Advance in nicotinic acetylcholine receptors as analgesic targets

ZHU Deyuan; WANG Yiran; CAI Guojun; XU Tianying

doi:10.3969/j.issn.1006-0111.2015.04.005

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Article Navigation > Journal of Pharmaceutical Practice and Service > 2015 > 33(4): 309-312,375

ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005

Citation:

ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005

Advance in nicotinic acetylcholine receptors as analgesic targets

doi: 10.3969/j.issn.1006-0111.2015.04.005

1.
Changhai Hospital, Second Military Medical University, Shanghai 200433, China
2.
Department of pharmacology, Second Military Medical University, Shanghai 200433, China

Received Date: 2015-01-07
Rev Recd Date: 2015-05-05

Abstract

Nicotinic acetylcholine receptors (nAChRs),also known as neuronal nicotinic receptors,are widely expressed throughout the central and peripheral nervous system. nAChRs play crucial roles in pain signaling. Recently, agonists that target specific nAChR subtypes have shown substantial efficacy in a wide range of acute and chronic pain models, contributing to developing novel analgesic drugs with low drug dependence. Positive allosteric modulators offer new approaches for increasing the potency and therapeutic window of these drugs. This review summarizes the advances in nicotinic acetylcholine receptors as analgesic targets and anticipate the future directions in this field.
- nAChRs,
- analgesia,
- positive allosteric modulators

References

[1]	Del Bufalo A, Cesario A, Salinaro G, et al. Alpha9 alpha10 nicotinic acetylcholine receptors as target for the treatment of chronic pain [J]. Curr Pharm Des, 2014, 20(38): 6042-6047.
[2]	Woodcock J. A difficult balance——pain management, drug safety, and the FDA [J]. N Engl J Med, 2009, 361(22): 2105-2107.
[3]	Ballantyne JC, Shin NS. Efficacy of opioids for chronic pain: a review of the evidence [J]. Clin J Pain, 2008, 24(6): 469-478.
[4]	Smith HS. Opioids and neuropathic pain [J]. Pain Physician, 2012, 15(3 Suppl): ES93-110.
[5]	Corti C. A history of smoking [M]. Montana: Kessinger Publishing, 2007:112.
[6]	Davis L, Pollock LJ, Stone T. Visceral pain [J]. Surg Gynecol Obstetr, 1932, 55: 418-427.
[7]	Sahley TL, Berntson GG. Antinociceptive effects of central and systemic administrations of nicotine in the rat [J]. Psychopharmacology, 1979, 65(3):279-283.
[8]	Garraffo HM, Spande TF, Williams M. Epibatidine: from frog alkaloid to analgesic clinical candidates. A testimonial to true grit! [J]. Heterocycles, 2009, 79: 207-217.
[9]	Rupniak NM, Patel S, Marwood R, et al. Antinociceptive and toxic effects of (+)-epibatidine oxalate attributableto nicotinic agonist activity [J]. Br J Pharmacol, 1994, 113(4): 1487-1493.
[10]	Umana IC, Daniele CA, McGehee DS. Neuronal nicotinic receptors as analgesic targets: it's a winding road [J]. Biochem Pharmacol, 2013, 86(8): 1208-1214.
[11]	Marubio LM, del Mar Arroyo-Jimenez M, Cordero-Erausquin M, et al. Reduced antinociception in mice lacking neuronal nicotinic receptor subunits [J]. Nature, 1999, 398(6730): 805-810.
[12]	Nirogi R, Goura V, Abraham R, et al. α4β2* neuronal nicotinic receptor ligands (agonist, partial agonist and positive allosteric modulators) as therapeutic prospects for pain [J]. Eur J Pharmacol, 2013, 712(1-3): 22-29.
