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 ORCID:

Xiangyu HONG

https://orcid.org/0009-0003-0460-1196

Caiyun FU

https://orcid.org/0000-0003-4090-885X

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Journal of Zhejiang University SCIENCE B 2024 Vol.25 No.2 P.91-105

http://doi.org/10.1631/jzus.B2300455


Advances in the research and application of neurokinin-1 receptor antagonists


Author(s):  Xiangyu HONG, Junjie MA, Shanshan ZHENG, Guangyu ZHAO, Caiyun FU

Affiliation(s):  College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China

Corresponding email(s):   fucy03@zstu.edu.cn

Key Words:  Neurokinin-1 receptor (NK-1R) antagonist, Pathophysiological disorder, Tumor target, Bioavailability, Nanoencapsulation, Synergistic therapy


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Xiangyu HONG, Junjie MA, Shanshan ZHENG, Guangyu ZHAO, Caiyun FU. Advances in the research and application of neurokinin-1 receptor antagonists[J]. Journal of Zhejiang University Science B, 2024, 25(2): 91-105.

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Abstract: 
Recently, the substance P (SP)/neurokinin-1 receptor (NK-1R) system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019 (COVID-19). Besides, studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis. These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy. This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers, as well as the underlying mechanisms. Furthermore, the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized, such as solid dispersion systems, nanonization, and nanoencapsulation. As a radiopharmaceutical therapeutic, the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors. However, combining NK-1R antagonists with other drugs can produce a synergistic effect, thereby enhancing the therapeutic effect, alleviating the symptoms, and improving patients’ quality of life in several diseases and cancers.

神经激肽1受体拮抗剂的研究与应用进展

洪翔宇,马俊杰,郑珊珊,赵光宇,付彩云
浙江理工大学生命科学与医学学院,中国杭州市,310018
摘要:目前研究已经发现神经肽(SP)/神经激肽1受体(NK-1R)拮抗剂系统参与了包括2019冠状病毒病(COVID-19)症状在内的多种人体生理疾病。肿瘤学领域的最新研究表明:NK-1R的上调和SP/NK-1R系统的激活与多种癌症类型的进展和不良临床预后之间存在复杂的相关性,使用NK-1R拮抗剂来调节SP/NK-1R系统可成为一种潜在的广谱抗肿瘤策略。本文综述了NK-1R拮抗剂在人体生理疾病和癌症治疗中的最新应用和潜力以及相关机制,总结了改善NK-1R拮抗剂生物利用度和药效的策略(如固体分散系统、纳米化、纳米封装等),同时探讨了在放射药物治疗中,阿瑞匹坦作为放射配体受体以靶向过表达NK-1R的肿瘤疗法。此外,本文还总结了NK-1R拮抗剂与其他药物的协同效应,为NK-1R拮抗剂的创新应用提供了参考。

关键词:神经激肽1受体(NK-1R)拮抗剂;阿瑞匹坦;生理疾病;2019冠状病毒病(COVID-19);肿瘤靶点;纳米包被;生物相容性;放射性配体受体;联合疗法

Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article

Reference

[1]AfshariAR, Motamed-SanayeA, SabriH, et al., 2021. Neurokinin-1 receptor (NK-1R) antagonists: potential targets in the treatment of glioblastoma multiforme. Curr Med Chem, 28(24):4877-4892.

[2]AgelopoulosK, RülanderF, DangelmaierJ, et al., 2019. Neurokinin 1 receptor antagonists exhibit peripheral effects in prurigo nodularis including reduced ERK1/2 activation. J Eur Acad Dermatol Venereol, 33(12):2371-2379.

[3]AlwazzanA, MehboobR, HassanA, et al., 2020. Elevated neurokinin-1 receptor expression in uterine products of conception is associated with first trimester miscarriages. Front Physiol, 11:554766.

[4]BaiTR, ZhouD, WeirT, et al., 1995. Substance P (NK1)- and neurokinin A (NK2)-receptor gene expression in inflammatory airway diseases. Am J Physiol, 269(3 Pt 1):L309-L317.

[5]BakirtziK, LawIKM, FangK, et al., 2019. MiR-21 in substance P-induced exosomes promotes cell proliferation and migration in human colonic epithelial cells. Am J Physiol, 317(6):G802-G810.

[6]BarbeMF, HilliardBA, FisherPW, et al., 2020. Blocking substance P signaling reduces musculotendinous and dermal fibrosis and sensorimotor declines in a rat model of overuse injury. Connect Tissue Res, 61(6):604-619.

