Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity α4β2 subunit combination

Anderson, David J.; Malysz, John; Grønlien, Jens Halvard; El Kouhen, Rachid; Håkerud, Monika; Wetterstrand, Caroline; Briggs, Clark A.; Gopalakrishnan, Murali

doi:10.1016/j.bcp.2009.06.024

Cited by 46Nicotinic Acetylcholine Receptors StudyNeuroscience and Neuropharmacology ResearchReceptor Mechanisms and Signaling

Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity α4β2 subunit combination

Anderson, David J., Malysz, John, Grønlien, Jens Halvard, El Kouhen, Rachid, Håkerud, Monika, Wetterstrand, Caroline, Briggs, Clark A., Gopalakrishnan, Murali·2009·Biochemical Pharmacology

DOI 10.1016/j.bcp.2009.06.024

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Abstract

alpha4beta2 neuronal nicotinic receptors (nAChRs) can exist in high and low sensitivity states possibly due to distinct stoichiometries during subunit assembly: (alpha4)(2)(beta2)(3) pentamer (high sensitivity, HS) and (alpha4)(3)(beta2)(2) pentamer (low sensitivity, LS). To determine if there is a linkage between HS or LS states and receptor-mediated responses in brain, we profiled several clinically studied alpha4beta2* nAChR agonists for the displacement of radioligand binding to alpha4beta2 [(3)H]-cytisine sites in rat brain membranes, effects on stimulation of [(3)H]-dopamine release from slices of rat prefrontal cortex and striatum, and activation of HS and LS human alpha4beta2 nAChRs expressed in Xenopus laevis oocytes. Binding affinities (pK(i)) and potency (pEC(50)) values for [(3)H]-dopamine release closely correlated with a rank order: varenicline>(-)-nicotine>AZD3480>dianicline congruent with ABT-089. Further, a good correlation was observed between [(3)H]-dopamine release and HS alpha4beta2 pEC(50) values, but not between [(3)H]-dopamine release and LS alpha4beta2. The relative efficacies of the agonists ranged from full to partial agonists. Varenicline behaved as a partial agonist in stimulating [(3)H]-dopamine release and activating both HS and LS alpha4beta2 nAChRs expressed in oocytes. Conversely, ABT-089, AZD3480 and dianicline exhibited little efficacy at LS alpha4beta2 (<5%), were more effective at HS alpha4beta2 nAChRs, and in stimulating cortical and striatal [(3)H]-dopamine release >or=30%. In the presence of alpha-conotoxin MII to block alpha6beta2* nAChRs, the alpha4beta2* alpha-conotoxin-insensitive [(3)H]-dopamine release stimulated by these ligands correlates well with their interactions at HS, but not LS. In summary, this study provides support for HS alpha4beta2* nAChR involvement in neurotransmitter release.

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The effect of varenicline on α6β2* nAChR-mediated function in CNS dopaminergic systems is currently unclear.
“Although ␣6␤2* nAChRs play an important role in addiction, the effect of varenicline on ␣6␤2* nAChR-mediated function in CNS dopaminergic systems is currently unclear”
From Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum (2012) · cites this paper as Anderson et al., 2009

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Authors: Anderson, D. J., Malysz, J., Grønlien, J. H., El Kouhen, R., Håkerud, M., Wetterstrand, C., Briggs, C. A., & Gopalakrishnan, M.
Affiliations: Abbott (United States) (US)
Corresponding author: Anderson, David J.
ORCID: Malysz, John
Håkerud, Monika
Gopalakrishnan, Murali
Venue: Biochemical Pharmacology
Publisher: Elsevier BV
Published: 2009-10
Volume: 78
Issue: 7
Pages: 844-851
ISSN: 0006-2952 (ISSN-L)
DOI: 10.1016/j.bcp.2009.06.024
OpenAlex: W2092705861
Cited by: 44
References: 32
Citations by year: 2025: 1 · 2024: 2 · 2023: 1 · 2020: 2 · 2018: 2 · 2017: 1 · 2016: 4 · 2015: 1 · 2014: 5 · 2013: 3 · 2012: 11
FWCI: 2.95
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biochemical Pharmacology (publishedVersion)
PubMed (publishedVersion)
Funders: Abbott Laboratories
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: neuronal nicotinic acetylcholine receptors, alpha4beta2 nAChR, dopamine release, varenicline, nicotine, prefrontal cortex, striatum, alpha-conotoxin MII, receptor stoichiometry, neurotransmitter release, brain slices, Xenopus oocyte expression
MeSH terms: Animals, Brain, Corpus Striatum, Dopamine, Female, Humans, Ligands, Male, Oocytes, Radioligand Assay, Receptors, Nicotinic, Xenopus laevis, Prefrontal Cortex, Patch-Clamp Techniques, Nicotinic Agonists, Nicotinic Antagonists, Conotoxins, Protein Subunits, Rats, Protein Multimerization, In Vitro Techniques

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Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity α4β2 subunit combination

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