Involvement of substance P and the NK-1 receptor in pancreatic cancer

World Journal of Gastroenterology

Volumn 20, Issue 9, 2014, Pages 2321-2334

  Muñoz, Miguel ^a   Coveñas, Rafael ^b  

^a Instituto de Biomedicina de Sevilla   (Spain)

^b UNIVERSITY OF SALAMANCA   (Spain)

Author keywords

Angiogenesis; Antitumor; Apoptosis; Metastasis; Neurokinin 1 receptor antagonists; Pancreas; Pancreatic cancer; Substance P

Indexed keywords

APREPITANT; CHEMOKINE RECEPTOR CXCR2; CISPLATIN; CLATHRIN; CYCLIC AMP; CYCLOPHOSPHAMIDE; DOPAMINE; DOXORUBICIN; FOSAPREPITANT; G PROTEIN COUPLED RECEPTOR; GELATINASE A; IFOSFAMIDE; INTERLEUKIN 8; MITOGEN ACTIVATED PROTEIN KINASE; MITOMYCIN; MYOSIN LIGHT CHAIN PHOSPHATASE; NATURAL KILLER CELL RECEPTOR; NEUROKININ 1 RECEPTOR; NORADRENALIN; PHOSPHOLIPASE D; PROTEIN KINASE B; SUBSTANCE P RECEPTOR; TACHYKININ RECEPTOR; VINBLASTINE; ANGIOGENESIS INHIBITOR; NEUROKININ 1 RECEPTOR ANTAGONIST; SUBSTANCE P;

ANGIOGENESIS; APOPTOSIS; ARTICLE; CANCER INFILTRATION; CELL MIGRATION; CELL SPECIFICITY; GENE SILENCING; HUMAN; IMMUNOHISTOCHEMISTRY; INOSITOL PHOSPHATE ACCUMULATION ASSAY; MITOGENESIS; NEUROBLASTOMA; PANCREAS CANCER; PROTEIN EXPRESSION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; RHABDOMYOSARCOMA; TUMOR XENOGRAFT; ANIMAL; CELL MOTION; CELL PROLIFERATION; DRUG EFFECTS; METABOLISM; MOLECULARLY TARGETED THERAPY; NEOVASCULARIZATION (PATHOLOGY); PANCREATIC NEOPLASMS; PATHOLOGY; SIGNAL TRANSDUCTION; TREATMENT OUTCOME; TUMOR INVASION; VASCULARIZATION;

ANGIOGENESIS INHIBITORS; ANIMALS; APOPTOSIS; CELL MOVEMENT; CELL PROLIFERATION; HUMANS; MOLECULAR TARGETED THERAPY; NEOPLASM INVASIVENESS; NEOVASCULARIZATION, PATHOLOGIC; NEUROKININ-1 RECEPTOR ANTAGONISTS; PANCREATIC NEOPLASMS; RECEPTORS, NEUROKININ-1; SIGNAL TRANSDUCTION; SUBSTANCE P; TREATMENT OUTCOME;

EID: 84895883660     PISSN: 10079327     EISSN: 22192840     Source Type: Journal    
DOI: 10.3748/wjg.v20.i9.2321     Document Type: Article

References (110)

1. Siegel R, Naishadham D, Jemal A. Cancer statistics, 2013. CA Cancer J Clin 2013; 63: 11-30 [PMID: 23335087 DOI: 10.3322/caac.21166]
2. Li D, Xie K, Wolff R, Abbruzzese JL. Pancreatic cancer. Lancet 2004; 363: 1049-1057 [PMID: 15051286 DOI: 10.1016/ S0140-6736(04)15841-8]
3. Muñoz M, Coveñas R. Involvement of substance P and the NK-1 receptor in cancer progression. Peptides 2013; 48: 1-9 [PMID: 23933301]
4. Muñoz M, Rosso M, Coveñas R. A new frontier in the treatment of cancer: NK-1 receptor antagonists. Curr Med Chem 2010; 17: 504-516 [PMID: 20015033 DOI: 10.2174/0929867107 90416308]
5. Muñoz M, Rosso M, Coveñas R. The NK-1 receptor: a new target in cancer therapy. Curr Drug Targets 2011; 12: 909-921 [PMID: 21226668 DOI: 10.2174/138945011795528796]
6. Hennig IM, Laissue JA, Horisberger U, Reubi JC. Substance-P receptors in human primary neoplasms: tumoral and vascular localization. Int J Cancer 1995; 61: 786-792 [PMID: 7790112 DOI: 10.1002/ijc.2910610608]
7. DeFea KA, Vaughn ZD, O'Bryan EM, Nishijima D, Déry O, Bunnett NW. The proliferative and antiapoptotic effects of substance P are facilitated by formation of a beta-arrestin-dependent scaffolding complex. Proc Natl Acad Sci USA 2000; 97: 11086-11091 [PMID: 10995467 DOI: 10.1073/ pnas.190276697]
8. Feng F, Yang J, Tong L, Yuan S, Tian Y, Hong L, Wang W, Zhang H. Substance P immunoreactive nerve fibres are related to gastric cancer differentiation status and could promote proliferation and migration of gastric cancer cells. Cell Biol Int 2011; 35: 623-629 [PMID: 21091434 DOI: 10.1042/ CBI20100229]