[7]BeirithI, RenzBW, MudusettiS, et al., 2021. Identification of the neurokinin-1 receptor as targetable stratification factor for drug repurposing in pancreatic cancer. Cancers (Basel), 13(11):2703.

[8]BiadseeA, BiadseeA, KassemF, et al., 2020. Olfactory and oral manifestations of COVID-19: sex-related symptoms—a potential pathway to early diagnosis. Otolaryngol Head Neck Surg, 163(4):722-728.

[9]BubakAN, ComoCN, BlackmonAM, et al., 2018. Varicella zoster virus induces nuclear translocation of the neurokinin-1 receptor, promoting lamellipodia formation and viral spread in spinal astrocytes. J Infect Dis, 218(8):1324-1335.

[10]ChenY, ChauhanSK, LeeHS, et al., 2014. Chronic dry eye disease is principally mediated by effector memory TH17 cells. Mucosal Immunol, 7(1):38-45.

[11]ChuHW, KraftM, KrauseJE, et al., 2000. Substance P and its receptor neurokinin 1 expression in asthmatic airways. J Allergy Clin Immunol, 106(4):713-722.

[12]CraigVJ, ZhangL, HagoodJS, et al., 2015. Matrix metalloproteinases as therapeutic targets for idiopathic pulmonary fibrosis. Am J Respir Cell Mol Biol, 53(5):585-600.

[13]de FelipeC, HerreroJF, O'BrienJA, et al., 1998. Altered nociception, analgesia and aggression in mice lacking the receptor for substance P. Nature, 392(6674):394-397.

[14]Definition and Classification Subcommittee, 2007. The definition and classification of dry eye disease: report of the Definition and Classification Subcommittee of the International Dry Eye Workshop (2007). Ocul Surf, 5(2):75-92.

[15]DehlinHM, LevickSP, 2014. Substance P in heart failure: the good and the bad. Int J Cardiol, 170(3):270-277.

[16]DengXT, TangSM, WuPY, et al., 2019. SP/NK-1R promotes gallbladder cancer cell proliferation and migration. J Cell Mol Med, 23(12):7961-7973.

[17]DongJQ, FengF, XuGH, et al., 2015. Elevated SP/NK-1R in esophageal carcinoma promotes esophageal carcinoma cell proliferation and migration. Gene, 560(2):205-210.

[18]DongYY, MoX, HuYB, et al., 2020. Epidemiology of COVID-19 among children in China. Pediatrics, 145(6):e20200702.

[19]DouglasSD, LeemanSE, 2011. Neurokinin-1 receptor: functional significance in the immune system in reference to selected infections and inflammation. Ann N Y Acad Sci, 1217:83-95.

[20]EbrahimiS, JavidH, AlaeiA, et al., 2020. New insight into the role of substance P/neurokinin-1 receptor system in breast cancer progression and its crosstalk with microRNAs. Clin Genet, 98(4):322-330.

[21]EbrahimiS, MirzaviF, Aghaee-BakhtiariSH, et al., 2022. SP/NK1R system regulates carcinogenesis in prostate cancer: shedding light on the antitumoral function of aprepitant. Biochim Biophys Acta Mol Cell Res, 1869(5):119221.

[22]FoulshamW, MarmalidouA, AmouzegarA, et al., 2017. Review: the function of regulatory T cells at the ocular surface. Ocul Surf, 15(4):652-659.

[23]García-ArandaM, TéllezT, McKennaL, et al., 2022. Neurokinin-1 receptor (NK-1R) antagonists as a new strategy to overcome cancer resistance. Cancers (Basel), 14(9):2255.

[24]GeCT, HuangHM, HuangFY, et al., 2019. Neurokinin-1 receptor is an effective target for treating leukemia by inducing oxidative stress through mitochondrial calcium overload. Proc Natl Acad Sci USA, 116(39):19635-19645.

[25]GhahremanlooA, JavidH, AfshariAR, et al., 2021. Investigation of the role of neurokinin-1 receptor inhibition using aprepitant in the apoptotic cell death through PI3K/Akt/NF-κB signal transduction pathways in colon cancer cells. Biomed Res Int, 2021:1383878.

[26]GhasemiA, HashemySI, AghaeiM, et al., 2018. Leptin induces matrix metalloproteinase 7 expression to promote ovarian cancer cell invasion by activating ERK and JNK pathways. J Cell Biochem, 119(2):2333-2344.

