Pharmacy and Pharmaceutical Sciences Commons^™

Water Soluble Amine Esters Of Testosterone For Intranasal Administration, Anwar A. Hussain

Pharmaceutical Sciences Faculty Patents

The present invention provides novel water soluble testosterone analogs. These testosterone analogs are suitable for intranasal administration to patients requiring increased plasma testosterone levels. The present invention also provides pharmaceutical compositions containing the testosterone analogs of the present invention. The present invention further provides a method of increasing plasma testosterone levels in patients in need of such treatment comprising the intranasal administration of the water-soluble testosterone analogs and pharmaceutical compositions of the present invention.

Camptothecin Analogs And Methods Of Preparation Thereof, Dennis P. Curran, Bom David, Thomas Burke

Pharmaceutical Sciences Faculty Patents

To see this abstract, please download this patent.

Morphine-6-Sulfate Analogues And Their Use For The Treatment Of Pain, Peter A. Crooks, Abdulghani A. Houdi, Santosh G. Kottayil, D. Allan Butterfield

Pharmaceutical Sciences Faculty Patents

3-O-Acetylmorphine-6-sulfate analogues are potent, centrally-acting morphine derivatives. The compounds are useful for the treatment of pain.

Return To Fertility After Extended Chemical Castration With A Gnrh Antagonist, Janusz W. Kostanski, Ge Jiang, Bhas A. Dani, Santos B. Murty, Wei Qiu, Bruce Schrier, B. C. Thanoo, Patrick P. Deluca

Pharmaceutical Sciences Faculty Publications

BACKGROUND: Antagonistic analogues of GnRH for the treatment of prostate cancer may be used clinically in persons for whom return to fertility after such treatment is important or desirable. The purpose of this study was, therefore, to evaluate the effects of a long term treatment with orntide, a GnRH antagonist, on testosterone levels and fertility in male rats.

METHODS: Two groups of male rats received either 120-day orntide microspheres (8.8 mg orntide/kg/120 days) or vehicle alone (control group). Serum orntide and testosterone levels in both groups were monitored at certain intervals for 9 months from the initiation of treatment. After …

Drug Delivery System Involving Interaction Between Protein Or Polypeptide And Hydrophobic Biodegradable Polymer, Patrick P. Deluca

Pharmaceutical Sciences Faculty Patents

A drug delivery system for controlled release of a protein or polypeptide comprising a hydrophobic biodegradable polymer and a protein or polypeptide. A physical interaction is present between the polymer and the protein or polypeptide, thus, allowing protection and controlled release of the protein or polypeptide in-vivo. The drug delivery system may be prepared by a polymer precipitation technique or a microsphere technique.

Water Soluble Derivatives Of Camptothecin/Homocamptothecin, Thomas Burke, Ayhan Demir, Cihangir Tanyeli, Ashok J. Chavan, Tie-Lin Wang, Yves Pommier

Pharmaceutical Sciences Faculty Patents

Camptothecin and homocamptothecin analogs and derivatives are provided incorporating alkylamine and polyalkylamine moieties.

Iodo-Nonoxynol-9-Derivatives And Methods For Their Use, George Digenis, Philip Fowler, Kazuya Matsumoto, Gustavo Doncel

Pharmaceutical Sciences Faculty Patents

Mono- and di-iodinated nonoxynol-9-derivatives and methods for their use are disclosed.

Use Of The Naturally-Occuring Quinones Thymoquinone And Dithymoquinone As Antineoplastic And Cytotoxic Agents, Peter A. Crooks, David R. Worthen, Omar A. Ghosheh

Pharmaceutical Sciences Faculty Patents

Nigella sativa derivatives, thymoquinone (TM) and dithymoquinone (DIM) are used in treatment of parental and multi-drug resistant human cancers.

Aluminium Toxicokinetics: An Updated Minireview, Robert A. Yokel, Patrick J. Mcnamara

Pharmaceutical Sciences Faculty Publications

This MiniReview updates and expands the MiniReview of aluminium toxicokinetics by Wilhelm et al. published by this journal in 1990. The use of ²⁶Al, analyzed by accelerator mass spectrometry, now enables determination of Al toxicokinetics under physiological conditions. There is concern about aluminium in drinking water. The common sources of aluminium for man are reviewed. Oral Al bioavailability from water appears to be about 0.3%. Food is the primary common source. Al bioavailability from food has not been adequately determined. Industrial and medicinal exposure, and perhaps antiperspirant use, can significantly increase absorbed aluminium. Inhalation bioavailability of airborne soluble Al …