9. Lewis KM, Harford-Wright E, Vink R, Nimmo AJ, Ghabriel MN. Walker 256 tumour cells increase substance P immunoreactivity locally and modify the properties of the bloodbrain barrier during extravasation and brain invasion. Clin Exp Metastasis 2013; 30: 1-12 [PMID: 22610781 DOI: 10.1007/ s10585-012-9487-z]
10. Friess H, Zhu Z, Liard V, Shi X, Shrikhande SV, Wang L, Lieb K, Korc M, Palma C, Zimmermann A, Reubi JC, Büchler MW. Neurokinin-1 receptor expression and its potential effects on tumor growth in human pancreatic cancer. Lab Invest 2003; 83: 731-742 [PMID: 12746482]
11. Guha S, Eibl G, Kisfalvi K, Fan RS, Burdick M, Reber H, Hines OJ, Strieter R, Rozengurt E. Broad-spectrum G proteincoupled receptor antagonist, [D-Arg1, D-Trp5,7,9, Leu11]SP: a dual inhibitor of growth and angiogenesis in pancreatic cancer. Cancer Res 2005; 65: 2738-2745 [PMID: 15805273 DOI: 10.1158/0008-5472.CAN-04-3197]
12. Muñoz M, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs 2010; 28: 187-193 [PMID: 19148578 DOI: 10.1007/ s10637-009-9218-8]
13. Muñoz M, Rosso M, Coveñas R. The NK-1 receptor is involved in the antitumoural action of L-733,060 and in the mitogenic action of substance P on human pancreatic cancer cell lines. Lett Drug Des Discov 2006; 3: 323-329 [DOI: 10.2174 /157018006777574168]
14. Li X, Ma G, Ma Q, Li W, Liu J, Han L, Duan W, Xu Q, Liu H, Wang Z, Sun Q, Wang F, Wu E. Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells. Mol Cancer Res 2013; 11: 294-302 [PMID: 23345604 DOI: 10.1158/1541-7786.MCR-12-0609]
15. Douglas SD, Leeman SE. Neurokinin-1 receptor: functional significance in the immune system in reference to selected infections and inflammation. Ann N Y Acad Sci 2011; 1217: 83-95 [PMID: 21091716 DOI: 10.1111/j.1749-6632.2010.05826.x]
16. Otsuka M, Yoshioka K. Neurotransmitter functions of mammalian tachykinins. Physiol Rev 1993; 73: 229-308 [PMID: 7682720]
17. Ho WZ, Douglas SD. Substance P and neurokinin-1 receptor modulation of HIV. J Neuroimmunol 2004; 157: 48-55 [PMID: 15579279]
18. Almeida TA, Rojo J, Nieto PM, Pinto FM, Hernandez M, Martín JD, Candenas ML. Tachykinins and tachykinin receptors: structure and activity relationships. Curr Med Chem 2004; 11: 2045-2081 [PMID: 15279567 DOI: 10.2174/09298670 43364748]
19. Satake H, Kawada T. Overview of the primary structure, tissue-distribution, and functions of tachykinins and their receptors. Curr Drug Targets 2006; 7: 963-974 [PMID: 16918325 DOI: 10.2174/138945006778019273]
20. Kwatra MM, Schwinn DA, Schreurs J, Blank JL, Kim CM, Benovic JL, Krause JE, Caron MG, Lefkowitz RJ. The substance P receptor, which couples to Gq/11, is a substrate of beta-adrenergic receptor kinase 1 and 2. J Biol Chem 1993; 268: 9161-9164 [PMID: 7683643]
21. Raddatz R, Crankshaw CL, Snider RM, Krause JE. Similar rates of phosphatidylinositol hydrolysis following activation of wild-type and truncated rat neurokinin-1 receptors. J Neurochem 1995; 64: 1183-1191 [PMID: 7532207 DOI: 10.1046/ j.1471-4159.1995.64031183.x]
22. Quartara L, Maggi CA. The tachykinin NK1 receptor. Part I: ligands and mechanisms of cellular activation. Neuropeptides 1997; 31: 537-563 [PMID: 9574822 DOI: 10.1016/ S0143-4179(97)90001-9]
23. Bowden JJ, Garland AM, Baluk P, Lefevre P, Grady EF, Vigna SR, Bunnett NW, McDonald DM. Direct observation of substance P-induced internalization of neurokinin 1 (NK1) receptors at sites of inflammation. Proc Natl Acad Sci USA 1994; 91: 8964-8968 [PMID: 7522326]
24. Garland AM, Grady EF, Payan DG, Vigna SR, Bunnett NW. Agonist-induced internalization of the substance P (NK1) receptor expressed in epithelial cells. Biochem J 1994; 303 (Pt 1): 177-186 [PMID: 7524481]