[27]GhasemiA, SaeidiJ, Azimi-NejadM, et al., 2019. Leptin-induced signaling pathways in cancer cell migration and invasion. Cell Oncol (Dordr), 42(3):243-260.

[28]GordonL, PolakJM, MoscosoGJ, et al., 1993. Development of the peptidergic innervation of human heart. J Anat, 183(Pt 1):131-140.

[29]HalikPK, LipińskiPFJ, MatalińskaJ, et al., 2020. Radiochemical synthesis and evaluation of novel radioconjugates of neurokinin 1 receptor antagonist aprepitant dedicated for NK1R-positive tumors. Molecules, 25(16):3756.

[30]HalikPK, KoźmińskiP, MatalińskaJ, et al., 2022. In vitro biological evaluation of aprepitant based 177Lu-radioconjugates. Pharmaceutics, 14(3):607.

[31]IsornaI, EstebanF, SolanellasJ, et al., 2020. The substance P and neurokinin-1 receptor system in human thyroid cancer: an immunohistochemical study. Eur J Histochem, 64(2):3117.

[32]JinP, QiDQ, CuiYH, et al., 2022. Aprepitant attenuates NLRC4-dependent neuronal pyroptosis via NK1R/PKCδ pathway in a mouse model of intracerebral hemorrhage. J Neuroinflammation, 19:198.

[33]KakadeP, PathanZ, GiteS, et al., 2022. Nanoparticle engineering of aprepitant using Nano-by-Design (NbD) approach. AAPS PharmSciTech, 23(6):204.

[34]KastRE, RamiroS, LladóS, et al., 2016. Antitumor action of temozolomide, ritonavir and aprepitant against human glioma cells. J Neurooncol, 126(3):425-431.

[35]KhomS, SteinkellnerT, HnaskoTS, et al., 2020. Alcohol dependence potentiates substance P/neurokinin-1 receptor signaling in the rat central nucleus of amygdala. Sci Adv, 6(12):eaaz1050.

[36]KhorasaniS, BoroumandN, Lavi ArabF, et al., 2020. The immunomodulatory effects of tachykinins and their receptors. J Cell Biochem, 121(5-6):3031-3041.

[37]KimRY, SunkaraKP, BrackeKR, et al., 2021. A microRNA-21-mediated SATB1/S100A9/NF-‍κB axis promotes chronic obstructive pulmonary disease pathogenesis. Sci Transl Med, 13(621):eaav7223.

[38]KitchensCA, McDonaldPR, PollackIF, et al., 2009. Synergy between microtubule destabilizing agents and neurokinin 1 receptor antagonists identified by an siRNA synthetic lethal screen. FASEB J, 23(S1):756.13-756.13.

[39]KorfiF, JavidH, Assaran DarbanR, et al., 2021. The effect of SP/NK1R on the expression and activity of catalase and superoxide dismutase in glioblastoma cancer cells. Biochem Res Int, 2021:6620708.

[40]KramerMS, CutlerN, FeighnerJ, et al., 1998. Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science, 281(5383):1640-1645.

[41]KumarS, GuptaSK, 2013. Pharmaceutical solid dispersion technology: a strategy to improve dissolution of poorly water-soluble drugs. Recent Pat Drug Deliv Formul, 7(2):111-121.

[42]LeeKS, LeeJ, KimHK, et al., 2021. Extracellular vesicles from adipose tissue-derived stem cells alleviate osteoporosis through osteoprotegerin and miR-21-5p. J Extracell Vesicles, 10(12):e12152.

[43]LiuJW, ZouMJ, PiaoHY, et al., 2015. Characterization and pharmacokinetic study of aprepitant solid dispersions with soluplus®. Molecules, 20(6):11345-11356.

[44]LiuJW, LiSY, AoW, et al., 2022a. Fabrication of an aprepitant nanosuspension using hydroxypropyl chitosan to increase the bioavailability. Biochem Biophys Res Commun, 631:72-77.

[45]LiuJW, LiYJ, AoW, et al., 2022b. Preparation and characterization of aprepitant solid dispersion with HPMCAS-LF. ACS Omega, 7(44):39907-39912.

[46]LiuL, BurcherE, 2005. Tachykinin peptides and receptors: putting amphibians into perspective. Peptides, 26(8):1369-1382.

[47]LiuXP, ZhuYL, ZhengW, et al., 2019. Antagonism of NK-1R using aprepitant suppresses inflammatory response in rheumatoid arthritis fibroblast-like synoviocytes. Artif Cells Nanomed Biotechnol, 47(1):1628-1634.

