Target Information

Target General Infomation
Target ID
T47094
Former ID
TTDS00194
Target Name
Substance-P receptor
Gene Name
TACR1
Synonyms
NK-1 receptor; NK-1R; Neurokinin 1 receptor; SPR; Substance P receptor; Tachykinin 1 receptor; Tachykinin neurokinin 1 receptor; Tachykinin receptor 1; TACR1
Target Type
Successful
Disease Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Asthma [ICD10: J45]
Brain injury [ICD10: S09.90]
Chemotherapy-induced nausea [ICD9: 787, 787.0; ICD10: R11]
Cancer pain [ICD9: 140-229, 338,780; ICD10: R52, G89]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cough [ICD9: 786.2; ICD10: R05]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Depression; Anxiety [ICD9: 300, 311; ICD10: F30-F39, F40-F42]
Depression [ICD9: 311; ICD10: F30-F39]
Eczema [ICD10: L20-L30]
Emesis; Irritable bowel syndrome [ICD9: 564.1, 787; ICD10: K58, R11]
Emesis [ICD9: 787; ICD10: R11]
Irritable bowel syndrome with diarrhoea [ICD9: 493, 564.1, 787.91; ICD10: A09, J45, K58, K59.1]
Irritable bowel syndrome; Chemo therapy induced emesis; Gastric motility disorder [ICD9: 536.8, 564.1, 787; ICD10: K30, K58, R11]
Incontinence; Anxiety disorder; Chemotherapyinduced emesis; Major depressive disorder [ICD9: 296.2, 296.3, 300, 787, 787.6, 788.3; ICD10: F32, F33, F40-F42, N39.3-N39.4]
Influenza virus [ICD10: J11.1]
Migraine [ICD9: 346; ICD10: G43]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Mood disorder [ICD10: F30-F39]
Nausea; Vomiting [ICD9: 787, 787.0; ICD10: R11]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Respiratory tract inflammation [ICD10: J00-J99]
Schizophrenia [ICD9: 295; ICD10: F20]
Severe mood disorders; Depression [ICD9: 296, 311; ICD10: F30-F39, F32]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T47094
UniProt ID
P25103
Sequence
MDNVLPVDSDLSPNISTNTSEPNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAH
KRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVICVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNKIYEKVYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHIFFLLPYINPDLYLKKFIQQVYLAIMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTIST
VVGAHEEEPEDGPKATPSSLDLTSNCSSRSDSKTMTESFSFSSNVLS
Drugs and Mode of Action
Drug(s) Aprepitant Drug Info Approved Nausea; Vomiting [1], [2]
MK-869 Drug Info Approved Depression [3], [4]
Rolapitant Drug Info Approved Chemotherapy-induced nausea [5], [6]
Netupitant Drug Info Phase 3 Chemotherapy-induced nausea [7], [8]
CP-122721 Drug Info Phase 2 Major depressive disorder [9]
DAPITANT Drug Info Phase 2 Pain [10]
GW 597599 Drug Info Phase 2 Mood disorder [11]
LANEPITANT Drug Info Phase 2 Pain [12], [13]
LY-2590443 Drug Info Phase 2 Migraine [14]
LY-686017 Drug Info Phase 2 Alcohol use disorders [15]
NKP 608 Drug Info Phase 2 Mood disorder [16]
Orvepitant Drug Info Phase 2 Depression; Anxiety [17]
SCH-900978 Drug Info Phase 2 Cough [18]
SSR240600 Drug Info Phase 2 Urinary incontinence [19]
TKA-731 Drug Info Phase 2 Pain [20]
VESTIPITANT MESYLATE Drug Info Phase 2 Major depressive disorder [21]
VOFOPITANT HYDROCHLORIDE Drug Info Phase 2 Emesis [22], [23]
CJ-12255 Drug Info Phase 1 Eczema [24]
Figopitant Drug Info Phase 1 Diabetes [25]
Casopitant Drug Info Withdrawn from market Chemotherapy-induced nausea [26], [27]
BL-1832 Drug Info Discontinued in Phase 3 Pain [28]
L-759274 Drug Info Discontinued in Phase 3 Severe mood disorders; Depression [26]
