Use of L-Canavanine as a Chemotherapeutic Agent for the Treatment of Pancreatic Cancer

A pharmaceutical composition of canavanine, and a method treatment of cancer, particularly pancreatic cancer with L-canavanine is disclosed

Canavanine Analogs and Their Use as Chemotherapeutic Agents

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

Bioactive Peptide-Based Probes

A method for preparing a site-specific peptide probe, wherein the peptide is specific to a receptor, includes modifying a marker to include a tether molecule and covalently binding the tether molecule to the peptide. The present invention also provides a labeled probe, comprising a peptide specific for a receptor and a marker. The marker is modified to include a tether molecule capable of covalently binding to the peptide. The peptide is typically derived from a bacteriophage or is a synthetic analog or derivative of the peptide. The receptor will typically be found on a surface of a bacterial cell. The method and probe of the invention are suitable for a rapid assay for a bacteria in a complex mixture

Use of Lobeline Compounds in the Treatment of Central Nervous System Diseases and Pathologies

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 membranes from rat striatum. Lobeline inhibits [3H]DTBZ binding with an IC50 of 0.90 μM, consistent with its IC50 of 0.88 μM for inhibition of [3H]DA uptake into vesicles. These results suggest that the action of lobeline is similar to that of amphetamine and that it specifically interacts with DTBZ sites on VMAT2 to inhibit DA uptake into synaptic vesicles. d-amphetamine inhibits [3H]DTBZ binding to vesicle membranes with an IC50 of 39.4 μM, a concentration 20 times greater than reported for inhibition of VMAT2 function, suggesting that d-amphetamine interacts with a different site than lobeline on VMAT2 to inhibit monoamine uptake. These results suggest the use of lobeline and analogs thereof in treating individuals for diseases and pathologies of the central nervous system

Lobeline Compounds as a Treatment for Psychostimulant Abuse and Withdrawal, and for Eating Disorders

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

Enantioselective Synthesis of (+) and (–)-2-[1-(2,6-Dichlorophenoxy)-Ethyl]-1,3-Diazacyclopent-2-Ene

Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof

(11R)-13-Dimethyl­ammonio-11,13-dihydro-4,5-epoxy­costunolide semifumarate

Crystals of the title salt, C17H28NO3 +·C4H3O4 −, were obtained by reacting parthenolide with dimethyl­amine followed by conversion of the amine adduct into a water-soluble fumarate salt. Subsequent crystallization of the fumarate salt from water afforded colorless ortho­rhom­bic crystals. The amine addition is highly stereospecific yielding exclusively a single diastereomer with R-configuration at the newly formed C-11 chiral carbon. In the crystal, intermolecular O—H⋯O and N—H⋯O hydrogen bonds help to establish the packing

Use of the Naturally-Occuring Quinones Thymoquinone and Dithymoquinone as Antineoplastic and Cytotoxic Agents

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

Use of Parthenolide Derivatives as Antileukemic and Cytotoxic Agents

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Opioid-Nornicotine Codrugs Combinations for Pain Management

The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain