Target Information

Target General Information

Target ID

T47094 (Former ID: TTDS00194)

Target Name

Substance-P receptor (TACR1)

Synonyms

Tachykinin receptor 1; Tachykinin neurokinin 1 receptor; Tachykinin 1 receptor; TACR1; Substance P receptor; SPR; Neurokinin 1 receptor; NK-1R; NK-1 receptor

Gene Name

TACR1

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Depression [ICD-11: 6A70-6A7Z]

Nausea/vomiting [ICD-11: MD90]

Function

This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K.

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BioChemical Class

GPCR rhodopsin

UniProt ID

NK1R_HUMAN

Sequence

MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAH
KRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTIST
VVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS

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3D Structure

Click to Show 3D Structure of This Target

PDB

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 4 Approved Drugs

Aprepitant

Drug Info

Approved

Depression

[2], [3]

Palonosetron + fosnetupitant

Drug Info

Approved

Chemotherapy-induced nausea

[4]

Rolapitant

Drug Info

Approved

Chemotherapy-induced nausea

[5], [6]

Selegiline

Drug Info

Approved

Major depressive disorder

[7], [8]

Clinical Trial Drug(s)

[+] 18 Clinical Trial Drugs

LY-686017

Drug Info

Phase 3

Atopic dermatitis

[9]

Netupitant

Drug Info

Phase 3

Chemotherapy-induced nausea

[10], [11]

Serlopitant

Drug Info

Phase 3

Prurigo nodularis

[9]

CP-122721

Drug Info

Phase 2

Major depressive disorder

[12]

DAPITANT

Drug Info

Phase 2

Pain

[13]

FR139317

Drug Info

Phase 2

Hypertension

[14], [15]

GW 597599

Drug Info

Phase 2

Mood disorder

[16]

LANEPITANT

Drug Info

Phase 2

Pain

[17], [18]

LY-2590443

Drug Info

Phase 2

Migraine

[19]

NKP 608

Drug Info

Phase 2

Mood disorder

[20]

Orvepitant

Drug Info

Phase 2

Anxiety disorder

[21]

SCH-900978

Drug Info

Phase 2

Cough

[22]

SSR240600

Drug Info

Phase 2

Urinary incontinence

[23]

TKA-731

Drug Info

Phase 2

Pain

[24]

VOFOPITANT HYDROCHLORIDE

Drug Info

Phase 2

Vomiting

[25], [26]

CJ-12255

Drug Info

Phase 1

Eczema

[27]

Figopitant

Drug Info

Phase 1

Diabetic complication

[28]

GSK1144814

Drug Info

Phase 1

Schizophrenia

[29]

Discontinued Drug(s)

[+] 24 Discontinued Drugs

Casopitant

Drug Info

Withdrawn from market

Chemotherapy-induced nausea

[30], [31]

BL-1832

Drug Info

Discontinued in Phase 3

Pain

[32]

L-759274

Drug Info

Discontinued in Phase 3

Depression

[31]

CGP-49823

Drug Info

Discontinued in Phase 2

Pain

[33]

CS-003

Drug Info

Discontinued in Phase 2

Chronic obstructive pulmonary disease

[34]

DNK-333

Drug Info

Discontinued in Phase 2

Irritable bowel syndrome

[34]

Ezlopitant

Drug Info

Discontinued in Phase 2

Irritable bowel syndrome

[35], [36]

FK-224

Drug Info

Discontinued in Phase 2

Asthma

[37], [38]

FK-888

Drug Info

Discontinued in Phase 2

Migraine

[39], [40]

GSK 679769

Drug Info

Discontinued in Phase 2

Major depressive disorder

[36]

Nolpitantium besilate

Drug Info

Discontinued in Phase 2

Asthma

[41], [42]

TA-5538

Drug Info

Discontinued in Phase 2

Overactive bladder

[43]

TAK-637

Drug Info

Discontinued in Phase 2

Depression

[31]

AVE-5883

Drug Info

Discontinued in Phase 1/2

Asthma

[44]

SDZ-NKT-343

Drug Info

Discontinued in Phase 1

Pain

[45]

SLV-323

Drug Info

Discontinued in Phase 1

Gastric motility disorder

[36]

FK-355

Drug Info

Terminated

Asthma

[46]

