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Since the discovery some 15 years ago of benzodiazepinemodulatory sites associated with GABA A receptors, greateffort has gone into understanding their molecularpharmacology and into developing new anxiolytic drugs thatinteract selectively with them. Prominent in this researchhas beenthe discovery that ~-carbolines, a differentchemical class from benzodiazepines, also act at thesereceptors but that their effects are sometimes quitedifferent from those of the benzodiazepines.This bookdocuments the latest discoveries in the molecularbiology of the GABA A receptor and reveals howan integration of the results of research inmolecularbiology, synthetic chemistry, biochemical and behavioralpharmacology, and clinical pharmacology has paved the wayforthe development of ~-carbolines from substances inducinganxiety and convulsions to a novel therapy for anxietystates, achieving a behavioral selectivity through selectiveactions at subtypes of receptors.
List of contents
Discovery of ?-Carboline Ligands for Benzodiazepine Receptors.- ?-Carboline-3-Carboxylic Acid Ethyl Ester: A Lead for New Psychotropic Drugs.- Molecular Biology of Gamma-Aminobutyric Acid Type A/Benzodiazepine Receptors.- Immunohistochemical Mapping of Gamma-Aminobutyric Acid Type A Receptor Alpha Subunits in Rat Central Nervous System.- Abecarnil is a Full Agonist at Some and a Partial Agonist at Other Recombinant Gamma-Aminobutyric Acid Type A Receptor Subtypes.- Pharmacological Evidence for Full Agonist Activity of Abecarnil at Certain Receptors.- Abecarnil: A Novel Anxiolytic with Mixed Full Agonist/Partial Agonist Properties in Animal Models of Anxiety and Sedation.- Abecarnil Shows Reduced Tolerance Development and Dependence Potential in Comparison to Diazepam.- Behavioral Pharmacology of Abecarnil in Baboons: Reduced Dependence and Abuse Potential.- Abecarnil Used to Treat Benzodiazepine Withdrawal.- Abecarnil, A New ?-Carboline Anxiolytic: Preliminary Clinical Pharmacology.