[13]	Rueter LE, Meyer MD, Decker MW. Spinal mechanisms underlying A-85380-induced effects on acute thermal pain [J]. Brain Res, 2000, 872(1-2): 93-101.
[14]	Daly JW, Garraffo HM, Spande TF, et al. Alkaloids from frog skin: the discovery of epibatidine and the potential for developing novel non-opioid analgesics [J]. Nat Prod Rep, 2000, 17(2): 131-135.
[15]	Bannon AW, Decker MW, Holladay MW, et al. Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors[J]. Science, 1998, 279(5347): 77-81.
[16]	Lynch JJ 3rd, Wade CL, Mikusa JP, et al. ABT-594 (a nicotinic acetylcholine agonist): anti-allodynia in a rat chemotherapy-induced pain model [J].Eur J Pharmacol, 2005, 509(1): 43-48.
[17]	Holladay MW, Wasicak JT, Lin NH, 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 [J]. J Med Chem, 1998, 41(4): 407-412.
[18]	Alsharari SD, Freitas K, Damaj MI. Functional role of alpha7 nicotinic receptor in chronic neuropathic and inflammatory pain: studies in transgenic mice [J]. Biochem Pharmacol, 2013, 86(8):1201-1207.
[19]	Gao B, Hierl M, Clarkin K, et al. Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptoragonists in animal models of persistent pain [J]. Pain,2010, 149(1): 33-49.
[20]	Bagdas D, Sonat FA, Hamurtekin E, et al. The antihyperalgesic effect of cytidine-50-diphosphate-choline in neuropathic and inflammatory pain models [J]. Behav Pharmacol, 2011, 22(5-6): 589-598.
[21]	刘献文, 张宗旺. 尼古丁镇痛作用机制的研究进展 [J]. 国际麻醉学与复苏杂志, 2013, 34(4): 368-370.
[22]	Cordero-Erausquin M, Changeux JP. Tonic nicotinic modulation of serotoninergic transmission in the spinal cord [J]. Proc Natl Acad Sci(USA), 2001, 98(5): 2803-2807.
[23]	Frber L, Stratz T, Brückle W, et al. Efficacy and tolerability of tropisetron in primary fibromyalgia--a highly selective and competitive 5-HT₃ receptor antagonist. German Fibromyalgia Study Group [J]. Scand J Rheumatol Suppl, 2000, 113: 49-54.
[24]	Ramirez-Latorre J, Yu CR, Qu X, et al. Functional contributions of alpha5 subunit to neuronal acetylcholine receptor channels [J]. Nature,1996, 380(6572): 347-351.
[25]	Jackson KJ, Sanjakdar SS, Muldoon PP, et al. a3b4*nicotinic acetylcholine receptor subtype mediates nicotine reward and physicalnicotine withdrawal signs independently of the a5 subunit in the mouse[J]. Neuropharmacology, 2013, 70: 228-235.
[26]	Lee CH, Zhu C, Malysz J, et al. a4b2neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of a4b2 nAChR agonists in pain [J]. Biochem Pharmacol, 2011, 82(8):959-966.
[27]	Uteshev VV. The therapeutic promise of positive allosteric modulation of nicotinic receptors [J]. Eur J Pharmacol, 2014, 727: 181-185.
[28]	Zhu CZ, Chin CL, Rustay NR, et al. Potentiation ofanalgesic efficacy but not side effects: co-administration of an alpha4beta2neuronal nicotinic acetylcholine receptor agonist and its positive allostericmodulator in experimental models of pain in rats [J]. Biochem Pharmacol, 2011, 82(8): 967-976.
[29]	Freitas K, Negus SS, Carroll FI, et al. In vivo pharmacological interactions between a type II positive allosteric modulator of α7 nicotinic ACh receptors and nicotinic agonists in a murine tonic pain model [J]. Br J Pharmacol, 2013, 169(3): 567-579.