25. Grady EF, Garland AM, Gamp PD, Lovett M, Payan DG, Bunnett NW. Delineation of the endocytic pathway of substance P and its seven-transmembrane domain NK1 receptor. Mol Biol Cell 1995; 6: 509-524 [PMID: 7545030 DOI: 10.1091/mbc.6.5.509]
26. Mantyh PW, Allen CJ, Ghilardi JR, Rogers SD, Mantyh CR, Liu H, Basbaum AI, Vigna SR, Maggio JE. Rapid endocytosis of a G protein-coupled receptor: substance P evoked internalization of its receptor in the rat striatum in vivo. Proc Natl Acad Sci USA 1995; 92: 2622-2626 [PMID: 7535928 DOI: 10.1073/pnas.92.7.2622]
27. Mitsuhashi M, Ohashi Y, Shichijo S, Christian C, Sudduth-Klinger J, Harrowe G, Payan DG. Multiple intracellular signaling pathways of the neuropeptide substance P receptor. J Neurosci Res 1992; 32: 437-443 [PMID: 1279191 DOI: 10.1002/ jnr.490320315]
28. Brener S, González-Moles MA, Tostes D, Esteban F, Gil-Montoya JA, Ruiz-Avila I, Bravo M, Muñoz M. A role for the substance P/NK-1 receptor complex in cell proliferation in oral squamous cell carcinoma. Anticancer Res 2009; 29: 2323-2329 [PMID: 19528498]
29. Eistetter HR, Mills A, Brewster R, Alouani S, Rambosson C, Kawashima E. Functional characterization of neurokinin-1 receptors on human U373MG astrocytoma cells. Glia 1992; 6: 89-95 [PMID: 1328053]
30. Esteban F, Gonzalez-Moles MA, Castro D, Martin-Jaen Mdel M, Redondo M, Ruiz-Avila I, Muñoz M. Expression of substance P and neurokinin-1-receptor in laryngeal cancer: linking chronic inflammation to cancer promotion and progression. Histopathology 2009; 54: 258-260 [PMID: 19207952 DOI: 10.1111/j.1365-2559.2008.03193.x]
31. González Moles MA, Mosqueda-Taylor A, Esteban F, Gil-Montoya JA, Díaz-Franco MA, Delgado M, Muñoz M. Cell proliferation associated with actions of the substance P/NK-1 receptor complex in keratocystic odontogenic tumours. Oral Oncol 2008; 44: 1127-1133 [PMID: 18486533 DOI: 10.1016/j.oraloncology.2008.02.010]
32. Mukerji I, Ramkissoon SH, Reddy KK, Rameshwar P. Autocrine proliferation of neuroblastoma cells is partly mediated through neurokinin receptors: relevance to bone marrow metastasis. J Neurooncol 2005; 71: 91-98 [PMID: 15690122 DOI: 10.1007/s11060-004-9182-2]
33. Muñoz M, González-Ortega A, Coveñas R. The NK-1 receptor is expressed in human leukemia and is involved in the antitumor action of aprepitant and other NK-1 receptor antagonists on acute lymphoblastic leukemia cell lines. Invest New Drugs 2012; 30: 529-540 [PMID: 21120581 DOI: 10.1007/ s10637-010-9594-0]
34. Muñoz M, González-Ortega A, Rosso M, Robles-Frias MJ, Carranza A, Salinas-Martín MV, Coveñas R. The substance P/neurokinin-1 receptor system in lung cancer: focus on the antitumor action of neurokinin-1 receptor antagonists. Peptides 2012; 38: 318-325 [PMID: 23026680 DOI: 10.1016/ j.peptides.2012.09.024]
35. Muñoz M, Rosso M, Coveñas R, Montero I, González-Moles MA, Robles MJ. Neurokinin-1 receptors located in human retinoblastoma cell lines: antitumor action of its antagonist, L-732,138. Invest Ophthalmol Vis Sci 2007; 48: 2775-2781 [PMID: 17525212 DOI: 10.1167/iovs.05-1591]
36. Muñoz M, Rosso M, Pérez A, Coveñas R, Rosso R, Zamarriego C, Piruat JI. The NK1 receptor is involved in the antitumoural action of L-733,060 and in the mitogenic action of substance P on neuroblastoma and glioma cell lines. Neuropeptides 2005; 39: 427-432 [PMID: 15939468 DOI: 10.1016/ j.npep.2005.03.004]
37. Muñoz M, Rosso M, Robles-Frias MJ, Salinas-Martín MV, Rosso R, González-Ortega A, Coveñas R. The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines. Lab Invest 2010; 90: 1259-1269 [PMID: 20458280 DOI: 10.1038/labinvest.2010.92]
