Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors

Neurochemical Research

Volumn 40, Issue 10, 2014, Pages 2047-2054

  Brown, Jack L ^a   Wonnacott, Susan ^a  

^a University of Bath   (United Kingdom)

Author keywords

Live cell calcium imaging; PNU 120596; Primary cortical neurons; SH SY5Y cells

Indexed keywords

1 (5 CHLORO 2,4 DIMETHOXYPHENYL) 3 (5 METHYL 3 ISOXAZOLYL)UREA; BUNGAROTOXIN RECEPTOR; CALCIUM; MECAMYLAMINE; PARTIAL AGONIST; SAZETIDINE A; UNCLASSIFIED DRUG; 1-(5-CHLORO-2,4-DIMETHOXYPHENYL)-3-(5-METHYLISOXAZOL-3-YL)UREA; AZETIDINE DERIVATIVE; BENZAMIDE DERIVATIVE; BRIDGED BICYCLO COMPOUNDS; CARBANILAMIDE DERIVATIVE; ISOXAZOLE DERIVATIVE; NICOTINIC RECEPTOR; NICOTINIC RECEPTOR ALPHA4BETA2; PNU-282987; PYRIDINE DERIVATIVE; SAZETIDINE-A;

ANIMAL CELL; ARTICLE; BRAIN CELL; BRAIN CELL CULTURE; CALCIUM CELL LEVEL; DOSE RESPONSE; DRUG EFFECT; DRUG PROTEIN BINDING; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; MOUSE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR DOWN REGULATION; SH SY5Y CELL; ANIMAL; DRUG EFFECTS; METABOLISM; NERVE CELL; PATCH CLAMP TECHNIQUE; PROCEDURES; TUMOR CELL LINE;

ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR; ANIMALS; AZETIDINES; BENZAMIDES; BRIDGED BICYCLO COMPOUNDS; CALCIUM; CELL LINE, TUMOR; HUMANS; ISOXAZOLES; MICE; NEURONS; PATCH-CLAMP TECHNIQUES; PHENYLUREA COMPOUNDS; PYRIDINES; RECEPTORS, NICOTINIC;

EID: 84946495452     PISSN: 03643190     EISSN: 15736903     Source Type: Journal    
DOI: 10.1007/s11064-014-1302-6     Document Type: Article

References (31)

