Table of Contents

Recognition, Receptors and Regulation
Introduction
Chirality-Basic Considerations
Molecular Recognition
Biological Recognition of Chiral Molecules
Regulatory and Commercial Considerations
Chirality and Biological Response
Theoretical Aspects of Chirality
Nomenclature of Chiral Molecules
Absolute Descriptors
Relative Descriptors
Interaction of Enantiomers with Biological Systems
Biological Activity and Bioassay
Eudismic Analysis
Chirality Coefficients
Multiple Eudismic Activity Correlations
Enantiomeric Purity
Use of Chirality as a Tool in Drug Design
Chirality and Receptors
Chirality and Ion Channel Receptors
General Aspects of Ion Channel Receptors
Ligand-Gated Ion Channels
Nicotinic Acetylcholine Receptor
Serotonin (5-Hydroxytryptamine) 5-HT3-Receptor
GABAA-Receptor
Excitatory Amino Acid Receptors
Nucleotide Sensitive K+ Channels
Calcium-Modulated Potassium Channels
Voltage-Dependent Channels
Voltage-Dependent Sodium Channels
Voltage-Dependent Potassium Channels
Chloride Channels
Voltage-Dependent Calcium Channels
Chirality and G-Protein Coupled Receptors
G-Protein Coupled Receptors, Family and Mechanisms
G-Protein Receptors Responding to Adrenaline and Noradrenaline
Adrenoceptor Agonists
a-Adrenoceptor Antagonists
b-Adrenoceptor Antagonists
Combined a- and b- Adrenoceptor Antagonists
G-Protein Receptors Responding to Dopamine
Aminotetralins
G-Protein Receptors Responding to Seretonin
5-HT1a-Receptors
G-Protein Receptors Responding to Histamine
Histamine Receptor Agonists
Histamine Receptor Antagonists
G-Protein Receptors Responding to GABA
Metabotropic Glutamate Receptors
G-Protein Receptors Responding to Acetylcholine
Muscarinic Agonists
Muscarinic Antagonists
G-Protein Receptors Responding to Angiotensin
G-Protein Receptors Responding to Cholecystokinin
Tachykinin Receptors
Opioid Receptors
G-Protein Receptors Responding to Platelet Activating Factor
G-Protein Receptors Responding to Leukotrienes
Drugs Acting by Other Mechanisms
Chirality and Neurotransmitter Re-uptake Mechanisms
GABA Uptake Inhibitors
Noradrenaline Uptake Inhibitors
Serotonin (5-HT) Uptake Inhibitors
Chirality and Enzyme Inhibition
MAO Inhibitors
Agents Affecting the Arachidonic Acid Pathway
Anti-viral Agents
Nucleoside-Related Anti-Viral Agents
Non-Nucleoside-Related Anti-Viral Agents
Anti-bacterial Agents
Antifungal Agents
Chiral Aspects of the Renin-Angiotensin System
Chirality and Diuretic Agents
Chirality and the Immune System
Immunorecognition
Antiarthritic Agents
Chirality and Aspects of Drug Development
Introduction
Chirality and Distributive Processes
Absorption
Uptake into Adipose Tissue
Plasma Protein Binding
Chirality and Metabolic Processes
Metabolism of Chiral Molecules
Metabolism of Prochiral Molecules
Metabolic Chiral Inversion
Metabolic Interaction Between Enantiomers
Metabolic Interactions Between Drugs
Chirality and Pharmacogenetics
Toxicological Implications of Chirality
Thalidomide-A Case of Misinterpretation?
Toxic Liability of the Profens
Chirality and Pharmacy