ArticleActa pharmacologica Sinica2009
Rat neuronal nicotinic acetylcholine receptors containing alpha7 subunit: pharmacological properties of ligand binding and function.
Article in Acta pharmacologica Sinica, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 23 citations in OpenAlex.
- Therapeutic Targeting ofPharmacological reviews · 2021Review
- Brain PET Imaging of α7-nAChR with [18F]ASEM: Reproducibility, Occupancy, Receptor Density, and Changes in Schizophrenia.The international journal of neuropsychopharmacology · 2018Article
- PET imaging of αEuropean journal of nuclear medicine and molecular imaging · 2017Article
- Competition, Selectivity and Efficacy of Analogs of A-84543 for Nicotinic Acetylcholine Receptors with Repositioning of Pyridine Nitrogen.Neurochemical research · 2015Article
- [(125)I]Iodo-ASEM, a specific in vivo radioligand for α7-nAChR.Nuclear medicine and biology · 2015Article
- 18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014Article
- Derivatives of dibenzothiophene for positron emission tomography imaging of α7-nicotinic acetylcholine receptors.Journal of medicinal chemistry · 2013Article
- Sub-anesthetic concentrations of (R,S)-ketamine metabolites inhibit acetylcholine-evoked currents in α7 nicotinic acetylcholine receptors.European journal of pharmacology · 2013Article
- Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs.PloS one · 2013Article
- Endogenously expressed muscarinic receptors in HEK293 cells augment up-regulation of stably expressed α4β2 nicotinic receptors.The Journal of biological chemistry · 2011Article
- Regulation of glutamate release by α7 nicotinic receptors: differential role in methamphetamine-induced damage to dopaminergic and serotonergic terminals.The Journal of pharmacology and experimental therapeutics · 2011Article
- In vitro and in vivo characterization of a novel negative allosteric modulator of neuronal nAChRs.Neuropharmacology · 2010Article
- Alexa Fluor 546-ArIB[V11L;V16A] is a potent ligand for selectively labeling alpha 7 nicotinic acetylcholine receptors.Journal of neurochemistry · 2010Article
- MD-354 selectively antagonizes the antinociceptive effects of (-)nicotine in the mouse tail-flick assay.Psychopharmacology · 2010Article
- A novel fluorescent alpha-conotoxin for the study of alpha7 nicotinic acetylcholine receptors.Journal of neurochemistry · 2009Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
aimTo compare pharmacological properties of heterologously expressed homomeric alpha7 nicotinic acetylcholine receptors (alpha7 nAChRs) with those of native nAChRs containing alpha7 subunit (alpha7* nAChRs) in rat hippocampus and cerebral cortex.
methodsWe established a stably transfected HEK-293 cell line that expresses homomeric rat alpha7 nAChRs. We studies ligand binding profiles and functional properties of nAChRs expressed in this cell line and native rat alpha7* nAChRs in rat hippocampus and cerebral cortex. We used [(125)I]-alpha-bungarotoxin to compare ligand binding profiles in these cells with those in rat hippocampus and cerebral cortex. The functional properties of the alpha7 nAChRs expressed in this cell line were studied using whole-cell current recording.
resultsThe newly established cell line, KXalpha7R1, expresses homomeric alpha7 nAChRs that bind [(125)I]-alpha-bungarotoxin with a K(d) value of 0.38+/-0.06 nmol/L, similar to K(d) values of native rat alpha7* nAChRs from hippocampus (K(d)=0.28+/-0.03 nmol/L) and cerebral cortex (K(d)=0.33+/-0.05 nmol/L). Using whole-cell current recording, the homomeric alpha7 nAChRs expressed in the cells were activated by acetylcholine and (-)-nicotine with EC(50) values of 280+/-19 micromol/L and 180+/-40 micromol/L, respectively. The acetylcholine activated currents were potently blocked by two selective antagonists of alpha7 nAChRs, alpha-bungarotoxin (IC(50)=19+/-2 nmol/L) and methyllycaconitine (IC(50)=100+/-10 pmol/L). A comparative study of ligand binding profiles, using 13 nicotinic ligands, showed many similarities between the homomeric alpha7 nAChRs and native alpha7* receptors in rat brain, but it also revealed several notable differences.
conclusionThis newly established stable cell line should be very useful for studying the properties of homomeric alpha7 nAChRs and comparing these properties to native alpha7* nAChRs.
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