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Book Cover
E-book
Author Fulton, Brian S.

Title Drug Discovery for the Treatment of Addiction : Medicinal Chemistry Strategies
Published Hoboken : Wiley, 2014

Copies

Description 1 online resource (360 pages)
Contents 880-01 What is drug addiction? -- Physiological basis of addiction : a chemist's interpretation -- Behavioral pharmacology and addiction -- Medication development for the treatment of drug addiction -- Medication development for narcotic addiction -- Medication development for stimulant addiction -- Medication development for depressant addiction -- Medication development for nicotine addiction -- Medication development for marijuana addiction -- Designer drugs
880-01/(S Machine generated contents note: 1. What Is Drug Addiction-- 1.1. Definitions -- 1.2. Drugs of Abuse -- 1.3. Schedule of Controlled Substances -- 1.3.1. Schedule I Controlled Substances -- 1.3.2. Schedule II Controlled Substances -- 1.3.3. Schedule III Controlled Substances -- 1.3.4. Schedule IV Controlled Substances -- 1.3.5. Schedule V Controlled Substances -- 1.4. Some Facts From 2012 NSDUH Study -- 1.5. Addictive State -- 1.5.1. Stages of Addiction -- 1.6. Theories of Addiction -- 1.7. Comorbidity -- 1.8. Genetic Aspects of Addiction -- 1.9. Approved Medications for the Treatment of Substance Abuse and Addiction -- 2. Physiological Basis of Addiction---A Chemist's Interpretation -- 2.1. Reward System -- 2.2. Neuroanatomy of the Reward System -- 2.3. Brief Review of the Central Nervous System and Addiction -- 2.3.1. Neuron Firing -- 2.4. Neurotransmitters and Their Targets -- 2.4.1. Neurotransmitters -- 2.4.2. Receptors -- 2.4.3. G-Protein-Coupled Receptors -- 2.4.4. Ion Channels -- 2.4.5. G-Protein-Activated Inwardly Rectifying K+ Channels -- 2.4.6. Transporters -- 2.5. Neurocircuitry and Neurotransmitters in Addiction -- 2.5.1. Glutaminergic System in Drug Addiction -- 2.5.2. GABAergic System in Drug Addiction -- 2.5.3. Cholinergic System in Drug Addiction -- 2.5.4. Dopaminergic System in Drug Addiction -- 2.5.5. Adrenergic System in Drug Addiction -- 2.5.6. Serotonergic System in Drug Addiction -- 2.5.7. Vesicular Monoamine Transporters -- 2.5.8. Cannabinoid System in Drug Addiction -- 2.5.9. Opioid System in Drug Addiction -- 2.6. Location of Receptors -- 2.7. Example -- 2.8. Use of Biological Markers -- 2.8.1. Alcohol Use Biomarkers -- 2.8.2. Methamphetamine Use Biomarkers -- 2.9. Memories and Addiction -- 2.10. Stress, the HPA Axis, and Addiction -- 3. Behavioral Pharmacology and Addiction -- 3.1. Animal Models of Addiction -- 3.2. Self-Administration -- 3.2.1. Chronic Intravenous Drug Self-Administration in Rats and Mice -- 3.2.2. Intravenous Self-Administration Techniques in Monkeys -- 3.3. Conditioned Place Preference -- 3.4. Tolerance -- 3.5. Extinction/Withdrawal -- 3.6. Reinstatement (Animal Models of Relapse) -- 3.7. Drug Discrimination -- 3.8. Operant Sensation Seeking Model -- 