[48]LorestaniS, GhahremanlooA, JangjooA, et al., 2020. Evaluation of serum level of substance P and tissue distribution of NK-1 receptor in colorectal cancer. Mol Biol Rep, 47(5):3469-3474.

[49]MaedaH, WuJ, SawaT, et al., 2000. Tumor vascular permeability and the epr effect in macromolecular therapeutics: a review. J Control Release, 65(1-2):271-284.

[50]MahtalN, LenoirO, TinelC, et al., 2022. MicroRNAs in kidney injury and disease. Nat Rev Nephrol, 18(10):643-662.

[51]Maroñas-JiménezL, EstrachT, GallardoF, et al., 2018. Aprepitant improves refractory pruritus in primary cutaneous T-cell lymphomas: experience of the Spanish Working Group on Cutaneous Lymphomas. Br J Dermatol, 178(4):e273-e274.

[52]MartinezAN, PhilippMT, 2016. Substance P and antagonists of the neurokinin-1 receptor in neuroinflammation associated with infectious and neurodegenerative diseases of the central nervous system. J Neurol Neuromedicine, 1(2):29-36.

[53]MehboobR, LavezziAM, 2021. Neuropathological explan

[54]ation of minimal COVID-19 infection rate in newborns, infants and children—a mystery so far. New insight into the role of substance P. J Neurol Sci, 420:117276.

[55]MeléndezGC, LiJP, LawBA, et al., 2011. Substance P induces adverse myocardial remodelling via a mechanism involving cardiac mast cells. Cardiovasc Res, 92(3):420-429.

[56]MiaoYB, QuinnTP, 2021. Advances in receptor-targeted radiolabeled peptides for melanoma imaging and therapy. J Nucl Med, 62(3):313-318.

[57]MistrovaE, KruzliakP, DvorakovaMC, 2016. Role of substance P in the cardiovascular system. Neuropeptides, 58:41-51.

[58]MohamedMZ, Abed El BakyMF, AliME, et al., 2022. Aprepitant exerts anti-fibrotic effect via inhibition of TGF-β/Smad3 pathway in bleomycin-induced pulmonary fibrosis in rats. Environ Toxicol Pharmacol, 95:103940.

[59]MohammadiF, JavidH, AfshariAR, et al., 2020. Substance P accelerates the progression of human esophageal squamous cell carcinoma via MMP-2, MMP-9, VEGF-A, and VEGFR1 overexpression. Mol Biol Rep, 47(6):4263-4272.

[60]Molinos-QuintanaA, Trujillo-HachaP, PiruatJI, et al., 2019. Human acute myeloid leukemia cells express Neurokinin-1 receptor, which is involved in the antileukemic effect of Neurokinin-1 receptor antagonists. Invest New Drugs, 37:17-26.

[61]MorgatC, MishraAK, VarshneyR, et al., 2014. Targeting neuropeptide receptors for cancer imaging and therapy: perspectives with bombesin, neurotensin, and neuropeptide-Y receptors. J Nucl Med, 55(10):1650-1657.

[62]MozafariM, EbrahimiS, DarbanRA, et al., 2022. Potential in vitro therapeutic effects of targeting SP/NK1R system in cervical cancer. Mol Biol Rep, 49(2):1067-1076.

[63]MuñozM, RossoM, 2010. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs, 28(2):187-193.

[64]MuñozM, CoveñasR, 2020a. The neurokinin-1 receptor antagonist aprepitant, a new drug for the treatment of hematological malignancies: focus on acute myeloid leukemia. J Clin Med, 9(6):1659.

[65]MuñozM, CoveñasR, 2020b. The neurokinin-1 receptor antagonist aprepitant: an intelligent bullet against cancer? Cancers, 12(9):2682.

[66]MuñozM, RossoM, Robles-FriasMJ, et al., 2010. 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, 90(8):‍1259-1269.

[67]MuñozM, González-OrtegaA, RossoM, et al., 2012. The substance P/neurokinin-1 receptor system in lung cancer: focus on the antitumor action of neurokinin-1 receptor antagonists. Peptides, 38(2):318-325.

[68]MuñozM, González-OrtegaA, Salinas-MartínMV, et al., 2014. The neurokinin-1 receptor antagonist aprepitant is a promising candidate for the treatment of breast cancer. Int J Oncol, 45(4):1658-1672.

