Regulation of nicotinic receptors in rat brain following quasi‐irreversible nicotinic blockade by chlorisondamine and chronic treatment with nicotine
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Chronic administration of nicotinic agonists in vivo increases the density of brain nicotinic binding sites. It has been proposed that this up‐regulation results from agonist‐induced functional blockade of nicotinic receptors. This hypothesis was tested by examining post mortem [3 H]‐nicotine and [125 I]‐α‐bungarotoxin ([125 I]‐αBTX) binding following treatment in vivo with the quasi‐irreversible and insurmountable CNS nicotinic blocker chlorisondamine, given either alone or in combination with chronic nicotine administration. In rats that had not received chlorisondamine pretreatment, chronic nicotine administration (0.6 mg kg−1 s.c, twice daily for 12 days) increased [3 H]‐nicotine binding density (Bmax) in forebrain tissue sections by 19%, with no change in the apparent dissociation constant (KD). Chlorisondamine (10 mg kg−1, s.c), given once prior to the chronic treatment phase, neither increased [3 H]‐nicotine binding by itself, nor altered the extent of nicotine‐induced up‐regulation. Nevertheless, chlorisondamine pretreatment resulted in a persistent blockade of CNS nicotinic receptors, as demonstrated by complete block of acute locomotor responses to nicotine. In a second experiment, [3 H]‐nicotine and [125 I]‐αBTX binding was measured in tissue homogenates prepared from several brain regions. In the absence of chlorisondamine pretreatment, chronic nicotine administration (1 mg kg−1 s.c, twice daily for 12 days) increased the Bmax of [3 H]‐nicotine binding in the cerebral cortex (by 34%), striatum (by 28%), midbrain (by 16%) and hippocampus (by 36%); KD was unchanged. As before, this up‐regulation was neither mimicked nor blocked by chlorisondamine pretreatment (10 mg kg−1, s.c, given twice), despite persistent blockade of acute locomotor responses to nicotine. Chronic nicotine treatment also increased the Bmax (but not KD) of [125 I]‐αBTX binding in cerebral cortex (by 35%), hippocampus (by 46%) and midbrain (by 35%). Chlorisondamine altered neither Bmax nor KD when given alone, but significantly attenuated the nicotine‐induced up‐regulation of toxin binding sites in midbrain, with a similar trend in the other two regions. The finding that chronic receptor blockade neither mimicked nor blocked the agonist‐induced up‐regulation of [3 H]‐nicotine binding sites suggests that up‐regulation of these receptors is not determined by their functional status. In contrast, it appears that chronic nicotine‐induced up‐regulation of [125 I]‐αBTX binding sites may result from receptor activation.
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Chlorisondamine has no effect on nicotine-induced upregulation in animals.
“it is not surprising that the latter has no effect on nicotine-induced upregulation in animals (63).”
From Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery (2009) · cites this paper as [63]
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- Authors
- El‐Bizri, H., & Clarke, P. B. S.
- Affiliations
- McGill University (CA)
- Corresponding author
- Clarke, P.B.S.
- ORCID
- Clarke, P.B.S.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 1994-11
- Volume
- 113
- Issue
- 3
- Pages
- 917-925
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- PMC
- PMC1510460
- OpenAlex
- W2027945500
- Cited by
- 51
- References
- 40
- Citations by year
- 2020: 1 · 2015: 2 · 2013: 1 · 2012: 1
- FWCI
- 1.90
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Pharmacology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- eScholarship@McGill (McGill) (submittedVersion)
- Funders
- Medical Research Council Canada
- Fonds de Recherche du Québec - Santé
- Medical Research Council
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- nicotinic acetylcholine receptors, receptor up-regulation, chlorisondamine, nicotine, alpha-bungarotoxin binding, cerebral cortex, hippocampus, striatum, midbrain, forebrain, chronic nicotine administration, rats
- MeSH terms
- Animals, Binding Sites, Brain Chemistry, Bungarotoxins, Chlorisondamine, Male, Motor Activity, Nicotine, Receptors, Nicotinic, Up-Regulation, Rats, Sprague-Dawley, Rats
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