The Toxicology Of Aluminum In The Brain: A Review, Robert A. Yokel

Pharmaceutical Sciences Faculty Publications

Aluminum is environmentally ubiquitous, providing human exposure. Usual human exposure is primarily dietary. The potential for significant Al absorption from the nasal cavity and direct distribution into the brain should be further investigated. Decreased renal function increases human risk of Al-induced accumulation and toxicity. Brain Al entry from blood may involve transferrin-receptor mediated endocytosis and a more rapid process transporting small molecular weight Al species. There appears to be Al efflux from the brain, probably as Al citrate. There is prolonged retention of a fraction of Al that enters the brain, suggesting the potential for accumulation with repeated exposure. Al …

Pathogen-Inducible Regulatory Element, Joseph Chappell, Catherine A. G. Cornett, Shauhui Yui

Pharmaceutical Sciences Faculty Patents

Qualitative transcriptional regulatory sequences functional in plants, plant tissue and in plant cells for inducible gene expression and quantitative transcriptional regulatory sequences for increasing the transcriptional expression of downstream genetic information in plants, plant tissue and plant cells are disclosed. Also disclosed are methods and recombinant DNA molecules for improving the disease resistance of transgenic plants, especially wherein an inducible promoter controls the expression of a protein capable of evoking the hypersensitive response in a plant.

Use Of Lobeline Compounds In The Treatment Of Central Nervous System Diseases And Pathologies, Peter A. Crooks, Linda P. Dwoskin

Pharmaceutical Sciences Faculty Patents

Lobeline and nicotine evoke [³H]overflow from rat striatal slices preloaded with [³H]dopamine ([³H]DA). The lobeline-evoked overflow is calcium-independent and not antagonized by mecamylamine, suggesting a mechanism of action other than the stimulation of nicotinic receptors. Whereas nicotine stimulates nicotinic receptors, lobeline inhibits [³H]DA uptake into synaptic vesicles and striatal synaptosomes. The results suggest that different mechanisms are responsible for the increase in striatal DA release evoked by lobeline and nicotine. [³H]-Dihydrotetrabenazine [³H]DTBZ), used routinely to probe a high-affinity binding site-on the vesicular monoamine transporter (VMAT2) binds to vesicle …

Formulations For Sustained-Release Of Topical Anesthetics And Methods Of Making And Using Same, Michael Joseph Jay, G. Thomas Kluemper, Sang Hun Kim

Pharmaceutical Sciences Faculty Patents

The present invention provides, inter alia, formulations useful to ameliorate symptoms associated with mucosal abrasions, specifically those due to dental orthodontic brackets; oral surgery; periodontal surgery or other procedures. For instance, there is a formulation comprising: 65 to 75% microcrystalline wax; 5 to 15% non-ionic polymer; 15 to 25% topical anesthetic; and 1 to 5% surfactant, wherein the ratio of non-ionic polymer to microcrystalline wax is no greater than 0.2. Preferably, for solid topical anesthetics, the particle size is less than the apertures of a 100-mesh screen. However, the topical anesthetic may also be a liquid. Formulations wherein the mixture …

Chemical Isoprenoid Synthases And Uses Thereof, Joseph Chappell, Kyoungwhan Back

Pharmaceutical Sciences Faculty Patents

Disclosed is a chimeric isoprenoid synthase polypeptide including a first domain from a first isoprenoid synthase joined to a second domain from a second, heterologous isoprenoid synthase, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced in the absence of the second domain of the second, heterologous isoprenoid synthase. Also disclosed is a chimeric isoprenoid synthase polypeptide including an asymmetrically positioned homologous domain, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced when the domain is positioned at its naturally-occurring …

Angiotensin Ii Promotes Atherosclerotic Lesions And Aneurysms In Apolipoprotein E-Deficient Mice, Alan Daugherty, Michael W. Manning, Lisa A. Cassis

Gill Heart & Vascular Institute Faculty Publications

Increased plasma concentrations of angiotension II (Ang II) have been implicated in atherogenesis. To examine this relationship directly, we infused Ang II or vehicle for 1 month via osmotic minipumps into mature apoE^–/– mice. These doses of Ang II did not alter arterial blood pressure, body weight, serum cholesterol concentrations, or distribution of lipoprotein cholesterol. However, Ang II infusions promoted an increased severity of aortic atherosclerotic lesions. These Ang II–induced lesions were predominantly lipid-laden macrophages and lymphocytes; moreover, Ang II promoted a marked increase in the number of macrophages present in the adventitial tissue underlying lesions. Unexpectedly, pronounced abdominal …