38. Rosso M, Robles-Frías MJ, Coveñas R, Salinas-Martín MV, Muñoz M. The NK-1 receptor is expressed in human primary gastric and colon adenocarcinomas and is involved in the antitumor action of L-733,060 and the mitogenic action of substance P on human gastrointestinal cancer cell lines. Tumour Biol 2008; 29: 245-254 [PMID: 18781096 DOI: 10.1159/000152942]
39. Patel HJ, Ramkissoon SH, Patel PS, Rameshwar P. Transformation of breast cells by truncated neurokinin-1 receptor is secondary to activation by preprotachykinin-A peptides. Proc Natl Acad Sci USA 2005; 102: 17436-17441 [PMID: 16291810 DOI: 10.1073/pnas.0506351102]
40. Moharita A, Harrison, JS, Rameshwar P. Neurokinin receptors and subtypes as potential targets in breast cancer: relevance to bone marrow metastasis. Drug Res Rev 2004; 1: 1-6 [DOI: 10.2174/1567269043390771]
41. Ramkissoon SH, Patel PS, Taborga M, Rameshwar P. Nuclear factor-kappaB is central to the expression of truncated neurokinin-1 receptor in breast cancer: implication for breast cancer cell quiescence within bone marrow stroma. Cancer Res 2007; 67: 1653-1659 [PMID: 17308106 DOI: 10.1158/0008-5472. CAN-06-3813]
42. Gillespie E, Leeman SE, Watts LA, Coukos JA, O'Brien MJ, Cerda SR, Farraye FA, Stucchi AF, Becker JM. Truncated neurokinin-1 receptor is increased in colonic epithelial cells from patients with colitis-associated cancer. Proc Natl Acad Sci USA 2011; 108: 17420-17425 [PMID: 21969570 DOI: 10.1073/pnas.1114275108]
43. Ehlers RA, Kim Sh, Zhang Y, Ethridge RT, Murrilo C, Hellmich MR, Evans DB, Townsend CM, Mark Evers B. Gut peptide receptor expression in human pancreatic cancers. Ann Surg 2000; 231: 838-848 [PMID: 10816627]
44. Schulz S, Stumm R, Röcken C, Mawrin C, Schulz S. Immunolocalization of full-length NK1 tachykinin receptors in human tumors. J Histochem Cytochem 2006; 54: 1015-1020 [PMID: 16651388 DOI: 10.1369/jhc.6A6966.2006]
45. Luo W, Sharif TR, Sharif M. Substance P-induced mitogenesis in human astrocytoma cells correlates with activation of the mitogen-activated protein kinase signaling pathway. Cancer Res 1996; 56: 4983-4991 [PMID: 8895754]
46. Lowenfels AB, Maisonneuve P, Cavallini G, Ammann RW, Lankisch PG, Andersen JR, Dimagno EP, Andrén-Sandberg A, Domellöf L. Pancreatitis and the risk of pancreatic cancer. International Pancreatitis Study Group. N Engl J Med 1993; 328: 1433-1437 [PMID: 8479461 DOI: 10.1056/ NEJM199305203282001]
47. Shrikhande SV, Friess H, di Mola FF, Tempia-Caliera A, Conejo Garcia JR, Zhu Z, Zimmermann A, Büchler MW. NK-1 receptor gene expression is related to pain in chronic pancreatitis. Pain 2001; 91: 209-217 [PMID: 11275376 DOI: 10.1016/S0304-3959(00)00436-X]
48. Palma C, Nardelli F, Manzini S, Maggi CA. Substance P activates responses correlated with tumour growth in human glioma cell lines bearing tachykinin NK1 receptors. Br J Cancer 1999; 79: 236-243 [PMID: 9888463 DOI: 10.1038/ sj.bjc.6690039]
49. Nakajima Y, Tsuchida K, Negishi M, Ito S, Nakanishi S. Direct linkage of three tachykinin receptors to stimulation of both phosphatidylinositol hydrolysis and cyclic AMP cascades in transfected Chinese hamster ovary cells. J Biol Chem 1992; 267: 2437-2442 [PMID: 1370820]
50. Takeda Y, Blount P, Sachais BS, Hershey AD, Raddatz R, Krause JE. Ligand binding kinetics of substance P and neurokinin A receptors stably expressed in Chinese hamster ovary cells and evidence for differential stimulation of inositol 1,4,5-trisphosphate and cyclic AMP second messenger responses. J Neurochem 1992; 59: 740-745 [PMID: 1321234 DOI: 10.1111/j.1471-4159.1992.tb09430.x]
