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Sigma receptors are promising drug development targets for a host of neurological, psychiatric, oncological, immunological, cardiovascular, ophthalmological, and gastrointestinal disorders. They are structurally unique proteins that are distinct from classical G protein-coupled receptors, ionotropic receptors, or receptor tyrosine kinases. With two subtypes currently known, they modulate cell survival and excitability, and subserve many critical functions in the body. Endogenous ligands for these receptors are unknown, though current clues point to neurosteroids.

This book provides a timely update on the medicinal chemistry, cell biology, and clinical implications of sigma receptors. It puts the information in a historical perspective to help new comers to the field successfully navigate the confusing early history surrounding these proteins, and provides a launching point for the development of exciting, new research.

Sigma Receptors: Chemistry, Cell Biology and Clinical Implications will be a valuable tool for pharmacologists, medicinal chemists, cell biologists, molecular biologists, clinicians, and others interested in a concise, state-of-the-art overview of the sigma receptor field with a particular view towards novel therapeutic advances.




Sigma receptors are promising drug development targets for a host of neurological, psychiatric, oncological, immunological, cardiovascular, ophthalmological, and gastrointestinal disorders. They are structurally unique proteins that are distinct from classical G protein-coupled receptors, ionotropic receptors, or receptor tyrosine kinases. With two subtypes currently known, they modulate cell survival and excitability, and subserve many critical functions in the body. Endogenous ligands for these receptors are unknown, though current clues point to neurosteroids.

This book provides a timely update on the medicinal chemistry, cell biology, and clinical implications of sigma receptors. It puts the information in a historical perspective to help new comers to the field successfully navigate the confusing early history surrounding these proteins, and provides a launching point for the development of exciting, new research.

Sigma Receptors: Chemistry, Cell Biology and Clinical Implications will be a valuable tool for pharmacologists, medicinal chemists, cell biologists, molecular biologists, clinicians, and others interested in a concise, state-of-the-art overview of the sigma receptor field with a particular view towards novel therapeutic advances.




Sigma receptors are promising drug development targets for a host of neurological, psychiatric, oncological, immunological, cardiovascular, ophthalmological, and gastrointestinal disorders. They are structurally unique proteins that are distinct from classical G protein-coupled receptors, ionotropic receptors, or receptor tyrosine kinases. With two subtypes currently known, they modulate cell survival and excitability, and subserve many critical functions in the body. Endogenous ligands for these receptors are unknown, though current clues point to neurosteroids.

This book provides a timely update on the medicinal chemistry, cell biology, and clinical implications of sigma receptors. It puts the information in a historical perspective to help new comers to the field successfully navigate the confusing early history surrounding these proteins, and provides a launching point for the development of exciting, new research.

Sigma Receptors: Chemistry, Cell Biology and Clinical Implications will be a valuable tool for pharmacologists, medicinal chemists, cell biologists, molecular biologists, clinicians, and others interested in a concise, state-of-the-art overview of the sigma receptor field with a particular view towards novel therapeutic advances.


Content:
Front Matter....Pages i-xi
? Receptors: Historical Perspective and Background....Pages 1-23
Medicinal Chemistry: New Chemical Classes and Subtype-Selective Ligands....Pages 25-44
Irreversible ? Compounds....Pages 45-69
Pharmacophore Models for ?1 Receptor Binding....Pages 71-98
Cloning of ?1 Receptor and Structural Analysis of Its Gene and Promoter Region....Pages 99-112
Site-Directed Mutagenesis....Pages 113-125
? Receptor Modulation of Ion Channels....Pages 127-149
Subcellular Localization and Interacellular Dynamics of ?1 Receptors....Pages 151-164
Intracellular Signaling and Synaptic Plasticity....Pages 165-193
Modulation of Classical Neurotransmitter Systems by ? Receptors....Pages 195-214
?2 Receptors: Regulation of Cell Growth and Implications for Cancer Diagnosis and Therapeutics....Pages 215-235
Cognitive Effects of ? Receptor Ligands....Pages 237-271
? Receptors and Scizophrenia....Pages 273-292
Potential Role of ? Ligands and Neurosteroids in Major Depression....Pages 293-314
? Receptors and Drug Abuse....Pages 315-336
?1 Receptors and the Modulation of Opiate Analgesics....Pages 337-350
? Receptors in the Immune System: Implications for Potential Therapeutic Intervention - An Overview....Pages 351-370
? Receptors and Gastrointestinal Function....Pages 371-391
Back Matter....Pages 393-414


Sigma receptors are promising drug development targets for a host of neurological, psychiatric, oncological, immunological, cardiovascular, ophthalmological, and gastrointestinal disorders. They are structurally unique proteins that are distinct from classical G protein-coupled receptors, ionotropic receptors, or receptor tyrosine kinases. With two subtypes currently known, they modulate cell survival and excitability, and subserve many critical functions in the body. Endogenous ligands for these receptors are unknown, though current clues point to neurosteroids.

This book provides a timely update on the medicinal chemistry, cell biology, and clinical implications of sigma receptors. It puts the information in a historical perspective to help new comers to the field successfully navigate the confusing early history surrounding these proteins, and provides a launching point for the development of exciting, new research.

Sigma Receptors: Chemistry, Cell Biology and Clinical Implications will be a valuable tool for pharmacologists, medicinal chemists, cell biologists, molecular biologists, clinicians, and others interested in a concise, state-of-the-art overview of the sigma receptor field with a particular view towards novel therapeutic advances.


Content:
Front Matter....Pages i-xi
? Receptors: Historical Perspective and Background....Pages 1-23
Medicinal Chemistry: New Chemical Classes and Subtype-Selective Ligands....Pages 25-44
Irreversible ? Compounds....Pages 45-69
Pharmacophore Models for ?1 Receptor Binding....Pages 71-98
Cloning of ?1 Receptor and Structural Analysis of Its Gene and Promoter Region....Pages 99-112
Site-Directed Mutagenesis....Pages 113-125
? Receptor Modulation of Ion Channels....Pages 127-149
Subcellular Localization and Interacellular Dynamics of ?1 Receptors....Pages 151-164
Intracellular Signaling and Synaptic Plasticity....Pages 165-193
Modulation of Classical Neurotransmitter Systems by ? Receptors....Pages 195-214
?2 Receptors: Regulation of Cell Growth and Implications for Cancer Diagnosis and Therapeutics....Pages 215-235
Cognitive Effects of ? Receptor Ligands....Pages 237-271
? Receptors and Scizophrenia....Pages 273-292
Potential Role of ? Ligands and Neurosteroids in Major Depression....Pages 293-314
? Receptors and Drug Abuse....Pages 315-336
?1 Receptors and the Modulation of Opiate Analgesics....Pages 337-350
? Receptors in the Immune System: Implications for Potential Therapeutic Intervention - An Overview....Pages 351-370
? Receptors and Gastrointestinal Function....Pages 371-391
Back Matter....Pages 393-414
....
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