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- Butyrylcholinesterase (2)
- Cocaine (2)
- Composition (2)
- Hydrolysis (2)
- Methods (2)
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- Neuronal (2)
- Nicotinic (2)
- Acetylcholine (1)
- Acetylcholine receptors (1)
- Administration (1)
- Agents (1)
- Ammonium (1)
- Anti-cocaine (1)
- Antileukemic (1)
- Bis-quaternary ammonium salts (1)
- Chemotherapeutic agents (1)
- Cytotoxic (1)
- Enantioselective synthesis (1)
- High activity (1)
- High-activity mutants (1)
- Indole compounds (1)
- Intranasal (1)
- Method (1)
- Modulating (1)
- Mutants (1)
- Opioid (1)
- Organic chemistry (1)
- Parthenolide derivatives (1)
- Radiation (1)
- Receptors (1)
Articles 1 - 9 of 9
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Anti-Cocaine Compositions And Treatment, Donald W. Landry, Joanne Macdonald, Shi-Xiang Deng, Chang-Guo Zhan, Daquan Gao, James H. Woods, Roger K. Sunahara, Diwahar L. Narasimhan, Victor Yang, Mei-Chuan Holden Ko, John J. Tesmer, Tien-Yi Lee, Young Min Kwon
Anti-Cocaine Compositions And Treatment, Donald W. Landry, Joanne Macdonald, Shi-Xiang Deng, Chang-Guo Zhan, Daquan Gao, James H. Woods, Roger K. Sunahara, Diwahar L. Narasimhan, Victor Yang, Mei-Chuan Holden Ko, John J. Tesmer, Tien-Yi Lee, Young Min Kwon
Pharmaceutical Sciences Faculty Patents
Embodiments of the invention disclosed herein generally relate to anti-cocaine therapeutics. Specifically, some embodiments of the invention relate to highly efficient, thermostable, and long-lasting cocaine esterase (CocE) mutants that can protect against the toxic and reinforcing effects of cocaine in subjects. Provided herein are mutant CocE polypeptides displaying thermostable esterase activity. Also provided are methods of treating cocaine-induced conditions in a subject in need via administration of mutant CocE as well as methods for high-throughput screening of candidate esterase polypeptides.
Indole Compounds And Their Use As Radiation Sensitizing Agents And Chemotherapeutic Agents, Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha Reddy Penthala, Michael L. Freeman, Sekhar R. Konjeti
Indole Compounds And Their Use As Radiation Sensitizing Agents And Chemotherapeutic Agents, Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha Reddy Penthala, Michael L. Freeman, Sekhar R. Konjeti
Pharmaceutical Sciences Faculty Patents
Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.
Tris-Quarternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
Tris-Quarternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
Pharmaceutical Sciences Faculty Patents
Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang
High Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis, Chang-Guo Zhan, Fang Zheng, Wenchao Yang
Pharmaceutical Sciences Faculty Patents
Butyrylcholinesterase (BChE) polypeptide variants of the presently-disclosed subject matter have enhanced catalytic efficiency for (−)-cocaine, as compared to wild-type BChE. Pharmaceutical compositions of the presently-disclosed subject matter include a BChE polypeptide variant having an enhanced catalytic efficiency for (−)-cocaine. A method of the presently-disclosed subject matter for treating a cocaine-induced condition includes administering to an individual an effective amount of a BChE polypeptide variant, as disclosed herein, to lower blood cocaine concentration.
Intranasal Opioid Compositions, Daniel Wermeling
Intranasal Opioid Compositions, Daniel Wermeling
Pharmaceutical Sciences Faculty Patents
The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.
High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai
High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai
Pharmaceutical Sciences Faculty Patents
A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …
Bis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Marharyta Pivavarchyk
Bis-Quaternary Ammonium Salts And Methods For Modulating Neuronal Nicotinic Acetylcholine Receptors, Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Marharyta Pivavarchyk
Pharmaceutical Sciences Faculty Patents
Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.
Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
Use Of Parthenolide Derivatives As Antileukemic And Cytotoxic Agents, Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
Pharmaceutical Sciences Faculty Patents
To view this abstract, please download this patent.
Enantioselective Synthesis Of (+) And (–)-2-[1-(2,6-Dichlorophenoxy)-Ethyl]-1,3-Diazacyclopent-2-Ene, Peter A. Crooks, Ashish Pramod Vartak
Enantioselective Synthesis Of (+) And (–)-2-[1-(2,6-Dichlorophenoxy)-Ethyl]-1,3-Diazacyclopent-2-Ene, Peter A. Crooks, Ashish Pramod Vartak
Pharmaceutical Sciences Faculty Patents
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.