51. Akazawa T, Kwatra SG, Goldsmith LE, Richardson MD, Cox EA, Sampson JH, Kwatra MM. A constitutively active form of neurokinin 1 receptor and neurokinin 1 receptor-mediated apoptosis in glioblastomas. J Neurochem 2009; 109: 1079-1086 [PMID: 19519779 DOI: 10.1111/j.1471-4159.2009.06032.x]
52. Fowler CJ, Brännström G. Substance P enhances forskolinstimulated cyclic AMP production in human UC11MG astrocytoma cells. Methods Find Exp Clin Pharmacol 1994; 16: 21-28 [PMID: 7513037]
53. Gitter BD, Regoli D, Howbert JJ, Glasebrook AL, Waters DC. Interleukin-6 secretion from human astrocytoma cells induced by substance P. J Neuroimmunol 1994; 51: 101-108 [PMID: 7512575 DOI: 10.1016/S0165-5728(97)00167-7]
54. Johnson CL, Johnson CG. Substance P regulation of glutamate and cystine transport in human astrocytoma cells. Receptors Channels 1993; 1: 53-59 [PMID: 7521733]
55. Medrano S, Gruenstein E, Dimlich RV. Substance P receptors on human astrocytoma cells are linked to glycogen breakdown. Neurosci Lett 1994; 167: 14-18 [PMID: 7513838 DOI: 10.1016/0304-3940(94)91017-0]
56. Tung WL, Lee CM. Effects of tachykinins on [3H]taurine release from human astrocytoma cells (U-373 MG). Brain Res 1991; 549: 171-173 [PMID: 1716506 DOI: 10.1002/glia.440110309]
57. Warburg O. On the origin of cancer cells. Science 1956; 123: 309-314 [PMID: 13298683 DOI: 10.1126/science.123.3191.309]
58. Sporn MB. The war on cancer. Lancet 1996; 347: 1377-1381 [PMID: 8637346 DOI: 10.1016/S0140-6736(96)91015-6]
59. Lang K, Drell TL, Lindecke A, Niggemann B, Kaltschmidt C, Zaenker KS, Entschladen F. Induction of a metastatogenic tumor cell type by neurotransmitters and its pharmacological inhibition by established drugs. Int J Cancer 2004; 112: 231-238 [PMID: 15352035 DOI: 10.1002/ijc.20410]
60. Fackler OT, Grosse R. Cell motility through plasma membrane blebbing. J Cell Biol 2008; 181: 879-884 [PMID: 18541702 DOI: 10.1083/jcb.200802081]
61. Meshki J, Douglas SD, Lai JP, Schwartz L, Kilpatrick LE, Tuluc F. Neurokinin 1 receptor mediates membrane blebbing in HEK293 cells through a Rho/Rho-associated coiled-coil kinase-dependent mechanism. J Biol Chem 2009; 284: 9280-9289 [PMID: 19179340 DOI: 10.1074/jbc.M808825200]
62. Reeve JG, Bleehen NM. [D-Arg1, D-Phe5, D-Trp7,9, Leu11] substance P induces apoptosis in lung cancer cell lines in vitro. Biochem Biophys Res Commun 1994; 199: 1313-1319 [PMID: 7511895 DOI: 10.1006/bbrc.1994.1374]
63. Woll PJ, Rozengurt E. [D-Arg1, D-Phe5, D-Trp7,9, Leu11]substance P, a potent bombesin antagonist in murine Swiss 3T3 cells, inhibits the growth of human small cell lung cancer cells in vitro. Proc Natl Acad Sci USA 1988; 85: 1859-1863 [PMID: 2450349]
64. Seckl MJ, Higgins T, Rozengurt E. [D-Arg1, D-Trp5,7,9, Leu11]Substance P coordinately and reversibly inhibits bombesin-and vasopressin-induced signal transduction pathways in Swiss 3T3 cells. J Biol Chem 1996; 271: 29453-29460 [PMID: 8910612 DOI: 10.1074/ jbc.271.46.29453]
65. Seckl MJ, Higgins T, Widmer F, Rozengurt E. [D-Arg1, DTrp5,7,9, Leu11]substance P: a novel potent inhibitor of signal transduction and growth in vitro and in vivo in small cell lung cancer cells. Cancer Res 1997; 57: 51-54 [PMID: 8988040]
66. Snider RM, Constantine JW, Lowe JA, Longo KP, Lebel WS, Woody HA, Drozda SE, Desai MC, Vinick FJ, Spencer RW. A potent nonpeptide antagonist of the substance P (NK1) receptor. Science 1991; 251: 435-437 [PMID: 1703323 DOI: 10.1126/science.1703323]
