Literature DB >> 19335063

Nicotinic acetylcholine receptors: an overview on drug discovery.

Dieter D'hoedt1, Daniel Bertrand.   

Abstract

BACKGROUND: Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that participate in many physiological functions. Receptors result from the assembly of five homologous or heterologous subunits that form the ligand-binding site and an ionic pore. In vertebrates, 17 subunits have been identified, alpha (1 - 10), beta (1 - 4), gamma, delta and epsilon. Assembly of different subunit combinations allows a diversity of physiological and pharmacological properties.
OBJECTIVE: To review the putative involvement of nAChRs in several diseases.
METHODS: We discuss the expression pattern of the subunits, the pharmacological tools for distinguishing them and their role in pathogenesis. RESULTS/
CONCLUSION: Long-standing efforts in this field should soon result in the finding of new molecules that might be applicable to situations ranging from neurological diseases to immune treatments.

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Year:  2009        PMID: 19335063     DOI: 10.1517/14728220902841045

Source DB:  PubMed          Journal:  Expert Opin Ther Targets        ISSN: 1472-8222            Impact factor:   6.902


  27 in total

Review 1.  Nicotinic modulation of innate immune pathways via α7 nicotinic acetylcholine receptor.

Authors:  Wen-Yan Cui; Ming D Li
Journal:  J Neuroimmune Pharmacol       Date:  2010-04-13       Impact factor: 4.147

Review 2.  The therapeutic potential of α7 nicotinic acetylcholine receptor (α7 nAChR) agonists for the treatment of the cognitive deficits associated with schizophrenia.

Authors:  Corinne Beinat; Samuel D Banister; Marco Herrera; Vivian Law; Michael Kassiou
Journal:  CNS Drugs       Date:  2015-07       Impact factor: 5.749

3.  Novel small molecule α9α10 nicotinic receptor antagonist prevents and reverses chemotherapy-evoked neuropathic pain in rats.

Authors:  Elzbieta P Wala; Peter A Crooks; J Michael McIntosh; Joseph R Holtman
Journal:  Anesth Analg       Date:  2012-05-18       Impact factor: 5.108

4.  Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression.

Authors:  Alan P Kozikowski; J Brek Eaton; Krishna Mohan Bajjuri; Sheela K Chellappan; Yihua Chen; Sudhakar Karadi; Rong He; Barbara Caldarone; Michael Manzano; Po-Wai Yuen; Ronald J Lukas
Journal:  ChemMedChem       Date:  2009-08       Impact factor: 3.466

Review 5.  Neuronal nicotinic acetylcholine receptors as pharmacotherapeutic targets for the treatment of alcohol use disorders.

Authors:  S Chatterjee; S E Bartlett
Journal:  CNS Neurol Disord Drug Targets       Date:  2010-03       Impact factor: 4.388

6.  Key residues in the nicotinic acetylcholine receptor β2 subunit contribute to α-conotoxin LvIA binding.

Authors:  Dongting Zhangsun; Xiaopeng Zhu; Yong Wu; Yuanyan Hu; Quentin Kaas; David J Craik; J Michael McIntosh; Sulan Luo
Journal:  J Biol Chem       Date:  2015-02-20       Impact factor: 5.157

7.  Synthesis and evaluation of new radioligands [(11)C]A-833834 and [(11)C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors.

Authors:  Andrew G Horti; Hayden T Ravert; Yongjun Gao; Daniel P Holt; William H Bunnelle; Michael R Schrimpf; Tao Li; Jianguo Ji; Heather Valentine; Ursula Scheffel; Hiroto Kuwabara; Dean F Wong; Robert F Dannals
Journal:  Nucl Med Biol       Date:  2013-01-05       Impact factor: 2.408

8.  The novel small molecule α9α10 nicotinic acetylcholine receptor antagonist ZZ-204G is analgesic.

Authors:  Joseph R Holtman; Linda P Dwoskin; Cheryl Dowell; Elzbieta P Wala; Zhenfa Zhang; Peter A Crooks; J Michael McIntosh
Journal:  Eur J Pharmacol       Date:  2011-09-17       Impact factor: 4.432

9.  Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors.

Authors:  Jeppe A Olsen; Philip K Ahring; Jette S Kastrup; Michael Gajhede; Thomas Balle
Journal:  J Biol Chem       Date:  2014-06-30       Impact factor: 5.157

10.  18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET.

Authors:  Andrew G Horti; Yongjun Gao; Hiroto Kuwabara; Yuchuan Wang; Sofya Abazyan; Robert P Yasuda; Thao Tran; Yingxian Xiao; Niaz Sahibzada; Daniel P Holt; Kenneth J Kellar; Mikhail V Pletnikov; Martin G Pomper; Dean F Wong; Robert F Dannals
Journal:  J Nucl Med       Date:  2014-02-20       Impact factor: 10.057

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