FR-113680

Drug Info

Terminated

Asthma

[47]

GR-82334

Drug Info

Terminated

Vomiting

[48]

L-741671

Drug Info

Terminated

Vomiting

[49]

MEN-11149

Drug Info

Terminated

Asthma

[50]

MEN-11467

Drug Info

Terminated

Respiratory tract inflammation

[51]

RP-67580

Drug Info

Terminated

Pain

[52], [53]

WIN-64821

Drug Info

Terminated

Asthma

[54]

Mode of Action

[+] 4 Modes of Action

Antagonist

[+] 51 Antagonist drugs

Aprepitant

Drug Info

[1]

Palonosetron + fosnetupitant

Drug Info

[4]

Rolapitant

Drug Info

[55]

Selegiline

Drug Info

[56]

LY-686017

Drug Info

[57]

Netupitant

Drug Info

[55]

Serlopitant

Drug Info

[9]

CP-122721

Drug Info

[58]

DAPITANT

Drug Info

[2], [59]

FR139317

Drug Info

[56]

GW 597599

Drug Info

[60]

LANEPITANT

Drug Info

[2], [61]

LY-2590443

Drug Info

[62]

NKP 608

Drug Info

[20]

Orvepitant

Drug Info

[56]

SCH-900978

Drug Info

[63]

SSR240600

Drug Info

[64]

TKA-731

Drug Info

[24]

VOFOPITANT HYDROCHLORIDE

Drug Info

[2], [65]

CJ-12255

Drug Info

[2], [66]

Figopitant

Drug Info

[67]

Casopitant

Drug Info

[31]

BL-1832

Drug Info

[69]

L-759274

Drug Info

[31]

CGP-49823

Drug Info

[70]

CS-003

Drug Info

[34]

Ezlopitant

Drug Info

[36], [72]

FK-888

Drug Info

[76]

GSK 679769

Drug Info

[36]

Nolpitantium besilate

Drug Info

[77]

TA-5538

Drug Info

[78]

TAK-637

Drug Info

[31]

SDZ-NKT-343

Drug Info

[80]

CI-1021

Drug Info

[81]

FK-355

Drug Info

[74]

GR-82334

Drug Info

[84]

MEN-11149

Drug Info

[88]

MEN-11467

Drug Info

[89]

RP-67580

Drug Info

[90]

WIN-64821

Drug Info

[91]

befetupitant

Drug Info

[97]

CP-100263

Drug Info

[36]

CP-99,994

Drug Info

[81]

L-703,606

Drug Info

[98]

R116031

Drug Info

[104]

S-41744

Drug Info

[62]

SCH 206272

Drug Info

[105]

spantide II

Drug Info

[108]

T2328

Drug Info

[110]

[125I]L703,606

Drug Info

[116]

[18F]SPA-RQ

Drug Info

[62]

Modulator

[+] 10 Modulator drugs

GSK1144814

Drug Info

[68]

DNK-333

Drug Info

[71]

FK-224

Drug Info

[73], [74], [75]

AVE-5883

Drug Info

[79]

SLV-323

Drug Info

[36]

EU-C-001

Drug Info

[62]

WIN-64745

Drug Info

[112]

WIN-66306

Drug Info

[113]

WIN-68577

Drug Info

[113]

ZD-6021

Drug Info

[114], [114], [115]

Inhibitor

[+] 47 Inhibitor drugs

CP-96345

Drug Info

[82]

FR-113680

Drug Info

[83]

L-732138

Drug Info

[85]

L-733060

Drug Info

[86]

L-741671

Drug Info

[87]

(D)-Phe-(D)-Phe-NH2

Drug Info

[92]

(D)-Phe-(L)-Phe-NH2

Drug Info

[92]

(L)-Phe-(D)-Phe-NH2

Drug Info

[92]

2-Phenyl-3-(1-phenyl-ethoxy)-piperidine

Drug Info

[86]

3,6-Diphenyl-1-oxa-7-aza-spiro[4.5]decane

Drug Info

[93]

3-Benzyloxy-2-phenyl-piperidine

Drug Info

[86]

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[94]

7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX)

Drug Info

[95]

7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(R)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX)

Drug Info

[95]

7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(S)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX)

Drug Info

[95]

