Rat thalamic α 4β 2 neuronal nicotinic acetylcholine receptor occupancy assay using LC-MS/MS

Journal of Pharmacological and Toxicological Methods

Volumn 65, Issue 3, 2012, Pages 136-141

  Nirogi, Ramakrishna ^a   Kandikere, Vishwottam ^a   Bhyrapuneni, Gopinadh ^a   Saralaya, Ramanatha ^a   Muddana, Nageswararao ^a   Ajjala, Devender Reddy ^a  

^a SUVEN LIFE SCIENCES LTD   (India)

Author keywords

4 2; In vivo receptor occupancy; LC MS MS; Neuronal nicotinic acetylcholine receptor; Non radiolabeled ZW 104

Indexed keywords

A 366833; ATROPINE; CYTISINE; ISPRONICLINE; NICOTINIC AGENT; NICOTINIC RECEPTOR ALPHA4BETA2; POZANICLINE; TRACER; UNCLASSIFIED DRUG; ZW 104;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BABOON; BINDING AFFINITY; BRAIN LEVEL; CEREBELLUM; CONTROLLED STUDY; CORPUS STRIATUM; FRONTAL CORTEX; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIPPOCAMPUS; IN VIVO STUDY; LIMIT OF QUANTITATION; MALE; MOUSE; NONHUMAN; PROCESS OPTIMIZATION; PROTEIN BLOOD LEVEL; PROTEIN DETERMINATION; PROTEIN LOCALIZATION; RAT; RECEPTOR OCCUPANCY; TANDEM MASS SPECTROMETRY; THALAMUS; VALIDATION PROCESS;

ANIMALS; ATROPINE; BIOLOGICAL ASSAY; BRAIN; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DRUG DISCOVERY; LIGANDS; MALE; NICOTINE; RATS; RATS, WISTAR; RECEPTORS, NICOTINIC; TANDEM MASS SPECTROMETRY; TISSUE DISTRIBUTION;

ANIMALIA; MUS; PAPIO; RATTUS;

EID: 84861483499     PISSN: 10568719     EISSN: 1873488X     Source Type: Journal    
DOI: 10.1016/j.vascn.2012.04.007     Document Type: Article

References (33)

