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Current therapeutic drugs act on four main types of molecular targets: enzymes, receptors, ion channelsand transporters, among which a major part (60–70%) are membrane proteins. This review discussesthe molecular structures and potential impact of membrane transporter proteins on new drug discovery. Thethree-dimensional (3D) molecular structure of a protein contains information about the active siteand...
This review will detail the medicinal chemistry involved in the design, synthesis and discovery ofselective serotonin, noradrenaline reuptake inhibitors and dual serotonin/noradrenaline reuptake inhibitors.In particular, this review will focus exclusively on series and compounds which have been disclosed withinthe medicinal chemistry literature between January 2000 and June 2008. Background information...
The dopamine transporter (DAT) has been a primary target for cocaine abuse/addiction medicationdiscovery. However predicted addiction liability and limited clinical evaluation has provided a formidablechallenge for development of these agents for human use. The unique and atypical pharmacological profileof the benztropine (BZT) class of dopamine uptake inhibitors, in preclinical models of cocaine...
The evolution of antidepressants over the past four decades has involved the replacement of drugswith a multiplicity of effects (e.g., TCAs) by those with selective actions (i.e., SSRIs). This strategywas employed to reduce the adverse effects of TCAs, largely by eliminating interactions with certain neurotransmittersor receptors. Although these more selective compounds may be better tolerated by...
Positron emission tomography (PET) visualization of brain components in vivo is a rapidlygrowing field. Molecular imaging with PET is also increasingly used in drug development, especiallyfor the determination of drug receptor interaction for CNS-active drugs. This gives the opportunityto relate clinical efficacy to per cent receptor occupancy of a drug on a certain targetedreceptor and to relate...
As the primary excitatory neurotransmitter in the mammalian CNS, l-glutamateparticipates not only in standard fast synaptic communication, but also contributes to higher order signalprocessing, as well as neuropathology. Given this variety of functional roles, interest has been growingas to how the extracellular concentrations of l-glutamate surroundingneurons are regulated by cellular transporter...
Glycine plays a ubiquitous role in many biological processes. In the central nervous systemit serves as an important neurotransmitter acting as an agonist at strychnine-sensitive glycine receptorsand as an essential co-agonist with glutamate at the NMDA receptor complex. Control of glycine concentrationsin the vicinity of these receptors is mediated by the specific glycine transporters, GlyT1 and...
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