Ac-Phe-Phe-NH2

Drug Info

[92]

Arg-Pro-Lys-Pro-Ala-Gln-Phe-Phe-Gly-Leu-Met-NH2

Drug Info

[96]

Arg-Pro-Lys-Pro-Ala-Ser-Phe-Phe-Gly-Leu-Met-NH2

Drug Info

[96]

Arg-Pro-Lys-Pro-Gln-Ser-Phe-Phe-Gly-Leu-Met-NH2

Drug Info

[96]

ENDOMORPHIN 2

Drug Info

[92]

H-Ala-Pro-Phe-Phe-NH2

Drug Info

[92]

H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-OH

Drug Info

[92]

H-Leu-Phe-NH2

Drug Info

[92]

H-Phe-NH2

Drug Info

[92]

H-Phe-Phe-NH2

Drug Info

[92]

H-Pro-Phe-Phe-NH2

Drug Info

[92]

H-Tyr(OMe)-Phe(2-Me)-NH2

Drug Info

[92]

H-Tyr-Ala-Phe-Phe-NH2

Drug Info

[92]

H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2

Drug Info

[99]

H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2

Drug Info

[99]

H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl

Drug Info

[99]

H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2

Drug Info

[99]

H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl

Drug Info

[99]

H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl

Drug Info

[99]

H-Tyr-Pro-Ala-Phe-NH2

Drug Info

[92]

H-Tyr-Pro-Phe-Ala-NH2

Drug Info

[92]

H-Tyr-Pro-Phe-Phe-OH

Drug Info

[92]

L-708568

Drug Info

[100]

L-736281

Drug Info

[87]

MDL-28163

Drug Info

[101]

Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2

Drug Info

[96]

R-226161

Drug Info

[103]

SP-SAP

Drug Info

[62]

SPANTIDE

Drug Info

[107]

Substance P

Drug Info

[109]

Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl

Drug Info

[111]

[Sar9,Met(O2)11]-SP

Drug Info

[117]

Agonist

[+] 6 Agonist drugs

eledoisin

Drug Info

[98]

Homspera

Drug Info

[62]

kassinin

Drug Info

[98]

neurokinin A

Drug Info

[102]

physalaemin

Drug Info

[98]

Septide

Drug Info

[106]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 3 KEGG Pathways

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Measles

Panther Pathway

[+] 1 Panther Pathways

CCKR signaling map ST

Reactome

[+] 1 Reactome Pathways

G alpha (q) signalling events

WikiPathways

[+] 6 WikiPathways

SIDS Susceptibility Pathways

Gastrin-CREB signalling pathway via PKC and MAPK

Spinal Cord Injury

Peptide GPCRs

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.

REF 2

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 3

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009602)

REF 4

2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.

REF 5

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5749).

REF 6

ClinicalTrials.gov (NCT01500213) A Safety and Efficacy Study of Rolapitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Subjects Receiving Highly Emetogenic Chemotherapy. U.S. National Institutes of Health.

REF 7

REF 8

ClinicalTrials.gov (NCT00640159) Tolerability and Efficacy of Switch From Oral Selegiline to Orally Disintegrating Selegiline (Zelapar) in Patients With Parkinson's Disease. U.S. National Institutes of Health.

REF 9

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 10

REF 11

ClinicalTrials.gov (NCT01339260) An Efficacy and Safety Study of Oral Netupitant and Palonosetron for the Prevention of Nausea and Vomiting. U.S. National Institutes of Health.

REF 12

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007429)

REF 13

Dapitant. RPR 100893. Drugs R D. 1999 Dec;2(6):383-4.

REF 14

REF 15

Acute Endothelin-Receptor Inhibition Does Not Attenuate Acetylcholine-Induced Coronary Vasoconstriction in Experimental Hypercholesterolemia. Arteriosclerosis, Thrombosis, and Vascular Biology, 1998.18: 108-113.

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015473)

REF 17

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006197)

REF 19

ClinicalTrials.gov (NCT00804973) Study in Subjects With Acute Migraines Headaches.. U.S. National Institutes of Health.

REF 20

Neurokinin-1-receptor antagonism decreases anxiety and emotional arousal circuit response to noxious visceral distension in women with irritable bowel syndrome: a pilot study. Aliment Pharmacol Ther.2012 Feb;35(3):360-7.