1. Albuquerque E.X., Pereira E.F., Alkondon M., Rogers S.W. Mammalian nicotinic acetylcholine receptors: From structure to function. Physiological Reviews 2009, 89:73-120.
2. Barth V.N., Chernet E., Martin L.J., Need A.B., Rash K.S., Morin M., et al. Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radio labeled or nonlabeled raclopride tracer. Life Sciences 2006, 78:3007-3012.
3. 18F-fluoro-A-85380 in healthy volunteers. Journal of Nuclear Medicine 2003, 44:596-601.
4. Buccafusco J.J. Neuronal nicotinic receptor subtypes: Defining therapeutic targets. Molecular Interventions 2004, 4:285-295.
5. Cassels B.K., Bermúdez I., Dajas F., Abin-Carriquiry J.A., Wonnacott S. From ligand design to therapeutic efficacy: The challenge for nicotinic receptor research. Drug Discovery Today 2005, 10:1657-1665.
6. Chen D.N., Patrick J.W. The α-bungarotoxin-binding nicotinic acetylcholine receptor from rat brain contains only the α7 subunit. Journal of Biological Chemistry 1997, 272:24024-24029.
7. Chernet E., Martin L.J., Li D., Need A.B., Barth V.N., Rash K.S., et al. Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: Dopamine D2, serotonin 2A and NK-1 receptors as examples. Life Sciences 2005, 78:340-346.
8. 18F]Fluoro-A-85380, a new PET tracer for the nicotinic acetylcholine receptor: Studies in the human brain and in vivo demonstration of specific binding in white matter. Synapse 2004, 53:184-189.
9. 123I]-I-A-85380 SPECT. Journal of Nuclear Medicine 2000, 41:1552-1560.
10. Gotti C., Clementi F. Neuronal nicotinic receptors: From structure to pathology. Progress in Neurobiology 2004, 74:363-396.
11. Holladay M.W., Wasicak J.T., Lin N.H., He Y., Ryther K.B., Bannon A.W., et al. Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. Journal of Medicinal Chemistry 1998, 41:407-412.
12. 18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors. Nuclear Medicine and Biology 1998, 25:599-603.
13. Ji J., Bunnelle W.H., Anderson D.J., Faltynek C., Dyhring T., Ahring P.K., et al. A-366833: A novel nicotinonitrile-substituted 3,6-diazabicyclo[3.2.0]-heptane alpha4beta2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in animal models. Biochemical Pharmacology 2007, 74:1253-1262.
14. 18F-nifene binding to α4β2 nicotinic receptors in the rat brain using microPET imaging. EJNMMI Research 2011, 1:6.
15. Kulak J.M., Musachio J.L., McIntosh J.M., Quik M. Declines in different β2* nicotinic receptor populations in monkey striatum after nigrostriatal damage. Journal of Pharmacology and Experimental Therapeutics 2002, 303:633-639.
16. Lida Y., Ogawa M., Ueda M., Tominaga A., Kawashima H., Magata Y., et al. Evaluation of 5-11C-methyl-A-85380 as an imaging agent for PET investigations of brain nicotinic acetylcholine receptors. Journal of Nuclear Medicine 2004, 45:878-884.
17. Lloyd G.K., Williams M. Neuronal nicotinic acetylcholine receptors as novel drug targets. Journal of Pharmacology and Experimental Therapeutics 2000, 292:461-467.
18. Lukas R.J., Changeux J.P., Le Novere N., Albuquerque E.X., Balfour D.J., Berg D.K., et al. International union of pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits. Pharmacological Reviews 1999, 51:397-401.
19. Ueda M., Iida Y., Yoneyama T., Kawai T., Ogawa M., Magata Y., et al. In vivo relationship between thalamic nicotinic acetylcholine receptor occupancy rates and antiallodynic effects in rat model of neuropathic pain: Persistent agonist binding inhibits the expression of antiallodynic effects. Synapse 2011, 65:77-83.
20. Musachio J.L., Villemagne V.L., Scheffel U.A., Dannals R.F., Dogan A.S., Yokoi F., et al. Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon. Nuclear Medicine and Biology 1999, 26:201-207.
21. Need A.B., McKinzie J.H., Mitch C.H., Statnick M.A, Phebus L.A., et al. In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously. Life Sciences 2007, 81:1389-1396.
22. 3 receptor antagonist in rats using non-radiolabeled tracer. Journal of Pharmacological and Toxicological Methods 2012, 10.1016/j.vascn.2012.03.003.
23. Obinu M.C., Reibaud M., Miquet J.M., Pasquet M., Rooney T. Brain-selective stimulation of nicotinic receptors by TC-1734 enhances ACh transmission from frontoparietal cortex and memory in rodents. Progress in Neuro-Psychopharmacology & Biological Psychiatry 2002, 26:913-918.
24. 3H]-2-FA and the agonist AZD3480 (TC-1734) at neuronal nicotinic receptors; 2008-S-100556-SfN: 2008 2008.
25. Perry D.C., Xiao Y., Nguyen H.N., Musachio J.L., Dávila-García M.I., Kellar K.J. Measuring nicotinic receptors with characteristics of alpha4 beta2, alpha3 beta2 and alpha3 beta4 subtypes in rat tissues by autoradiography. Journal of Neurochemistry 2002, 82:468-481.
26. Pimlott S.L., Piggott M., Patterson J., Cavanagh J., Wyper D.J. SPECT imaging of the α4β2 nicotinic receptor using [5-123I] A85380. Journal of Labelled Compounds and Radiopharmaceuticals 2007, 50:250-253.
27. Rao T.S., Adams P.B., Correa L.D., Santori E.M., Sacaan A.I., Reid R.T., et al. Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist. Brain Research 2008, 1234:16-24.
28. 18F]ZW-104, a new radioligand for imaging α2-α3-α4/β2 central nicotinic acetylcholine receptors: Evaluation in mutant mice. Synapse 2010, 64:570-572.
29. Sullivan J.P., Donnelly-Roberts D., Briggs C.A., Anderson D.J., Gopalakrishnan M., Xue I.C., et al. ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties. Journal of Pharmacology and Experimental Therapeutics 1997, 283:235-246.
30. Summers K.L., Lippiello P., Giacobini E. A microdialysis study of the effects of the nicotinic agonist RJR-2403 on cortical release of acetylcholine and biogenic amines. Neurochemical Research 1996, 21:1181-1186.
31. 18F-ZW-104: A new radioligand for imaging neuronal nicotinic acetylcholine receptors in vitro binding properties and PET studies in baboons. Journal of Nuclear Medicine 2009, 50:1349-1355.
32. 18F]F-A-85380. NeuroImage 2007, 34:1352-1362.
33. Whiting P.J., Liu R., Morley B.J., Lindstrom J.M. Structurally different neuronal nicotinic acetylcholine receptor subtypes purified and characterized using monoclonal antibodies. Journal of Neuroscience 1987, 7:4005-4016.