University of Michigan

Columbia University

The University of Texas System

University of Kentucky Research Foundation

University System of Maryland

University of Kansas

Virginia Commonwealth University

Research Triangle Institute

The Mclean Hospital Corporation

James H Woods

Roger K Sunahara

Diwahar L Narasimhan

Donald W Landry

John J Tesmer

Joanne MacDonald

Shaomeng Wang

Chang-Guo Zhan

Shi-Xian Deng

Jianyong Chen

Young Min Kwon

Victor C Yang

Remy L Brim

Emily M Jutkiewicz

Mei-Chuan Holden Ko

Tien-Yi Lee

Daquan Gao

Gregory Collins

Beth Levant

Frank Ivy Carroll

Hernan A Navarro

Milan N Stojanovic

Pauline Wanjiku Ondachi

M Imad Damaj

John J G Tesmer

Charles France

Chad R Johnson

Brian D Kangas

Milan N Stojanovich

Mark R Nance

Elin Edwald

Andrew Coop

Jack Bergman

Gail Winger

Joanne Macdonald

Victor Yang

Muscarinic antagonist are provided that are used in the treatment of depression in a subject, such as humans. The muscarinic antagonist of the invention can relieve depression without effecting cognitive functions in the treated subject.

Methods of using muscarinic antagonists in the treatment of depression

The disclosure relates to compositions and methods of preventing or treating a subject suffering from opioid toxicity or overdose. The method comprises administering to a patient in need of treatment an effective amount of methocinnamox.

Compositions and methods for treating opioid overdose and opioid abuse

Provided are compositions comprising a cocaine esterase (CocE) and a compound that thermostabilizes the CocE. Also provided are methods of thermostabilizing a cocaine esterase. Additionally provided are methods of treating a mammal undergoing a cocaine-induced condition. Methods of determining whether a compound is a thermostabilizing agent for a protein are also provided. Uses of the above-described compositions for the treatment of a cocaine-induced condition is additionally provided. Additionally provided is an isolated nucleic acid encoding a CocE polypeptide having the substitutions L169K and G173Q, and the CocE polypeptide encoded by that nucleic acid, and pharmaceutical compositions thereof. Further provided is the use of that composition for the manufacture of a medicament for the treatment of a cocaine-induced condition and for the treatment of a cocaine-induced condition.

Thermostabilization of proteins

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.

Anti-cocaine compositions and treatment

Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2'-fluoro-3&#x2032;-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.

Nicotinic receptor compounds

The present invention relates to compositions and methods for treating and preventing cocaine addiction. In particular, the present invention provides mutated cocaine esterase proteins for use in treating and preventing cocaine addiction.

Compositions and methods for altering cocaine esterase activity

Potent and selective ligands for the dopamine 3 (D) receptor are disclosed. The Dreceptor ligands have a structural formula: wherein Ris Calkyl or Ccycloalkyl; or wherein Ris substituted with one or two halogen(s) or OCalkyl.

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Potent and selective ligands for the dopamine 3 (D) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C&#x2550;O or SO, Ris Calkyl, Ris aryl, heteroaryl, aryl, &#x2014;(CH)aryl, or &#x2014;(CH)heteroaryl, and n is 0 or 1. Methods of using the Dreceptor ligands in the treatment of diseases and conditions wherein modulation of the Dreceptor provides a benefit also are disclosed. 

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Ann Arbor, MI, United States of America

James H Woods