67. Maggi CA, Patacchini R, Rovero P, Giachetti A. Tachykinin receptors and tachykinin receptor antagonists. J Auton Pharmacol 1993; 13: 23-93 [PMID: 8382703]
68. Regoli D, Boudon A, Fauchére JL. Receptors and antagonists for substance P and related peptides. Pharmacol Rev 1994; 46: 551-599 [PMID: 7534932]
69. Giardina GA, Gagliardi S, Martinelli M. Antagonists at the neurokinin receptors--recent patent literature. IDrugs 2003; 6: 758-772 [PMID: 12917772]
70. Muñoz M, Coveñas R. Safety of neurokinin-1 receptor antagonists. Expert Opin Drug Saf 2013; 12: 673-685 [PMID: 23706125 DOI: 10.1517/14740338.2013.804059]
71. Munoz M, Covenas R. NK-1 receptor antagonists: a new generation of anticancer drugs. Mini Rev Med Chem 2012; 12: 593-599 [PMID: 22512565 DOI: 10.2174/138955712800626692]
72. Harrison T, Williams BJ, Swain CJ, Ball RG. Piperidine-ether based hNK1 antagonists 1: determination of the relative and absolute stereochemical requirements. Biomed Chem Lett 1994: 4: 2545-2550 [DOI: 10.1016/S0960-894X(01)80280-8]
73. Rupniak NM, Carlson E, Boyce S, Webb JK, Hill RG. Enantioselective inhibition of the formalin paw late phase by the NK1 receptor antagonist L-733,060 in gerbils. Pain 1996; 67: 189-195 [PMID: 8895247]
74. Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek JJ, Reines SA, Liu G, Snavely D, Wyatt-Knowles E, Hale JJ, Mills SG, MacCoss M, Swain CJ, Harrison T, Hill RG, Hefti F, Scolnick EM, Cascieri MA, Chicchi GG, Sadowski S, Williams AR, Hewson L, Smith D, Carlson EJ, Hargreaves RJ, Rupniak NM. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 1998; 281: 1640-1645 [PMID: 9733503 DOI: 10.1126/science. 281.5383.1640]
75. Varty GB, Cohen-Williams ME, Hunter JC. The antidepressant-like effects of neurokinin NK1 receptor antagonists in a gerbil tail suspension test. Behav Pharmacol 2003; 14: 87-95 [PMID: 12576885]
76. Rupniak NM, Carlson EC, Harrison T, Oates B, Seward E, Owen S, de Felipe C, Hunt S, Wheeldon A. Pharmacological blockade or genetic deletion of substance P (NK(1) receptors attenuates neonatal vocalisation in guinea-pigs and mice. Neuropharmacology 2000; 39: 1413-1421 [PMID: 10818257 DOI: 10.1016/S0028-3908(00)00052-6]
77. Bang R, Sass G, Kiemer AK, Vollmar AM, Neuhuber WL, Tiegs G. Neurokinin-1 receptor antagonists CP-96,345 and L-733,060 protect mice from cytokine-mediated liver injury. J Pharmacol Exp Ther 2003; 305: 31-39 [PMID: 12649350 DOI: 10.1124/jpet.102.043539]
78. Muñoz M, Pérez A, Rosso M, Zamarriego C, Rosso R. Antitumoral action of the neurokinin-1 receptor antagonist L-733 060 on human melanoma cell lines. Melanoma Res 2004; 14: 183-188 [PMID: 15179186]
79. Muñoz M, Rosso M, Pérez A, Coveñas R, Rosso R, Zamarriego C, Soult JA, Montero I. Antitumoral action of the neurokinin-1-receptor antagonist L-733,060 and mitogenic action of substance P on human retinoblastoma cell lines. Invest Ophthalmol Vis Sci 2005; 46: 2567-2570 [PMID: 15980249 DOI: 10.1167/iovs.04-1530]
80. Muñoz M, Rosso M, Aguilar FJ, González-Moles MA, Redondo M, Esteban F. NK-1 receptor antagonists induce apoptosis and counteract substance P-related mitogenesis in human laryngeal cancer cell line HEp-2. Invest New Drugs 2008; 26: 111-118 [PMID: 17906845 DOI: 10.1007/s10637-007-9087-y]
81. Muñoz M, Pérez A, Coveñas R, Rosso M, Castro E. Antitumoural action of L-733,060 on neuroblastoma and glioma cell lines. Arch Ital Biol 2004; 142: 105-112 [PMID: 15248566]
82. Humphrey JM. Medicinal chemistry of selective neurokinin-1 antagonists. Curr Top Med Chem 2003; 3: 1423-1435 [PMID: 12871173]