REF 21

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020168)

REF 22

Clinical pipeline report, company report or official report of OPKO Health Inc.

REF 23

ClinicalTrials.gov (NCT00174798) MILADY: A Randomized, Placebo-controlled Safety and Efficacy Trial of SSR240600C in Treatment of Overactive Bladder or Urge Urinary Incontinence.. U.S. National Institutes of Health.

REF 24

The NK1-receptor antagonist TKA731 in painful diabetic neuropathy: a randomised, controlled trial. Eur J Pain. 2006 Aug;10(6):567-71.

REF 25

REF 26

ClinicalTrials.gov (NCT00606697) A Study With GW597599 And GR205171: Potential New Drugs For The Treatment Of Primary Insomnia. U.S. National Institutes of Health.

REF 27

HIV ANTIRETROVIRAL DRUG SUSCEPTIBILITY AND DRUG INTERACTIONS (DIRECTOR: MARK MANAK). The Children's Hospital of Philadelphia.

REF 28

ClinicalTrials.gov (NCT02199899) Safety, Tolerability and Pharmacodynamics of BIIF 1149 BS in Healthy Young Male Volunteers. U.S. National Institutes of Health.

REF 29

ClinicalTrials.gov (NCT01090440) Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy Subjects (MNK112891) in GlaxoSmithKline.

REF 30

REF 31

Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015961)

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004456)

REF 34

Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.

REF 35

REF 36

Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.

REF 37

REF 38

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001455)

REF 39

REF 40

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001953)

REF 41

REF 42

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003930)

REF 43

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021639)

REF 44

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021516)

REF 45

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010524)

REF 46

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014508)

REF 47

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001352)

REF 48

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005872)

REF 49

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009849)

REF 50

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009948)

REF 51

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010564)

REF 52

REF 53

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001969)

REF 54

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005879)

REF 55

Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.

REF 56

Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

REF 57

Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.

REF 58

A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.

REF 59

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004225)

REF 60

Application of LC-NMR to the identification of bulk drug impurities in NK1 antagonist GW597599 (vestipitant). Magn Reson Chem. 2010 Jul;48(7):523-30.

REF 61

NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783-94.

REF 62

REF 63

Clinical pipeline report, company report or official report of OPKO Health, Inc.

REF 64

SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2002 Dec;303(3):1171-9.

REF 65

Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.

REF 66

Neurokinin-1 receptor, a new modulator of lymphangiogenesis in obese-asthma phenotype. Life Sci. 2013 Aug 6;93(4):169-77.

REF 67

Investigation of figopitant and its metabolites in rat tissue by combining whole-body autoradiography with liquid extraction surface analysis mass spectrometry. Drug Metab Dispos. 2012 Mar;40(3):419-25.

REF 68

Pharmacokinetics and central nervous system effects of the novel dual NK1 /NK3 receptor antagonist GSK1144814 in alcohol-intoxicated volunteers.Br J Clin Pharmacol.2013 May;75(5):1328-39.

REF 69

WO patent application no. 2006,0132,05, Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation.

REF 70

The potency of the novel tachykinin receptor antagonist CGP49823 at rat and gerbil motoneurones in vitro. Eur J Pharmacol. 1998 Jan 26;342(2-3):203-8.

REF 71

Dual tachykinin NK1/NK2 antagonist DNK333 inhibits neurokinin A-induced bronchoconstriction in asthma patients. Eur Respir J. 2004 Jan;23(1):76-81.

REF 72

Targeting pain-depressed behaviors in preclinical assays of pain and analgesia: drug effects on acetic acid-depressed locomotor activity in ICR mice. Life Sci. 2009 Aug 12;85(7-8):309-15.

REF 73

Effects of FK224, a novel compound NK1 and NK2 receptor antagonist, on airway constriction and airway edema induced by neurokinins and sensory nerv... J Pharmacol Exp Ther. 1992 Jul;262(1):403-8.

REF 74

FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity. J Pharmacol Exp Ther. 1992 Jul;262(1):398-402.

REF 75

[Discovery and pharmacological properties of selective neurokinin-receptor antagonists, FK224 and FK888].Nihon Yakurigaku Zasshi.1995 Sep;106(3):193-204.

REF 76

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