[69]MuñozM, CovenasR, EstebanF, et al., 2015. The substance P/NK-1 receptor system: NK-1 receptor antagonists as anti-cancer drugs. J Biosci, 40(2):441-463.

[70]MuñozM, CrespoJC, CrespoJP, et al., 2019a. Neurokinin-1 receptor antagonist aprepitant and radiotherapy, a successful combination therapy in a patient with lung cancer: a case report. Mol Clin Oncol, 11(1):50-54.

[71]MuñozM, RossoM, CoveñasR, 2019b. Neurokinin-1 receptor antagonists against hepatoblastoma. Cancers (Basel), 11(9):1258.

[72]MuñozM, RossoM, CoveñasR, 2020. Triple negative breast cancer: how neurokinin-1 receptor antagonists could be used as a new therapeutic approach. Mini Rev Med Chem, 20(5):408-417.

[73]MuñozMF, ArgüellesS, RossoM, et al., 2022. The neurokinin-1 receptor is essential for the viability of human glioma cells: a possible target for treating glioblastoma. Biomed Res Int, 2022:6291504.

[74]MuraS, NicolasJ, CouvreurP, 2013. Stimuli-responsive nanocarriers for drug delivery. Nat Mater, 12(11):991-1003.

[75]NizamE, ErinN, 2018. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; effects independent of substance P. Biomed Pharmacother, 108:263-270.

[76]NoronhaV, BhattacharjeeA, PatilVM, et al., 2020. Aprepitant for cough suppression in advanced lung cancer: a randomized trial. Chest, 157(6):1647-1655.

[77]The Novel Coronavirus Pneumonia Emergency Response Epidemiology Team, 2020. The epidemiological characteristics of an outbreak of 2019 novel coronavirus diseases (COVID-19)—China, 2020. China CDC Wkly, 2(8):113-122.

[78]OlivieriF, PrattichizzoF, GiulianiA, et al., 2021. miR-21 and miR-146a: the micrornas of inflammaging and age-related diseases. Ageing Res Rev, 70:101374.

[79]OlverI, ShelukarS, ThompsonKC, 2007. Nanomedicines in the treatment of emesis during chemotherapy: focus on aprepitant. Int J Nanomedicine, 2(1):13-18.

[80]QuartaraL, AltamuraM, 2006. Tachykinin receptors antagonists: from research to clinic. Curr Drug Targets, 7(8):975-992.

[81]RamanujamD, SchönAP, BeckC, et al., 2021. MicroRNA-21-dependent macrophage-to-fibroblast signaling determines the cardiac response to pressure overload. Circulation, 143(15):1513-1525.

[82]Ramírez-GarcíaPD, RetamalJS, ShenoyP, et al., 2019. A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prevent chronic pain. Nat Nanotechnol, 14(12):1150-1159.

[83]RattiE, BetticaP, AlexanderR, et al., 2013. Full central neurokinin-1 receptor blockade is required for efficacy in depression: evidence from orvepitant clinical studies. J Psychopharmacol, 27(5):424-434.

[84]Reinoso-ArijaR, López-RamírezC, Jimenez-RuizJA, et al., 2021. Effectiveness of aprepitant in post-acute COVID19 syndrome. Clin Case Rep, 9(9):e04646.

[85]RidhurkarDN, AnsariKA, KumarD, et al., 2013. Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties. Drug Dev Ind Pharm, 39(11):1783-1792.

[86]RobinsonP, KasembeliM, BharadwajU, et al., 2016. Substance P receptor signaling mediates doxorubicin-induced cardiomyocyte apoptosis and triple-negative breast cancer chemoresistance. Biomed Res Int, 2016:1959270.

[87]RoosC, DahlgrenD, BergS, et al., 2017. In vivo mechanisms of intestinal drug absorption from aprepitant nanoformulations. Mol Pharm, 14(12):4233-4242.

[88]RouenPA, WhiteML, 2018. Dry eye disease: prevalence, assessment, and management. Home Healthc Now, 36(2):74-83.

[89]ShiY, WangX, MengY, et al., 2021. A novel mechanism of endoplasmic reticulum stress- and c-Myc-degradation-mediated therapeutic benefits of antineurokinin-1 receptor drugs in colorectal cancer. Adv Sci (Weinh), 8(21):e2101936.

[90]SchöppeJ, EhrenmannJ, KlenkC, et al., 2019. Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists. Nat Commun, 10:17.