83. Tattersall FD, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, Hale JJ, Mills SG, Finke PE, MacCoss M, Sadowski S, Ber E, Cascieri M, Hill RG, MacIntyre DE, Hargreaves RJ. The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets. Neuropharmacology 2000; 39: 652-663 [PMID: 10728886 DOI: 10.1016/S0028-3908(99)00172-0]
84. Navari RM. Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Expert Opin Investig Drugs 2007; 16: 1977-1985 [PMID: 18042005 DOI: 10.1517/13543784.16.12.1977]
85. MacLeod AM, Merchant KJ, Brookfield F, Kelleher F, Stevenson G, Owens AP, Swain CJ, Casiceri MA, Sadowski S, Ber E. Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. J Med Chem 1994; 37: 1269-1274 [PMID: 7513763 DOI: 10.1021/ jm00035a006]
86. Cascieri MA, Macleod AM, Underwood D, Shiao LL, Ber E, Sadowski S, Yu H, Merchant KJ, Swain CJ, Strader CD. Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J Biol Chem 1994; 269: 6587-6591 [PMID: 7509807]
87. Cahill CM, Coderre TJ. Attenuation of hyperalgesia in a rat model of neuropathic pain after intrathecal pre-or post-treatment with a neurokinin-1 antagonist. Pain 2002; 95: 277-285 [PMID: 11839427 DOI: 10.1016/S0304-3959(01)00410-9]
88. Gitter BD, Waters DC, Threlkeld PG, Lovelace AM, Matsumoto K, Bruns RF. Cyclosporin A is a substance P (tachykinin NK1) receptor antagonist. Eur J Pharmacol 1995; 289: 439-446 [PMID: 7556412 DOI: 10.1016/0922-4106(95)90152-3]
89. Muñoz M, Rosso M, González A, Saenz J, Coveñas R. The broad-spectrum antitumor action of cyclosporin A is due to its tachykinin receptor antagonist pharmacological profile. Peptides 2010; 31: 1643-1648 [PMID: 20542069 DOI: 10.1016/ j.peptides.2010.06.002]
90. Bigioni M, Benzo A, Irrissuto C, Maggi CA, Goso C. Role of NK-1 and NK-2 tachykinin receptor antagonism on the growth of human breast carcinoma cell line MDA-MB-231. Anticancer Drugs 2005; 16: 1083-1089 [PMID: 16222150]
91. Huang WQ, Wang JG, Chen L, Wei HJ, Chen H. SR140333 counteracts NK-1 mediated cell proliferation in human breast cancer cell line T47D. J Exp Clin Cancer Res 2010; 29: 55 [PMID: 20497542 DOI: 10.1186/1756-9966-29-55]
92. Esteban F, Muñoz M, González-Moles MA, Rosso M. A role for substance P in cancer promotion and progression: a mechanism to counteract intracellular death signals following oncogene activation or DNA damage. Cancer Metastasis Rev 2006; 25: 137-145 [PMID: 16680578 DOI: 10.1007/ s10555-006-8161-9]
93. Choi MR, Jiles C, Seibel NL. Aprepitant use in children, adolescents, and young adults for the control of chemotherapyinduced nausea and vomiting (CINV). J Pediatr Hematol Oncol 2010; 32: e268-e271 [PMID: 20736848 DOI: 10.1097/ MPH.0b013e3181e5e1af]
94. Paul B, Trovato JA, Thompson J, Badros AZ, Goloubeva O. Efficacy of aprepitant in patients receiving high-dose chemotherapy with hematopoietic stem cell support. J Oncol Pharm Pract 2010; 16: 45-51 [PMID: 19525301 DOI: 10.1177/1078155 209105399]
95. Roila F, Rolski J, Ramlau R, Dediu M, Russo MW, Bandekar RR, Grunberg SM. Randomized, double-blind, dose-ranging trial of the oral neurokinin-1 receptor antagonist casopitant mesylate for the prevention of cisplatin-induced nausea and vomiting. Ann Oncol 2009; 20: 1867-1873 [PMID: 19541792 DOI: 10.1093/annonc/mdp194]
96. Ständer S, Siepmann D, Herrgott I, Sunderkötter C, Luger TA. Targeting the neurokinin receptor 1 with aprepitant: a novel antipruritic strategy. PLoS One 2010; 5: e10968 [PMID: 20532044 DOI: 10.1371/journal.pone.0010968]
97. Kitchens CA, McDonald PR, Pollack IF, Wipf P, Lazo JS. Synergy between microtubule destabilizing agents and neurokinin 1 receptor antagonists identified by an siRNA synthetic lethal screen. FASEB J 2009; 23: 756
