2014
DOI: 10.1016/j.bcp.2014.01.029
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Abstract: This review covers history underlying the discovery of the molecular mediators of nicotine's effects in the brain and the diversity of the nicotinic acetylcholine receptor (nAChR) subtypes. Models are presented for both their structure and their function as mediators of signal transduction, with special consideration of the differences between the two main subtypes: heteromeric receptors, which are specialized for rapid electrochemical signal transduction, and homomeric α7 receptors, which have come to be impl… Show more

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Cited by 155 publications
(195 citation statements)
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References 100 publications
(143 reference statements)
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“…GAT193 was isolated as a pure cis diastereomer. 1 Molecular Modeling-A homology model for the ␣7 nAChR was constructed using the humanized AChBP structure Protein Data Bank code 3SQ9 (18) as the starting structure. The initial monomeric model was created using SwissModel (19).…”
Section: -(4-(3-bromopropyl)phenyl)-3a459b-tetrahydro-3h-cyclopenmentioning
confidence: 99%
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“…GAT193 was isolated as a pure cis diastereomer. 1 Molecular Modeling-A homology model for the ␣7 nAChR was constructed using the humanized AChBP structure Protein Data Bank code 3SQ9 (18) as the starting structure. The initial monomeric model was created using SwissModel (19).…”
Section: -(4-(3-bromopropyl)phenyl)-3a459b-tetrahydro-3h-cyclopenmentioning
confidence: 99%
“…First, ␣7 receptors can be activated by choline as well as ACh (3), removing it from the position of being strictly optimized for synaptic function and suggesting that it may respond to tissue factors, especially in the context of playing a role in the modulation of inflammation (4). Additional insights have come from the exploration of the rich pharmacology of this receptor, beginning with the identification of a variety of selective agonists and partial agonists that control the conformational dynamics of activation and desensitization in ways that are totally unlike the behavior of other nAChRs, such as those of the neuromuscular junction and autonomic ganglia that are clearly optimized for fast synaptic transmission (1,5). To a large degree, the specializations of synaptic nAChR arise from the evolution of different types of subunits that create the ACh-binding site at the interface between ␣ and non-␣-type subunits.…”
mentioning
confidence: 99%
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“…Clearly, nicotine failed for the purpose of nAChR imaging. The discovery of various nAChR subtypes during the last two decades and their investigation have revealed different distributions and functions in various brain regions [6,99] .Accordingly, different lead structures are needed to image them separately.The selection process for development of 18 F-labeled radiotracers resembles the strategy used by the pharmaceutical industry in drug discovery. Although some features of radiotracers and drugs are different, the principal need remains: specific target binding.…”
mentioning
confidence: 99%
“…Clearly, nicotine failed for the purpose of nAChR imaging. The discovery of various nAChR subtypes during the last two decades and their investigation have revealed different distributions and functions in various brain regions [6,99] .…”
mentioning
confidence: 99%