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1.
Bioorg Med Chem Lett ; 21(21): 6343-7, 2011 Nov 01.
Article in English | MEDLINE | ID: mdl-21944381

ABSTRACT

A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.


Subject(s)
Steroids/pharmacology , Sulfhydryl Compounds/chemistry , Administration, Inhalation , Animals , Asthma/drug therapy , Cell Line , Drug Discovery , Lung/drug effects , Rats , Steroids/administration & dosage , Steroids/chemistry , Steroids/therapeutic use , Structure-Activity Relationship
2.
Vet Ophthalmol ; 8(6): 367-73, 2005.
Article in English | MEDLINE | ID: mdl-16359359

ABSTRACT

OBJECTIVE: To examine the angioarchitecture of the ciliary body in the West Indian manatee (Trichechus manatus), through the use of three-dimensional reconstruction. PROCEDURE: Specimens from West Indian manatee were preserved in 10% buffered formalin, embedded in paraffin, serial sectioned and stained by Masson trichrome for light microscopic three-dimensional reconstruction and evaluation. RESULTS: The network of blood vessels in the ciliary processes of the West Indian manatee is fed by the major arterial circle that lies mostly near the base of the iris. The branching arterioles give rise to a capillary-sinusoidal bed that extends internally along each process, emptying into two sets of veins, one being elevated. The elevated and nonelevated veins join posteriorly before emptying into the choroidal venous system. CONCLUSIONS: The angioarchitecture of the ciliary body of the West Indian manatee is clearly unique when compared to those previously examined in land mammals. Three-dimensional reconstruction of paraffin sections is an effective means to evaluate vascular patterns in ocular specimens, especially those unavailable for corrosion casting.


Subject(s)
Ciliary Body/anatomy & histology , Ciliary Body/blood supply , Imaging, Three-Dimensional/veterinary , Trichechus manatus/anatomy & histology , Animals , Arterioles/anatomy & histology , Arterioles/ultrastructure , Capillaries/anatomy & histology , Capillaries/ultrastructure , Ciliary Body/ultrastructure , Imaging, Three-Dimensional/methods , Microscopy, Electron/veterinary , Regional Blood Flow , Veins/anatomy & histology , Veins/ultrastructure
3.
Vet Ophthalmol ; 8(6): 375-85, 2005.
Article in English | MEDLINE | ID: mdl-16359360

ABSTRACT

OBJECTIVE: To examine the anatomy of the ciliary body in the West Indian manatee (Trichechus manatus), paying close attention to its vascularization and to compare to those of its distant relative, the African elephant (Loxodonta africana), the amphibious hippopotamus (Hippopotamus amphibius) and the aquatic short-finned pilot whale (Globicephala macrorhynchus). PROCEDURE: Specimens from each species were preserved in 10% buffered formalin, and observed stereomicroscopically before being embedded in paraffin, sectioned and stained by Masson trichrome, hematoxylin and eosin, and periodic acid-Schiff for light microscopic evaluation. RESULTS: The network of blood vessels in the ciliary processes of the West Indian manatee appear to have an intricate pattern, especially with regard to venous outflow. Those of the elephant are slightly less complex, while those of the hippopotamus and whale have different vascular patterns within the ciliary body. Musculature within the ciliary body is absent within the manatee and pilot whale. CONCLUSIONS: In general, there appears to be a direct relationship between the increased development of vasculature and the loss of musculature within the ciliary bodies of the aquatic and amphibious mammals presently studied. Specifically, the ciliary body of the West Indian manatee has a comparatively unique construction, especially with regard to its vasculature.


Subject(s)
Ciliary Body/anatomy & histology , Ciliary Body/blood supply , Mammals/anatomy & histology , Trichechus manatus/anatomy & histology , Animals , Artiodactyla/anatomy & histology , Artiodactyla/physiology , Ciliary Body/pathology , Elephants/anatomy & histology , Elephants/physiology , Immunohistochemistry/veterinary , Regional Blood Flow , Species Specificity , Trichechus manatus/physiology , Whales, Pilot/anatomy & histology , Whales, Pilot/physiology
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