3.9. Use of Animal Behavioral Models -- Acknowledgments -- 4. Medication Development for the Treatment of Drug Addiction -- 4.1. Lead Discovery -- 4.1.1. NIDA Addiction Treatment Discovery Program -- 4.2. Pharmacological Assays -- 4.2.1. In vitro Binding Assays -- 4.2.2. In vitro Functional Activity -- 4.3. Partial Agonist Approach -- 4.4. Allosteric Modulators -- 4.4.1. Biased Ligands -- 4.5. Functional Interactions Between Receptors -- 4.5.1. CB1/μ-opioid Synergism -- 4.5.2. Bivalent Ligands and Receptor Dimers -- 4.6. Multi-Target Drugs -- 4.7. Physicochemical Properties of CNS Drugs and Blood-Brain Barrier -- 4.7.1. Receptor Occupancy -- 4.7.2. Physical Properties of CNS Drugs -- 4.8. Brain Imaging Agents -- 4.9. QT Prolongation -- 5. Medication Development for Narcotic Addiction -- 5.1. Pharmacology of Narcotic Addiction and Pain -- 5.2. Prescription Drug Addiction -- 5.3. Approved Medications -- 5.3.1. Methadone-Opioid Partial Agonist -- 5.3.2. LAAM-Opioid Agonist -- 5.3.3. Buprenorphine-Opioid Partial Agonist -- 5.3.4. Naltrexone-Opioid Antagonist -- 5.3.5. Lofexidine-Adrenergic Agonist -- 5.4. Medication Development -- 5.4.1. μ-Opioid Agonist and NET/SERT Reuptake Inhibiter: Tramadol -- 5.4.2. NMDA Antagonist: Memantine -- 5.4.3. Fatty Acid Amide Hydrolase Inhibitors -- 5.4.4. 5-HT3C Antagonist: Ondansetron -- 5.4.5. Ibogaine Alkaloids -- 6. Medication Development for Stimulant Addiction -- 6.1. Pharmacology of Cocaine Addiction -- 6.1.1. Mechanism of Action -- 6.2. Pharmacology of Methamphetamine Addiction -- 6.2.1. Mechanism of Action -- 6.3. Medication Development -- 6.3.1. Phosphodiesterase Inhibition: Ibudilast -- 6.3.2. GABA-AT Irreversible Enzyme Inhibitors: Vigabatrin (CPP-109) and CPP-115 -- 6.3.3. Disulfiram---Multimodal Enzyme Inhibitor -- 6.3.4. Dopamine-β-hydroxylase Inhibition: Nepicastat -- 6.3.5. Aldehyde Dehydrogenase 2 Inhibition: CVT-10216 -- 6.3.6. Cholinergic System M1/M4 Agonists: VU 0357017 and Xanomeline -- 6.3.7. Metabotropic Glutamate Receptors -- 6.3.8. Metabotropic Glutamate Receptor Subtype 2 Positive Allosteric Modulators (mGlu2 PAM) -- 6.3.9. Metabotropic Glutamate Receptor Subtype 5 Negative Allosteric Modulators (mGlu5, NAM) -- 6.3.10. Metabotropic Glutamate Receptor Subtype 7 Agonist (mGlu7) -- 6.3.11. Glutaminergic System Modulator: N-acetylcysteine -- 6.3.12. D3 Partial Agonist/Antagonist -- 6.3.13. D2 Partial Agonist -- 6.3.14. DAT Reuptake Inhibition -- 6.3.15. DAT Reuptake Inhibitor and σ-Receptor Antagonist: Rimcazole -- 6.3.16. σ1, Agonist: SA4503 -- 6.3.17. Mirtazapine -- 6.3.18. 5-HT2A Antagonist and 5-HT2C Agonist -- 6.3.19. 