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通讯作者: 陈斌, bchen63@163.com

1.
沈阳化工大学材料科学与工程学院沈阳 110142

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Advance in nicotinic acetylcholine receptors as analgesic targets

1. Changhai Hospital, Second Military Medical University, Shanghai 200433, China

2. Department of pharmacology, Second Military Medical University, Shanghai 200433, China

Received Date: 2015-01-07

Rev Recd Date: 2015-05-05

Key words:

Abstract: Nicotinic acetylcholine receptors (nAChRs),also known as neuronal nicotinic receptors,are widely expressed throughout the central and peripheral nervous system. nAChRs play crucial roles in pain signaling. Recently, agonists that target specific nAChR subtypes have shown substantial efficacy in a wide range of acute and chronic pain models, contributing to developing novel analgesic drugs with low drug dependence. Positive allosteric modulators offer new approaches for increasing the potency and therapeutic window of these drugs. This review summarizes the advances in nicotinic acetylcholine receptors as analgesic targets and anticipate the future directions in this field.

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Reference (29)

[1]	Del Bufalo A, Cesario A, Salinaro G, et al. Alpha9 alpha10 nicotinic acetylcholine receptors as target for the treatment of chronic pain [J]. Curr Pharm Des, 2014, 20(38): 6042-6047.
[2]	Woodcock J. A difficult balance——pain management, drug safety, and the FDA [J]. N Engl J Med, 2009, 361(22): 2105-2107.
[3]	Ballantyne JC, Shin NS. Efficacy of opioids for chronic pain: a review of the evidence [J]. Clin J Pain, 2008, 24(6): 469-478.
[4]	Smith HS. Opioids and neuropathic pain [J]. Pain Physician, 2012, 15(3 Suppl): ES93-110.
[5]	Corti C. A history of smoking [M]. Montana: Kessinger Publishing, 2007:112.
[6]	Davis L, Pollock LJ, Stone T. Visceral pain [J]. Surg Gynecol Obstetr, 1932, 55: 418-427.
[7]	Sahley TL, Berntson GG. Antinociceptive effects of central and systemic administrations of nicotine in the rat [J]. Psychopharmacology, 1979, 65(3):279-283.
[8]	Garraffo HM, Spande TF, Williams M. Epibatidine: from frog alkaloid to analgesic clinical candidates. A testimonial to true grit! [J]. Heterocycles, 2009, 79: 207-217.
[9]	Rupniak NM, Patel S, Marwood R, et al. Antinociceptive and toxic effects of (+)-epibatidine oxalate attributableto nicotinic agonist activity [J]. Br J Pharmacol, 1994, 113(4): 1487-1493.
[10]	Umana IC, Daniele CA, McGehee DS. Neuronal nicotinic receptors as analgesic targets: it's a winding road [J]. Biochem Pharmacol, 2013, 86(8): 1208-1214.
[11]	Marubio LM, del Mar Arroyo-Jimenez M, Cordero-Erausquin M, et al. Reduced antinociception in mice lacking neuronal nicotinic receptor subunits [J]. Nature, 1999, 398(6730): 805-810.
[12]	Nirogi R, Goura V, Abraham R, et al. α4β2* neuronal nicotinic receptor ligands (agonist, partial agonist and positive allosteric modulators) as therapeutic prospects for pain [J]. Eur J Pharmacol, 2013, 712(1-3): 22-29.
[13]	Rueter LE, Meyer MD, Decker MW. Spinal mechanisms underlying A-85380-induced effects on acute thermal pain [J]. Brain Res, 2000, 872(1-2): 93-101.
[14]	Daly JW, Garraffo HM, Spande TF, et al. Alkaloids from frog skin: the discovery of epibatidine and the potential for developing novel non-opioid analgesics [J]. Nat Prod Rep, 2000, 17(2): 131-135.
[15]	Bannon AW, Decker MW, Holladay MW, et al. Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors[J]. Science, 1998, 279(5347): 77-81.
[16]	Lynch JJ 3rd, Wade CL, Mikusa JP, et al. ABT-594 (a nicotinic acetylcholine agonist): anti-allodynia in a rat chemotherapy-induced pain model [J].Eur J Pharmacol, 2005, 509(1): 43-48.
[17]	Holladay MW, Wasicak JT, Lin NH, 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 [J]. J Med Chem, 1998, 41(4): 407-412.
[18]	Alsharari SD, Freitas K, Damaj MI. Functional role of alpha7 nicotinic receptor in chronic neuropathic and inflammatory pain: studies in transgenic mice [J]. Biochem Pharmacol, 2013, 86(8):1201-1207.
[19]	Gao B, Hierl M, Clarkin K, et al. Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptoragonists in animal models of persistent pain [J]. Pain,2010, 149(1): 33-49.
[20]	Bagdas D, Sonat FA, Hamurtekin E, et al. The antihyperalgesic effect of cytidine-50-diphosphate-choline in neuropathic and inflammatory pain models [J]. Behav Pharmacol, 2011, 22(5-6): 589-598.
[21]	刘献文, 张宗旺. 尼古丁镇痛作用机制的研究进展 [J]. 国际麻醉学与复苏杂志, 2013, 34(4): 368-370.
[22]	Cordero-Erausquin M, Changeux JP. Tonic nicotinic modulation of serotoninergic transmission in the spinal cord [J]. Proc Natl Acad Sci(USA), 2001, 98(5): 2803-2807.
[23]	Frber L, Stratz T, Brückle W, et al. Efficacy and tolerability of tropisetron in primary fibromyalgia--a highly selective and competitive 5-HT₃ receptor antagonist. German Fibromyalgia Study Group [J]. Scand J Rheumatol Suppl, 2000, 113: 49-54.
[24]	Ramirez-Latorre J, Yu CR, Qu X, et al. Functional contributions of alpha5 subunit to neuronal acetylcholine receptor channels [J]. Nature,1996, 380(6572): 347-351.
[25]	Jackson KJ, Sanjakdar SS, Muldoon PP, et al. a3b4*nicotinic acetylcholine receptor subtype mediates nicotine reward and physicalnicotine withdrawal signs independently of the a5 subunit in the mouse[J]. Neuropharmacology, 2013, 70: 228-235.
[26]	Lee CH, Zhu C, Malysz J, et al. a4b2neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of a4b2 nAChR agonists in pain [J]. Biochem Pharmacol, 2011, 82(8):959-966.
[27]	Uteshev VV. The therapeutic promise of positive allosteric modulation of nicotinic receptors [J]. Eur J Pharmacol, 2014, 727: 181-185.
[28]	Zhu CZ, Chin CL, Rustay NR, et al. Potentiation ofanalgesic efficacy but not side effects: co-administration of an alpha4beta2neuronal nicotinic acetylcholine receptor agonist and its positive allostericmodulator in experimental models of pain in rats [J]. Biochem Pharmacol, 2011, 82(8): 967-976.
[29]	Freitas K, Negus SS, Carroll FI, et al. In vivo pharmacological interactions between a type II positive allosteric modulator of α7 nicotinic ACh receptors and nicotinic agonists in a murine tonic pain model [J]. Br J Pharmacol, 2013, 169(3): 567-579.

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Advance in nicotinic acetylcholine receptors as analgesic targets

doi: 10.3969/j.issn.1006-0111.2015.04.005

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References

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通讯作者: 陈斌, bchen63@163.com

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