Chirality and Biological Activity of Drugs: 1st Edition (Hardback) book cover

Chirality and Biological Activity of Drugs

1st Edition

By Roger J. Crossley

CRC Press

208 pages

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Hardback: 9780849391408
pub: 1995-09-11
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This book brings together the theoretical, commercial, and practical aspects of chirality and biological activity of drugs and acts as a ready reference for the effects of enantiomers of drug substances.

Table of Contents

Recognition, Receptors and Regulation


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


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


G-Protein Receptors Responding to Seretonin


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


Antiarthritic Agents

Chirality and Aspects of Drug Development


Chirality and Distributive Processes


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

About the Series

New Directions in Organic & Biological Chemistry

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Subject Categories

BISAC Subject Codes/Headings:
MEDICAL / Biochemistry
SCIENCE / Chemistry / General