1. Xiao Y, Fan H, Musachio JL, Wei Z-L, Chellappan SK, Kozikowski AP, Kellar KJ (2006) Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them. Mol Pharmacol 70:1454–1460
2. Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, Broad LM, Williams AC, Zhang D, Ding C, Heinz BA, Sher E (2008) Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors. Mol Phamacol 73:1838–1843. doi:10.1124/mol.108.045104
3. Carbone AL, Moroni M, Groot-Kormelink PJ, Bermudez I (2009) Pentameric concatenated (alpha4)(2)(beta2)(3) and (alpha4)(3)(beta2)(2) nicotinic acetylcholine receptors: subunit arrangement determines functional expression. Br J Pharmacol 156:970–981. doi:10.1111/j.1476-5381.2008.00104.x
4. Kuryatov A, Onksen J, Lindstrom J (2008) Roles of accessory subunits in alpha4beta2(*) nicotinic receptors. Mol Pharmacol 74:132–143. doi:10.1124/mol.108.046789
5. Zhang J, Xiao YD, Jordan KG, Hammond PS, Van Dyke KM, Mazurov AA, Speake JD, Lippiello PM, James JW, Letchworth SR, Bencherif M, Hauser TA (2012) Analgesic effects mediated by neuronal nicotinic acetylcholine receptor agonists: correlation with desensitization of α4β2* receptors. Eur J Pharm Sci 47:813–823. doi:10.1016/j.ejps.2012.09.014
6. Kuryatov A, Lindstrom J (2011) Expression of functional human α6β2β3* acetylcholine receptors in Xenopus laevis oocytes achieved through subunit chimeras and concatamers. Mol Pharmacol 79:126–140. doi:10.1124/mol.110.066159
7. Campling BG, Kuryatov A, Lindstrom J (2013) Acute activation, desensitization and smoldering activation of human acetylcholine receptors. PLoS ONE 14(8):e79653. doi:10.1371/journal.pone.0079653
8. Eaton JB, Lucero LM, Stratton H, Chang Y, Cooper JF, Lindstrom JM, Lukas RJ, Whiteaker P (2014) The unique α4 ± α4 agonist binding site in (α4)3(β2)2 subtype nicotinic acetylcholine receptors permits differential agonist desensitization pharmacology versus the (α4)2(β2)3 subtype. J Pharmacol Exp Ther 348:46–58. doi:10.1124/jpet.113.208389
9. Liu Y, Richardson J, Tran T, Al-Muhtasib N, Xie T, Yenugonda VM, Sexton HG, Rezvani AH, Levin ED, Sahibzada N, Kellar KJ, Brown ML, Xiao Y, Paige M (2013) Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats. J Med Chem 11(56):3000–3011. doi:10.1021/jm4000374
10. Johnson JE, Slade S, Wells C, Petro A, Sexton H, Rezvani AH, Brown ML, Paige MA, McDowell BE, Xiao Y, Kellar KJ, Levin ED (2012) Assessing the effects of chronic sazetidine-A delivery on nicotine self-administration in both male and female rats. Psychopharmacology 222:269–276. doi:10.1007/s00213-012-2642-z
11. Rezvani AH, Cauley M, Sexton H, Xiao Y, Brown ML, Paige MA, McDowell BE, Kellar KJ, Levin ED (2012) Sazetidine-A, a selective α4β2 nicotinic acetylcholine receptor ligand: effects on dizocilpine and scopolamine-induced attentional impairments in female Sprague-Dawley rats. Psychopharmacology 215:621–630. doi:10.1007/s00213-010-2161-8
12. Alsharari SD, Carroll FI, McIntosh JM, Damaj MI (2012) The antinociceptive effects of nicotinic partial agonists varenicline and sazetidine-A in murine acute and tonic pain models. J Pharmacol Exp Ther 342:742–749. doi:10.1124/jpet.112.194506
13. Liu J, Yu LF, Eaton JB, Caldarone B, Cavino K, Ruiz C, Terry M, Fedolak A, Wang D, Ghavami A, Lowe DA, Brunner D, Lukas RJ, Kozikowski AP (2011) Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression. J Med Chem 54:7280–7288. doi:10.1021/jm200855b
14. Zwart R, Strotton M, Ching J, Astles PC, Sher E (2014) Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. Eur J Pharmacol 726C:77–86. doi:10.1016/j.ejphar.2014.01.031
15. Lendvai B, Kassai F, Szájli A, Némethy Z (2013) α7 nicotinic acetylcholine receptors and their role in cognition. Brain Res Bull 93:86–96. doi:10.1016/j.brainresbull.2012.11.003
16. Wallace TL, Bertrand D (2013) Importance of the nicotinic acetylcholine receptor system in the prefrontal cortex. Biochem Pharmacol 85:1713–1720. doi:10.1016/j.bcp.2013.04.001
17. Filippini P, Cesario A, Fini M, Locatelli F, Rutella S (2012) The Yin and Yang of non-neuronal α7-nicotinic receptors in inflammation and autoimmunity. Curr Drug Targets 13:644–655
18. Ridley DL, Pakkanen J, Wonnacott S (2002) Effects of chronic drug treatments on increases in intracellular calcium mediated by nicotinic acetylcholine receptors in SH-SY5Y cells. Br J Pharmacol 135:1051–1059
19. Hoey SE, Williams RJ, Perkinton MS (2009) Synaptic NMDA receptor activation stimulates alpha-secretase amyloid precursor protein processing and inhibits amyloid-beta production. J Neurosci 29:4442–4460. doi:10.1523/JNEUROSCI.6017-08.2009
20. 2+ stores. J Neurochem 81:606–614
21. Lukas RJ, Norman SA, Lucero L (1993) Characterization of Nnicotinic acetylcholine receptors expressed by cells of the SH-SY5Y human neuroblastoma clonal line. Mol Cell Neurosci 4:1–12. doi:10.1006/mcne.1993.1001
22. Peng X, Katz M, Gerzanich V, Anand R, Lindstrom J (1994) Human alpha 7 acetylcholine receptor: cloning of the alpha 7 subunit from the SH-SY5Y cell line and determination of pharmacological properties of native receptors and functional alpha 7 homomers expressed in Xenopus oocytes. Mol Pharmacol 45:546–554
23. Riganti L, Matteoni C, Di Angelantonio S, Nistri A, Gaimarri A, Sparatore F, Canu-Boido C, Clementi F, Gotti C (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br J Pharmacol 146:1096–1109
24. Innocent N, Livingstone PD, Hone A, Kimura A, Young T, Whiteaker P, McIntosh JM, Wonnacott S (2008) Alpha-conotoxin Arenatus IB[V11L, V16D] [corrected] is a potent and selective antagonist at rat and human native alpha7 nicotinic acetylcholine receptors. J Pharmacol Exp Ther 327:529–537. doi:10.1124/jpet.108.142943
25. Grønlien JH, Håkerud M, Ween H, Thorin-Hagene K, Briggs CA, Gopalakrishnan M, Malysz J (2007) Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol Pharmacol 72:715–724
26. Malysz J, Anderson DJ, Grønlien JH, Ji J, Bunnelle WH, Håkerud M, Thorin-Hagene K, Ween H, Helfrich R, Hu M, Gubbins E, Gopalakrishnan S, Puttfarcken PS, Briggs CA, Li J, Meyer MD, Dyhring T, Ahring PK, Nielsen EØ, Peters D, Timmermann DB, Gopalakrishnan M (2010) In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107. J Pharmacol Exp Ther 334:863–874. doi:10.1124/jpet.110.167072
27. Kalappa BI, Gusev AG, Uteshev VV (2010) Activation of functional α7-containing nAChRs in hippocampal CA1 pyramidal neurons by physiological levels of choline in the presence of PNU-120596. PLoS ONE 12(5):e13964. doi:10.1371/journal.pone.0013964
28. Hussmann GP, Turner JR, Lomazzo E, Venkatesh R, Cousins V, Xiao Y, Yasuda RP, Wolfe BB, Perry DC, Rezvani AH, Levin ED, Blendy JA, Kellar KJ (2012) Chronic sazetidine-A at behaviorally active doses does not increase nicotinic cholinergic receptors in rodent brain. J Pharmacol Exp Ther 343:441–450. doi:10.1124/jpet.112.198085
29. Lambe EK, Picciotto MR, Aghajanian GK (2003) Nicotine induces glutamate release from thalamocortical terminals in prefrontal cortex. Neuropsychopharmacology 28:216–225
30. Aracri P, Amadeo A, Pasini ME, Fascio U, Becchetti A (2013) Regulation of glutamate release by heteromeric nicotinic receptors in layer V of the secondary motor region (Fr2) in the dorsomedial shoulder of prefrontal cortex in mouse. Synapse 67:338–357. doi:10.1002/syn.21655
31. Poorthuis RB, Bloem B, Schak B, Wester J, de Kock CP, Mansvelder HD (2013) Layer-specific modulation of the prefrontal cortex by nicotinic acetylcholine receptors. Cereb Cortex 23:148–161. doi:10.1093/cercor/bhr390