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Phencyclidine --- Methyl aspartate --- Sigma receptors. --- Neural receptors. --- Drug abuse --- Methyl aspartate. --- Phencyclidine. --- Receptors.

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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. --- Drug receptors --- Proteins --- Neurosciences. --- Chemistry. --- Toxicology. --- Biochemistry. --- Cytology. --- Psychiatry. --- Chemistry/Food Science, general. --- Pharmacology/Toxicology. --- Biochemistry, general. --- Cell Biology. --- Medicine and psychology --- Mental health --- Psychology, Pathological --- Cell biology --- Cellular biology --- Biology --- Cells --- Cytologists --- Biological chemistry --- Chemical composition of organisms --- Organisms --- Physiological chemistry --- Chemistry --- Medical sciences --- Chemicals --- Medicine --- Pharmacology --- Poisoning --- Poisons --- Physical sciences --- Neural sciences --- Neurological sciences --- Neuroscience --- Nervous system --- Composition --- Toxicology

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Bioactive compounds and drugs are designed and screened on the basis of specific molecular targets as well as via the identification of active ingredients from traditional medicine or by serendipitous discovery. The development of novel therapeutic strategies not only requires a deep knowledge of the molecular processes and the cellular pathways involved in each pathological condition and disease, but also the specific protein targets and the effects of drug binding on protein conformation and activity. Understanding of how drugs can modify and modulate specific cellular pathways and functions will be helpful during the process of drug development and clinical trials.

Research & information: general --- Chemistry --- serum half-life extension --- fatty acid conjugation --- FcRn-mediated recycling --- serum albumin --- translocator protein (TSPO) --- CoCl2 --- mitochondrial membrane potential --- reactive oxygen species (ROS) --- cell viability --- cell death --- lung cancer cell line --- acetylcholinesterase --- amyloid beta aggregation --- neuroprotection --- molecular docking --- multi-target drug --- structure–activity relationship --- brassicasterol --- phytosterols --- HSV --- Mycobacterium tuberculosis --- HSV-1 DNA polymerase --- HSV-1 TK --- human CDK2 --- ACE --- UDP-galactopyranose mutase --- heat shock protein 70 --- Hsp70 --- piperine --- fluorescence spectroscopy --- molecular dynamics --- molecular biophysics --- GADD45β --- MKK7 --- multiple myeloma --- protein-ligand interaction --- STD-NMR --- sigma receptors --- sigma ligands --- cancer --- SIGMAR1 --- PGRMC1 --- TMEM97 --- NCI60 COMPARE analysis --- membrane --- lipid-protein interaction --- lipid signalling --- kinase regulation --- phosphatidylinositols --- molecular docking simulation --- target identification --- small-molecule derivatives of salicylanilide --- drug discovery --- drug development --- thyroid diseases --- endocrine disruptor compound --- human umbilical artery --- vascular homeostasis

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Bioactive compounds and drugs are designed and screened on the basis of specific molecular targets as well as via the identification of active ingredients from traditional medicine or by serendipitous discovery. The development of novel therapeutic strategies not only requires a deep knowledge of the molecular processes and the cellular pathways involved in each pathological condition and disease, but also the specific protein targets and the effects of drug binding on protein conformation and activity. Understanding of how drugs can modify and modulate specific cellular pathways and functions will be helpful during the process of drug development and clinical trials.

serum half-life extension --- fatty acid conjugation --- FcRn-mediated recycling --- serum albumin --- translocator protein (TSPO) --- CoCl2 --- mitochondrial membrane potential --- reactive oxygen species (ROS) --- cell viability --- cell death --- lung cancer cell line --- acetylcholinesterase --- amyloid beta aggregation --- neuroprotection --- molecular docking --- multi-target drug --- structure–activity relationship --- brassicasterol --- phytosterols --- HSV --- Mycobacterium tuberculosis --- HSV-1 DNA polymerase --- HSV-1 TK --- human CDK2 --- ACE --- UDP-galactopyranose mutase --- heat shock protein 70 --- Hsp70 --- piperine --- fluorescence spectroscopy --- molecular dynamics --- molecular biophysics --- GADD45β --- MKK7 --- multiple myeloma --- protein-ligand interaction --- STD-NMR --- sigma receptors --- sigma ligands --- cancer --- SIGMAR1 --- PGRMC1 --- TMEM97 --- NCI60 COMPARE analysis --- membrane --- lipid-protein interaction --- lipid signalling --- kinase regulation --- phosphatidylinositols --- molecular docking simulation --- target identification --- small-molecule derivatives of salicylanilide --- drug discovery --- drug development --- thyroid diseases --- endocrine disruptor compound --- human umbilical artery --- vascular homeostasis