98. Alfieri AB, Cubeddu LX. Efectos de los antagonistas de los receptores NK1 y de la dexametasona sobre la inflamación neurogénica inducida por ciclofosfamida y por radiación X, en la rata. AVFT 2004; 23: 61-66
99. Muñoz M, Berger M, Rosso M, Gonzalez-Ortega A, Carranza A, Coveñas R. Antitumor activity of neurokinin-1 receptor antagonists in MG-63 human osteosarcoma xenografts. Int J Oncol 2014; 44: 137-146 [PMID: 24190675 DOI: 10.3892/ ijo.2013.2164]
100. Walsh DT, Weg VB, Williams TJ, Nourshargh S. Substance P-induced inflammatory responses in guinea-pig skin: the effect of specific NK1 receptor antagonists and the role of endogenous mediators. Br J Pharmacol 1995; 114: 1343-1350 [PMID: 7541689]
101. Ziche M, Morbidelli L, Pacini M, Geppetti P, Alessandri G, Maggi CA. Substance P stimulates neovascularization in vivo and proliferation of cultured endothelial cells. Microvasc Res 1990; 40: 264-278 [PMID: 1701206]
102. Furmark T, Appel L, Michelgård A, Wahlstedt K, Ahs F, Zancan S, Jacobsson E, Flyckt K, Grohp M, Bergström M, Pich EM, Nilsson LG, Bani M, Långström B, Fredrikson M. Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo. Biol Psychiatry 2005; 58: 132-142 [PMID: 16038684 DOI: 10.1016/j.biopsych.2005.03.029]
103. Ebner K, Sartori SB, Singewald N. Tachykinin receptors as therapeutic targets in stress-related disorders. Curr Pharm Des 2009; 15: 1647-1674 [PMID: 19442179 DOI: 10.2174/13816 1209788168074]
104. Gilman JM, Hommer DW. Modulation of brain response to emotional images by alcohol cues in alcohol-dependent patients. Addict Biol 2008; 13: 423-434 [PMID: 18507736]
105. Borsook D, Upadhyay J, Klimas M, Schwarz AJ, Coimbra A, Baumgartner R, George E, Potter WZ, Large T, Bleakman D, Evelhoch J, Iyengar S, Becerra L, Hargreaves RJ. Decisionmaking using fMRI in clinical drug development: revisiting NK-1 receptor antagonists for pain. Drug Discov Today 2012; 17: 964-973 [PMID: 22579743 DOI: 10.1016/j.drudis.2012.05.004]
106. Dionne RA, Max MB, Gordon SM, Parada S, Sang C, Gracely RH, Sethna NF, MacLean DB. The substance P receptor antagonist CP-99,994 reduces acute postoperative pain. Clin Pharmacol Ther 1998; 64: 562-568 [PMID: 9834049 DOI: 10.1016/S0009-9236(98)90140-0]
107. Tebas P, Tuluc F, Barrett JS, Wagner W, Kim D, Zhao H, Gonin R, Korelitz J, Douglas SD. A randomized, placebo controlled, double masked phase IB study evaluating the safety and antiviral activity of aprepitant, a neurokinin-1 receptor antagonist in HIV-1 infected adults. PLoS One 2011; 6: e24180 [PMID: 21931661 DOI: 10.1371/journal.pone.0024180]
108. Saito H, Yoshizawa H, Yoshimori K, Katakami N, Katsumata N, Kawahara M, Eguchi K. Efficacy and safety of singledose fosaprepitant in the prevention of chemotherapy-induced nausea and vomiting in patients receiving high-dose cisplatin: a multicentre, randomised, double-blind, placebocontrolled phase 3 trial. Ann Oncol 2013; 24: 1067-1073 [PMID: 23117073 DOI: 10.1093/annonc/mds541]
109. Abidi MH, Tageja N, Ayash L, Abrams J, Ratanatharathorn V, Al-Kadhimi Z, Lum L, Cronin S, Ventimiglia M, Uberti J. Aprepitant for prevention of nausea and vomiting secondary to high-dose cyclophosphamide administered to patients undergoing autologous peripheral blood stem cells mobilization: a phase II trial. Support Care Cancer 2012; 20: 2363-2369 [PMID: 22193771 DOI: 10.1007/s00520-011-1341-3]
110. Olver I, Shelukar S, Thompson KC. Nanomedicines in the treatment of emesis during chemotherapy: focus on aprepitant. Int J Nanomedicine 2007; 2: 13-18 [PMID: 17722507]