Host-Derived Signals For Inducing Isoprenoid Gene Expression And Uses Thereof, Joseph Chappell, Marcos Lusso

Pharmaceutical Sciences Faculty Patents

Disclosed is a method for preparing a composition that is capable of activating the expression of a gene involved in the synthesis of an isoprenoid, the method involving: (a) contacting a plant cell with an elicitor under conditions that allow an elicitor-induced release of a compound that activates the synthesis of an isoprenoid; and (b) recovering a composition including the compound, wherein the compound is diffusible and has a molecular weight less than or equal to 10,000 daltons. Also disclosed is a substantially pure elicitor-induced composition, the composition being capable of activating a gene involved in the synthesis of a …

Novel Function Of Phosphoinositide 3-Kinase In T Cell Ca2+ Signaling, Ao-Lin Hsu, Tsui-Ting Ching, Goutam Sen, Da-Sheng Wan, Subbarao Bondada, Kalwant S. Authi, Ching-Shih Chen

Pharmaceutical Sciences Faculty Publications

This study presents evidence that phosphoinositide (PI) 3-kinase is involved in T cell Ca²⁺ signaling via a phosphatidylinositol 3,4,5-trisphosphate PI(3,4,5)P₃-sensitive Ca²⁺entry pathway. First, exogenous PI(3,4,5)P₃ at concentrations close to its physiological levels induces Ca²⁺ influx in T cells, whereas PI(3,4)P₂, PI(4,5)P₂, and PI(3)P have no effect on [Ca²⁺]_i. This Ca²⁺ entry mechanism is cell type-specific as B cells and a number of cell lines examined do not respond to PI(3,4,5)P₃ stimulation. Second, inhibition of PI 3-kinase by wortmannin and by overexpression of the …

Transcriptional Silencing Elements And Their Binding Factors, Joseph Chappell, Jeffrey D. Newman, Shaohui Yin

Pharmaceutical Sciences Faculty Patents

The invention features an isolated gene silencing regulatory element that includes 5' TACNNTAC 3'. Vectors, transgenic plants and seeds thereof that include such a gene silencing regulatory element are also disclosed. The invention further provides methods of decreasing the transcription of a DNA sequence in a transgenic plant using the isolated gene silencing regulatory element.

Derivatives Of N-Chloro-N-Methyl Glucamine And N-Chloro-N-Methyl Glucamine Esters, Anwar A. Hussain, Bassam Tashtoush, Lewis W. Dittert

Pharmaceutical Sciences Faculty Patents

The present invention relates to N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters, and their use as agents for water disinfection and as mild oxidizing agents for the radiolabeling of oxidation-sensitive biomolecules.

Elicitin-Mediated Plant Resistance, Joseph Chappell, Shaohui Yin, Catherine Cornett

Pharmaceutical Sciences Faculty Patents

Qualitative transcriptional regulatory sequences functional in plants, plant tissue and in plant cells for inducible gene expression and quantitative transcriptional regulatory sequences for increasing the transcriptional expression of downstream genetic information in plants, plant tissue and plant cells are disclosed. Also disclosed are methods and recombinant DNA molecules for improving the disease resistance of transgenic plants, especially wherein an inducible promoter controls the expression of a protein capable of evoking the hypersensitive response in a plant.

Methods Of Treating Eye Conditions With Human Leukocyte Elastase (Hle) Inhibitory Agents, George A. Digenis, Charles Khouri

Pharmaceutical Sciences Faculty Patents

A method of reducing corneal scarring or fibroblast proliferation comprises applying to an area of a subject's eye afflicted with the condition a corneal scar-fibroblast proliferation-reducing amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect. A method of reducing neovascularization of corneal scar tissue comprises applying to an area of a subject's eye afflicted with the condition a neovascularization-inhibitory amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect.

Aluminum And Phosphorus Separation: Application To Preparation Of Target From Brain Tissue For 26Al Determination By Accelerator Mass Spectrometry, Russell D. Brauer, J. David Robertson, Pankaj Sharma, Robert A. Yokel

Pharmaceutical Sciences Faculty Publications

Acid digested brain containing 4 mg added ²⁷Al was ashed at 1000°C to prepare an Al₂O₃ target for accelerator mass spectrometry (AMS) analysis of ²⁶Al. A glass-like material usually resulted which was thought to be aluminum (Al) oxyphosphate. The separation of Al and phosphate was investigated. Al, but not phosphate, was bound by a cation exchange resin (AG 50-X8). Hydrofluoric acid eluted the Al from the resin. Removal of phosphate from acid digested brain by this method produced an amorphous material after ashing that was easier to recover from the porcelain crucible and had a …

Canavanine Analogs And Their Use As Chemotherapeutic Agents, Peter A. Crooks, Gerald A. Rosenthal

Pharmaceutical Sciences Faculty Patents

This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.

