Measuring nicotinic receptors with characteristics of alpha4beta2, alpha3beta2 and alpha3beta4 subtypes in rat tissues by autoradiography - PubMed (original) (raw)
Measuring nicotinic receptors with characteristics of alpha4beta2, alpha3beta2 and alpha3beta4 subtypes in rat tissues by autoradiography
David C Perry et al. J Neurochem. 2002 Aug.
Free article
Abstract
Comparison of [125I]epibatidine and 5-[125I]iodo-3-(2-azetidinylmethoxy)pyridine ([125I]A-85380) autoradiography showed evidence for nicotinic receptor heterogeneity. To identify the receptor subtypes, we performed [125I]epibatidine autoradiography in the presence of cytisine or A-85380. By comparing these results with binding data from human embryonic kidney (HEK) 293 cells stably transfected with different combinations of rat nicotinic receptor subunits, we were able to quantify three distinct populations of [125I]epibatidine binding sites with characteristics of alpha4beta2, alpha3beta2 and alpha3beta4 receptors. Although the predominant subtype in rat brain was alpha4beta2, non-alpha4beta2 binding sites were prominent in many regions. In the habenulo-peduncular system, cerebellum, substantia gelatinosa, and many medullary nuclei, alpha3beta4-like binding accounted for more than 40% of [125I]epibatidine binding, and nearly all binding in superior cervical ganglion and pineal gland. Other regions enriched in alpha3beta4-like binding included locus ceruleus, dorsal tegmentum, subiculum and anteroventral thalamic nucleus. Regions enriched in alpha3beta2-like binding included the habenulo-peduncular system, many visual system structures, certain geniculate nuclei, and dopaminergic regions. The combination of autoradiography using a broad spectrum radioligand in the presence of selective competitors, and data from binding to defined receptor subtypes in expression systems, allowed us to quantify the relative populations of these three subtypes.
Similar articles
- Subtype-selective up-regulation by chronic nicotine of high-affinity nicotinic receptors in rat brain demonstrated by receptor autoradiography.
Nguyen HN, Rasmussen BA, Perry DC. Nguyen HN, et al. J Pharmacol Exp Ther. 2003 Dec;307(3):1090-7. doi: 10.1124/jpet.103.056408. Epub 2003 Oct 14. J Pharmacol Exp Ther. 2003. PMID: 14560040 - Chronic nicotine administration does not increase nicotinic receptors labeled by [125I]epibatidine in adrenal gland, superior cervical ganglia, pineal or retina.
Dávila-García MI, Musachio JL, Kellar KJ. Dávila-García MI, et al. J Neurochem. 2003 Jun;85(5):1237-46. doi: 10.1046/j.1471-4159.2003.01774.x. J Neurochem. 2003. PMID: 12753083 - Distribution and pharmacology of alpha 6-containing nicotinic acetylcholine receptors analyzed with mutant mice.
Champtiaux N, Han ZY, Bessis A, Rossi FM, Zoli M, Marubio L, McIntosh JM, Changeux JP. Champtiaux N, et al. J Neurosci. 2002 Feb 15;22(4):1208-17. doi: 10.1523/JNEUROSCI.22-04-01208.2002. J Neurosci. 2002. PMID: 11850448 Free PMC article. - Recent progress in the development of subtype selective nicotinic acetylcholine receptor ligands.
Astles PC, Baker SR, Boot JR, Broad LM, Dell CP, Keenan M. Astles PC, et al. Curr Drug Targets CNS Neurol Disord. 2002 Aug;1(4):337-48. doi: 10.2174/1568007023339256. Curr Drug Targets CNS Neurol Disord. 2002. PMID: 12769608 Review. - Ligands for in vivo imaging of nicotinic receptor subtypes in Alzheimer brain.
Sihver W, Långström B, Nordberg A. Sihver W, et al. Acta Neurol Scand Suppl. 2000;176:27-33. doi: 10.1034/j.1600-0404.2000.00304.x. Acta Neurol Scand Suppl. 2000. PMID: 11261802 Review.
Cited by
- Distinct cholinergic circuits underlie discrete effects of reward on attention.
Runyon K, Bui T, Mazanek S, Hartle A, Marschalko K, Howe WM. Runyon K, et al. Front Mol Neurosci. 2024 Aug 29;17:1429316. doi: 10.3389/fnmol.2024.1429316. eCollection 2024. Front Mol Neurosci. 2024. PMID: 39268248 Free PMC article. Review. - Evaluation of (S)-T1 and (S)-T2 ligands targeting α3β4 nAChR as potential nicotine addiction pharmacotherapy.
Nianpanich S, Rodsiri R, Islamie R, Limpikirati P, Thanusuwannasak T, Vajragupta O, Kanasuwan A, Sarasamkan J. Nianpanich S, et al. Psychopharmacology (Berl). 2024 Aug 23. doi: 10.1007/s00213-024-06675-w. Online ahead of print. Psychopharmacology (Berl). 2024. PMID: 39177808 - Enhanced Novel Object Recognition and Spatial Memory in Rats Selectively Bred for High Nicotine Preference.
Bekci E, Gokmen RC, Kanit L, Gozen O, Balkan B, Koylu EO, Keser A. Bekci E, et al. Brain Sci. 2024 Apr 25;14(5):427. doi: 10.3390/brainsci14050427. Brain Sci. 2024. PMID: 38790406 Free PMC article. - Neurobiology of Stress-Induced Nicotine Relapse.
Wang X, Chen Y, Dong J, Ge J, Liu X, Liu J. Wang X, et al. Int J Mol Sci. 2024 Jan 25;25(3):1482. doi: 10.3390/ijms25031482. Int J Mol Sci. 2024. PMID: 38338760 Free PMC article. Review. - How can I measure brain acetylcholine levels in vivo? Advantages and caveats of commonly used approaches.
Mineur YS, Picciotto MR. Mineur YS, et al. J Neurochem. 2023 Oct;167(1):3-15. doi: 10.1111/jnc.15943. Epub 2023 Aug 24. J Neurochem. 2023. PMID: 37621094 Free PMC article. Review.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Molecular Biology Databases
Miscellaneous