By Brian S. Fulton

ISBN-10: 0470614161

ISBN-13: 9780470614167

ISBN-10: 1118943678

ISBN-13: 9781118943670

ISBN-10: 1322024324

ISBN-13: 9781322024325

With habit a key aim for drug discovery efforts, this e-book fills a big and well timed want for medicinal chemists who have to comprehend advanced neuroscience concerns. the writer illustrates medicinal chemistry's trendy position in treating habit and covers particular medications of abuse together with narcotics, stimulants, depressants, nicotine, and marijuana.

• Interprets complicated neuro- organic and pharmacological details, just like the drug-reward method, for medicinal chemists
• Emphasizes neurotransmitters and neurochemical mechanisms of addictive drugs
• Pulls jointly info at the many capability drug ambitions for treating addiction
• Stresses specified medicinal chemistry difficulties whilst describing pharmacology trying out tools and drug development

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Extra info for Drug Discovery for the Treatment of Addiction : Medicinal Chemistry Strategies

Sample text

Genetic material was obtained from blood samples from individuals in St. Louis, MO, and Detroit, MI, who were part of the Collaborative Genetic Study of Nicotine Dependence. The blood samples were analyzed for the presence of two SNPs that are in the CHRNA5 gene. Along with nicotine dependence, evidence of the presence of alcohol dependence, cannabis dependence, major depressive disorder, panic attack, social phobia, posttraumatic stress disorder, attention deficit hyperactivity disorder, conduct disorder, and antisocial personality disorder was examined.

38 Then, in general, we can view the GPCR as mediating the actions of a neurotransmitter, or drug, from the exterior of the cell on cellular processes within the cell. GPCRs play an intimate and a fundamental role in signal transduction. Another function of G-proteins in neurons includes depolarization and firing of an action potential. When agonist binding causes the α- and βγ-subunits of the G-protein to dissociate from the receptor, the α- and βγ-subunits can then bind to a membrane-bound ion channel causing it to open or close.

The receptor component of GPCRs is composed of seven transmembrane (TM) domains with an extracellular N-terminus and an intracellular C-terminus. When a ligand (agonist) noncovalently binds to the receptor, it causes a conformational change in the receptor that can allow a G-protein to interact with the receptor through noncovalent intermolecular bonding interactions. Upon agonist binding, guanosine triphosphate (GTP) displaces GDP from the G-protein causing the G-protein to dissociate into two different components: an α-unit bound to the GTP and a βγ-unit.

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Drug Discovery for the Treatment of Addiction : Medicinal Chemistry Strategies by Brian S. Fulton

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