Synthesis and Pharmacological Characterization of Positive Allosteric Modulators (PAMs) of the GABAB Receptor

Research in the area of GABAB receptor PAMs may lead to the development of new potentially useful drugs for the treatment of a series of diseases and syndromes, including anxiety, alcohol, nicotine and cocaine dependence, osteoarthritic pain, chronic nociceptive pain, and gastro-esophageal reflux disease. The mode of action displayed by these novel therapeutic agents suggests that they may be devoid of drawbacks that characterize full agonists, such as receptor desensitization, tolerance, muscle-relaxant effects, hypothermia, and central and gastrointestinal side effects.


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