Lobeline Compounds As A Treatment For Psychostimulant Abuse And Withdrawal, And For Eating Disorders, Peter A. Crooks, Linda P. Dwoskin

Pharmaceutical Sciences Faculty Patents

Methods are disclosed that suggest the use of lobeline and analogs thereof in treating individuals for drug dependence and withdrawal and for eating disorders.

Chimeric Isoprenoid Synthases And Uses Thereof, Joseph Chappell, Kyoungwhan Back

Pharmaceutical Sciences Faculty Patents

Disclosed is a chimeric isoprenoid synthase polypeptide including a first domain from a first isoprenoid synthase joined to a second domain from a second, heterologous isoprenoid synthase, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced in the absence of the second domain of the second, heterologous isoprenoid synthase. Also disclosed is a chimeric isoprenoid synthase polypeptide including an assymetrically positioned homologous domain, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced when the domain is positioned at its naturally-occurring …

Nornicotine Enantiomers For Use As A Treatment For Dopamine Related Conditions And Disease States, Peter A. Crooks, Linda Phyliss Dwoskin, Michael Thomas Bardo

Pharmaceutical Sciences Faculty Patents

Optically active nornicotine compounds as a treatment for dopamine-related conditions and disease states. Such disease states include the treatment of myasthenia gravis, Parkinson's disease, Alzheimer's disease, schizophrenia, eating disorders, ulcers, drug addiction and as a substitute for psycho-stimulant self-administration.

N-Chloro-N-Methyl Glucamine And N-Chloro-N-Methyl Glucamine Esters As Novel Safe Agents For Water Disinfetion, Anwar A. Hussain, Bassam Tashtoush, Lewis W. Dittert

Pharmaceutical Sciences Faculty Patents

The present invention relates to N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters, and their use as agents for water disinfection and as mild oxidizing agents for the radiolabeling of oxidation-sensitive biomolecules.

An Overview Of The Methylxanthines And Their Regulation In The Horse, J Daniel Harkins, W. Allen Rees, G. D. Mundy, Scott D. Stanley, Thomas Tobin

Maxwell H. Gluck Equine Research Center Faculty Publications

Caffiene, theophylline and theobromine are naturally occurring members of the methylxanthine family;pentoxfylline, dyphylline and enprofylline are structurally related synthetic pharmaceuticals. Caffiene has predominantly central nervous system effects, theophylline, dyphylline and enprofylline have predominantly bronchodilator effects, while theobromine is associated with diuretic responses. Pentoxfylline is thought to increase red cell deformability and facillitate blood flow through capillary beds. The methylxanthines are not highly potent agents; they are typically administered in gram doses and they tend to have relatively long half-lives. They remain detectable in plasma and urine for relatively long periods. Similarly, traces of the naturally occurring members of this family …

Nicotinic Receptor Antagonists In The Treatment Of Neuropharmacological Disorders, Peter A. Crooks, Linda P. Dwoskin, Alain Ravard

Pharmaceutical Sciences Faculty Patents

Nicotine analogs that have nicotinic receptor antagonist properties. These compounds have been shown to competitively inhibit dopamine release induced by nicotine. The nicotine analog compounds are useful in the treatment of nicotine abuse, smoking cessation therapy, as an antidote for nicotine intoxication, treatment of cognitive disorders such as Alzheimer's disease and for the treatment of Parkinson's disease.

Multicompartment Hard Capsule With Control Release Properties, George Digenis, Dagmar Noskova

Pharmaceutical Sciences Faculty Patents

The present invention relates to a hard capsule made from a material such as gelatin, starch or a hydrophilic polymer. The capsule of the present invention is formulated into a delivery system which incorporates pharmacologically active components in three or more distinct compartments. When three compartments are utilized in the capsule, the outer compartment incorporates a drug and excipients into a layer which coats the outer part of the capsule. This layer represents the rapid release portion of the delivery system. The intermediate compartment comprises a powder formulation comprised of a drug and excipients which represents the intermediary speed release …