beta-adrenergic blocking activity was assessed against isoprenaline-tachycardia, the same results were obtained, i.e., AO led to a transient brief activity, whereas ALP produced a significant long-lasting beta blockade. These results support the potent ocular hypotensive action and the weak systemic beta-adrenergic blocking and cardiovascular activity of AO: a significant improvement in the therapeutic index. This finding recommends alprenoxime as a potent site-specific Antiglaucoma Agent with minimal systemic side effects.

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Alaaeldin Elkoussi – One of the best experts on this subject based on the ideXlab platform.

  • Improved Delivery Through Biological Membranes. LVI. Pharmacological Evaluation of Alprenoxime—A New Potential Antiglaucoma Agent
    Pharmaceutical Research, 1991
    Co-Authors: Nicholas Bodor, Alaaeldin Elkoussi

    Abstract:

    A new site-specific chemical delivery system (CDS) for alprenolol was designed and investigated as a potential novel Antiglaucoma Agent. The effect of this compound, alprenoxime (AO), on the intraocular pressure (IOP) of rabbits was evaluated after its uni- and bilateral administration. AO produced significant reduction of the IOP starting at 30 min and lasting for more than 6 hr after its topical administration. Both in rats and in rabbits the i.v. bolus injection of AO (6 mg/kg) led to insignificant transient bradycardia, while no activity was found after oral or topical administration. Alprenolol (ALP) in a similar dose produced a sustained and significant bradycardia for more than 30 min. When the beta-adrenergic blocking activity was assessed against isoprenaline-tachycardia, the same results were obtained, i.e., AO led to a transient brief activity, whereas ALP produced a significant long-lasting beta blockade. These results support the potent ocular hypotensive action and the weak systemic beta-adrenergic blocking and cardiovascular activity of AO: a significant improvement in the therapeutic index. This finding recommends alprenoxime as a potent site-specific Antiglaucoma Agent with minimal systemic side effects.

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  • improved delivery through biological membranes lvi pharmacological evaluation of alprenoxime a new potential Antiglaucoma Agent
    Pharmaceutical Research, 1991
    Co-Authors: Nicholas Bodor, Alaaeldin Elkoussi

    Abstract:

    A new site-specific chemical delivery system (CDS) for alprenolol was designed and investigated as a potential novel Antiglaucoma Agent. The effect of this compound, alprenoxime (AO), on the intraocular pressure (IOP) of rabbits was evaluated after its uni- and bilateral administration. AO produced significant reduction of the IOP starting at 30 min and lasting for more than 6 hr after its topical administration. Both in rats and in rabbits the i.v. bolus injection of AO (6 mg/kg) led to insignificant transient bradycardia, while no activity was found after oral or topical administration. Alprenolol (ALP) in a similar dose produced a sustained and significant bradycardia for more than 30 min. When the beta-adrenergic blocking activity was assessed against isoprenaline-tachycardia, the same results were obtained, i.e., AO led to a transient brief activity, whereas ALP produced a significant long-lasting beta blockade. These results support the potent ocular hypotensive action and the weak systemic beta-adrenergic blocking and cardiovascular activity of AO: a significant improvement in the therapeutic index. This finding recommends alprenoxime as a potent site-specific Antiglaucoma Agent with minimal systemic side effects.

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Shinsaku Yamane – One of the best experts on this subject based on the ideXlab platform.

  • Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.
    ACS Medicinal Chemistry Letters, 2016
    Co-Authors: Isamu Sugimoto, Tohru Kambe, Tomotaka Okino, Tetsuo Obitsu, Nobukazu Ohta, Taihei Nishiyama, Akihiro Kinoshita, Taku Fujimoto, Hiromu Egashira, Shinsaku Yamane

    Abstract:

    A novel series of prostaglandin analogues with a seven-membered ring scaffold was designed, synthesized, and evaluated for the functional activation of prostaglandin receptors to identify potent and subtype-selective FP and EP3 dual agonists. Starting from the prostacyclin derivative 5b, a nonselective agonist for prostaglandin receptors, replacement of the core structure with an octahydro-2H-cyclopenta[b]oxepine scaffold led to the discovery of the potent and selective FP and EP3 dual agonist 11b as a lead compound for the development of an Antiglaucoma Agent.

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  • Discovery of Novel Seven-Membered Prostacyclin Analogues
    as Potent and Selective Prostaglandin FP and EP3 Dual Agonists
    , 2016
    Co-Authors: Isamu Sugimoto, Tohru Kambe, Tomotaka Okino, Tetsuo Obitsu, Nobukazu Ohta, Taihei Nishiyama, Akihiro Kinoshita, Taku Fujimoto, Hiromu Egashira, Shinsaku Yamane

    Abstract:

    A novel
    series of prostaglandin analogues with a seven-membered
    ring scaffold was designed, synthesized, and evaluated for the functional
    activation of prostaglandin receptors to identify potent and subtype-selective
    FP and EP3 dual agonists. Starting from the prostacyclin derivative 5b, a nonselective agonist for prostaglandin receptors, replacement
    of the core structure with an octahydro-2H-cyclopenta­[b]­oxepine scaffold led to the discovery of the potent and
    selective FP and EP3 dual agonist 11b as a lead compound
    for the development of an Antiglaucoma Agent

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