[91]SinghS, KumaravelS, DholeS, et al., 2021. Neuropeptide substance P enhances inflammation-mediated tumor signaling pathways and migration and proliferation of head and neck cancers. Indian J Surg Oncol, 12 (S1):93-102.

[92]SmithJA, HarleA, DockryR, et al., 2021. Aprepitant for cough in lung cancer. A randomized placebo-controlled trial and mechanistic insights. Am J Respir Crit Care Med, 203(6):737-745.

[93]SosnikA, SeremetaKP, 2015. Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers. Adv Colloid Interface Sci, 223:40-54.

[94]SteinhoffMS, von MentzerB, GeppettiP, et al., 2014. Tachykinins and their receptors: contributions to physiological control and the mechanisms of disease. Physiol Rev, 94(1):265-301.

[95]SuganoK, TeradaK, 2015. Rate- and extent-limiting factors of oral drug absorption: theory and applications. J Pharm Sci, 104(9):2777-2788.

[96]TaketaniY, DohlmanT, ChenYH, et al., 2019. Restoration of regulatory T cell function in dry eye disease by targeting substance P/neurokinin 1 receptor. Invest Ophthalmol Vis Sci, 60(9):306.

[97]TangYJ, LiuJJ, ZhangDY, et al., 2020. Cytokine storm in COVID-19: the current evidence and treatment strategies. Front Immunol, 11:1708.

[98]TattersallFD, RycroftW, FrancisB, et al., 1996. Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets. Neuropharmacology, 35(8):1121-1129.

[99]ThomC, EhrenmannJ, VaccaS, et al., 2021. Structures of neurokinin 1 receptor in complex with Gq and Gs proteins reveal substance P binding mode and unique activation features. Sci Adv, 7(50):eabk2872.

[100]UnH, UganRA, KoseD, et al., 2020. A novel effect of Aprepitant: protection for cisplatin-induced nephrotoxicity and hepatotoxicity. Eur J Pharmacol, 880:173168.

[101]WanPX, SuWR, ZhangYY, et al., 2020. LncRNA H19 initiates microglial pyroptosis and neuronal death in retinal ischemia/reperfusion injury. Cell Death Differ, 27:176-191.

[102]WangXL, HeY, MackowiakB, et al., 2021. MicroRNAs as regulators, biomarkers and therapeutic targets in liver diseases. Gut, 70(4):784-795.

[103]WidiapradjaA, ManteufelEJ, DehlinHM, et al., 2019. Regulation of cardiac mast cell maturation and function by the neurokinin-1 receptor in the fibrotic heart. Sci Rep, 9:11004.

[104]WuHZ, ChengXE, HuangFY, et al., 2020. Aprepitant sensitizes acute myeloid leukemia cells to the cytotoxic effects of cytosine arabinoside in vitro and in vivo. Drug Des Devel Ther, 14:2413-2422.

[105]YamamotoH, 1993. Preserved endothelial function in the spastic segment of the human epicardial coronary artery in patients with variant angina—role of substance P in evaluating endothelial function. Eur Heart J, 14(Suppl I):118-122.

[106]YanaiR, NishidaT, HatanoM, et al., 2020. Role of the neurokinin-1 receptor in the promotion of corneal epithelial wound healing by the peptides FGLM-NH2 and SSSR in neurotrophic keratopathy. Invest Ophthalmol Vis Sci, 61(8):29.

[107]YangY, ZhouW, XuXQ, et al., 2021. Aprepitant inhibits JNK and p38/MAPK to attenuate inflammation and suppresses inflammatory pain. Front Pharmacol, 12:811584.

[108]YeoS, AnJ, ParkC, et al., 2020. Design and characterization of phosphatidylcholine-based solid dispersions of aprepitant for enhanced solubility and dissolution. Pharmaceutics, 12(5):407.

[109]ZhangXW, XingHJ, ZhaoY, et al., 2018. Pharmaceutical dispersion techniques for dissolution and bioavailability enhancement of poorly water-soluble drugs. Pharmaceutics, 10(3):74.

[110]ZhangXW, LiL, HuWQ, et al., 2022. Neurokinin-1 receptor promotes non-small cell lung cancer progression through transactivation of EGFR. Cell Death Dis, 13:41.

[111]ZhaoXN, BaiZZ, LiCH, et al., 2020. The NK-1R antagonist aprepitant prevents LPS-induced oxidative stress and inflammation in RAW264.7 macrophages. Drug Des Devel Ther, 14:1943-1952.

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