5-HT1A Partial Agonist and D3/D4 Antagonist: Buspirone -- 6.3.20. Antidepressants -- 6.3.21. Modafinil -- 6.3.22. VMAT2 Inhibition: Lobeline -- 6.3.23. DAT/NET Inhibition and nAChR Antagonist: Bupropion -- 6.3.24. GABA Uptake Inhibitor: Tiagabine -- 6.3.25. GABAB Agonist: Baclofen -- 6.3.26. Combination Therapy: Baclofen and Amantadine -- 6.3.27. GABAA Agonist and AMPA Antagonist: Topiramate -- 6.3.28. α2A Adrenergic Agonist: Clonidine -- 6.3.29. β-adrenergic Antagonist: Propranolol -- 6.3.30. Cannabinoid Antagonists: AM251 -- 6.3.31. CRF1-Antagonists: CP-154,526 -- 6.3.32. Trace Amine-Associated Receptor 1 -- 7. Medication Development for Depressant Addiction -- 7.1. Pharmacology of Alcohol Addiction -- 7.2. Approved Medications -- 7.2.1. Disulfiram---Aldehyde Dehydrogenase Inhibitor -- 7.2.2. Acamprosate---NMDA Antagonist and GABAA Agonist -- 7.2.3. Naltrexone---Opioid Antagonist -- 7.2.4. Nalmefene---Opioid Antagonist -- 7.3. Medication Development -- 7.3.1. Morphinans: Samidorphan -- 7.3.2. CB1 Antagonist: Rimonabant -- 7.3.3. GABAB Agonist: Baclofen -- 7.3.4. GABAA Agonist and AMPA Antagonist: Topiramate -- 7.3.5. CRF1 Antagonists: Pexacerfont and GSK561679 -- 7.3.6. Neurokinin 1 Receptor Antagonists: LY686071 -- 7.3.7. PPAR-γ Agonists: Pioglitazone -- 7.4. Benzodiazepines -- 7.5. Barbiturates -- 8. Medication Development for Nicotine Addiction -- 8.1. Pharmacology of Nicotine Addiction -- 8.2. Approved Medications -- 8.2.1. Varenicline-nAChR Partial Agonist -- 8.2.2. Bupropion-DAT/NET Inhibition and nAChR Antagonist -- 8.3. Medication Development -- 8.3.1. CB1 Antagonist: Rimonabant -- 8.3.2. D3 Antagonists -- 8.3.3. VMAT2: Lobeline -- 8.3.4. GABAA Agonist and AMPA Antagonist: Topiramate -- 8.3.5. PPAR-γ Agonists: Pioglitazone -- 9. Medication Development for Marijuana Addiction -- 9.1. Pharmacology of Marijuana Addiction -- 9.2. CB1 Antagonist: Rimonabant -- 9.3. Medication Development -- 9.3.1. CB1 Agonists -- 9.3.2. GABAB Agonist: Baclofen -- 9.3.3. Glutamate Modulation: Gabapentin -- 9.3.4. α2-Adrenergic Receptor Agonists: Clonidine and Lofexidine -- 9.3.5. FAAH Inhibition: PF-04457845 -- 10. Designer Drugs -- 10.1. Cathinone Drugs -- 10.1.1. Khat -- 10.1.2. Mephedrone -- 10.2. MDMA---ECSTASY -- 10.3. Cannabinoid Designer Drugs -- 10.3.1. Spice
Summary With addiction a key target for drug discovery efforts, this book fills an important and timely need for medicinal chemists who need to understand complex neuroscience issues. The author illustrates medicinal chemistry's prominent role in treating addiction and covers specific drugs of abuse including narcotics, stimulants, depressants, nicotine, and marijuana. Interprets complex neuro- biological and pharmacological information, like the drug-reward system, for medicinal chemists Emphasizes neurotransmitters and neurochemical mechanisms of addictive drugs Pulls together information on the
Bibliography Includes bibliographical references (pages 290-333) and index
Notes English
Print version record
Subject Substance abuse -- Treatment.
Neurotransmitters.
Substance-Related Disorders -- drug therapy
Drug Discovery
Neurotransmitter Agents
MEDICAL -- Pharmacology.
Neurotransmitters
Substance abuse -- Treatment
Form Electronic book
ISBN 9781118943670
1118943678
9780470614167
0470614161
9781322024325
1322024324
1118889576
9781118889572