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The isolation and identification of 14C-sulfamethazine (4-amino-n-(4,6-dimethyl-2-pyrimidinyl)[14C]benzenesulfonamide) metabolites in the tissues and excreta of swine.
Pigs were given a single oral dose of 14C-sulfamethazine (4-amino-N(I4,6-dimethyl-2-pyrimidinyl)[14C]benzenesulfonamide), and the major 15C-labeled compounds in the urine and feces were identified as sulfamethazines and N4-acetylsulf amethazine. Expand
Delivery of SAR 1118 to the retina via ophthalmic drops and its effectiveness in a rat streptozotocin (STZ) model of diabetic retinopathy (DR).
SAR 1118 eye drops significantly reduced leukostasis and blood-retinal barrier breakdown in a dose-dependent manner and can alleviate the retinal complications associated with diabetes. Expand
Catabolism of premercapturic acid pathway metabolites of naphthalene to naphthols and methylthio-containing metabolites in rats.
The discovery of the essential role of the intestinal microflora in the formation of naphthols from naphthalene indicates the existence of a novel pathway for hydroxylation of aromatic systems and challenges the current concept of the in vivo relevance ofThe in vitro production of n Aphthalene 1,2-oxide. Expand
Single ocular injection of a sustained-release anti-VEGF delivers 6 months pharmacokinetics and efficacy in a primate laser CNV model
Proof of concept for delivery of an anti-VEGF molecule within a sustained-release system is demonstrated, showing protection in a pre-clinical primate model of wet AMD over 6 months. Expand
Topical application of 0.005% latanoprost increases episcleral venous pressure in normal dogs.
The increase in EVP in the dog with exposure to topical 0.005% latanoprost has not been observed in other species that have been studied, such as in the mouse and in humans, where the drug had no significant effect on the EVP. Expand
Comparison of ocular tissue weights (volumes) and tissue collection techniques in commonly used preclinical animal species.
Ocular tissue weights for five commonly used preclinical species are compared using two collection techniques to correlate drug levels in pre clinical species with human dosages and exposures. Expand
Bimatoprost sustained‐release intracameral implant reduces episcleral venous pressure in dogs
In normal dogs, Bimatoprost SR was associated with a transient increase in EVP followed by a sustained decrease, which was accompanied by a sustaining dilation of aqueous outflow vessels. Expand
Metabolism of the mercapturic acid of 2,4',5-trichlorobiphenyl in rats and mice.
Radioactivity extracted from the lungs of mice was shown to be present as triCB-SO2CH3 and radioactivity accumulated in the tracheo-bronchial mucosa of mice given either intracaecal or tail-vein injections of tri CB-MA. Expand
Fragmentation patterns of trimethylsilyl derivatives of dihydrodiol glucuronides produced by metabolism of naphthalene and 1-methyl-N-naphthylcarbamate.
Mass spectra from trimethylsilyl derivatives of three dihydrodiol glucuronides are reported. The aglycone moieties were characterized to be 1,2-dihydro-1,2-dihydroxynapthalene,Expand