Zunrisa/Rezonic Drug Info Discontinued in Phase 3 Chemotherapy-induced nausea [29]
CGP-49823 Drug Info Discontinued in Phase 2 Pain [30]
CS-003 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [31]
DNK-333 Drug Info Discontinued in Phase 2 Irritable bowel syndrome with diarrhoea [31]
Ezlopitant Drug Info Discontinued in Phase 2 Emesis; Irritable bowel syndrome [32], [33]
FK-224 Drug Info Discontinued in Phase 2 Asthma [34], [35]
FK-888 Drug Info Discontinued in Phase 2 Migraine [36], [37]
GSK 679769 Drug Info Discontinued in Phase 2 Incontinence; Anxiety disorder; Chemotherapyinduced emesis; Major depressive disorder [32]
Nolpitantium besilate Drug Info Discontinued in Phase 2 Asthma [38], [39]
TA-5538 Drug Info Discontinued in Phase 2 Overactive bladder disorder [40]
TAK-637 Drug Info Discontinued in Phase 2 Depression [26]
AVE-5883 Drug Info Discontinued in Phase 1/2 Asthma [41]
GSK1144814 Drug Info Discontinued in Phase 1 Schizophrenia [42]
GSK424887 Drug Info Discontinued in Phase 1 Depression; Anxiety [43]
SDZ-NKT-343 Drug Info Discontinued in Phase 1 Pain [44]
SLV-323 Drug Info Discontinued in Phase 1 Irritable bowel syndrome; Chemo therapy induced emesis; Gastric motility disorder [32]
CI-1021 Drug Info Terminated Discovery agent [45]
CP-96345 Drug Info Terminated Discovery agent [46]
FK-355 Drug Info Terminated Asthma [47]
FR-113680 Drug Info Terminated Asthma [48]
GR-82334 Drug Info Terminated Emesis [49]
L-732138 Drug Info Terminated Discovery agent [50]
L-733060 Drug Info Terminated Discovery agent [51]
L-741671 Drug Info Terminated Emesis [52]
MEN-11149 Drug Info Terminated Asthma [53]
MEN-11467 Drug Info Terminated Respiratory tract inflammation [54]
RP-67580 Drug Info Terminated Pain [55], [56]
WIN-64821 Drug Info Terminated Asthma [57]
Inhibitor (D)-Phe-(D)-Phe-NH2 Drug Info [58]
(D)-Phe-(L)-Phe-NH2 Drug Info [58]
(L)-Phe-(D)-Phe-NH2 Drug Info [58]
2-Phenyl-3-(1-phenyl-ethoxy)-piperidine Drug Info [59]
3,6-Diphenyl-1-oxa-7-aza-spiro[4.5]decane Drug Info [60]
3-Benzyloxy-2-phenyl-piperidine Drug Info [59]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [61]
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 [62]
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 [62]
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 [62]
Ac-Phe-Phe-NH2 Drug Info [58]
Arg-Pro-Lys-Pro-Ala-Gln-Phe-Phe-Gly-Leu-Met-NH2 Drug Info [63]
Arg-Pro-Lys-Pro-Ala-Ser-Phe-Phe-Gly-Leu-Met-NH2 Drug Info [63]
Arg-Pro-Lys-Pro-Gln-Ser-Phe-Phe-Gly-Leu-Met-NH2 Drug Info [63]
CP-96345 Drug Info [64]
ENDOMORPHIN 2 Drug Info [58]
FR-113680 Drug Info [65]
H-Ala-Pro-Phe-Phe-NH2 Drug Info [58]
H-Arg-Pro-Lys-Pro-Gln-Gln-Phe-OH Drug Info [58]
H-Leu-Phe-NH2 Drug Info [58]
H-Phe-NH2 Drug Info [58]
H-Phe-Phe-NH2 Drug Info [58]
H-Pro-Phe-Phe-NH2 Drug Info [58]
H-Tyr(OMe)-Phe(2-Me)-NH2 Drug Info [58]
H-Tyr-Ala-Phe-Phe-NH2 Drug Info [58]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 Drug Info [66]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 Drug Info [66]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Drug Info [66]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 Drug Info [66]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Drug Info [66]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl Drug Info [66]
H-Tyr-Pro-Ala-Phe-NH2 Drug Info [58]
H-Tyr-Pro-Phe-Ala-NH2 Drug Info [58]
H-Tyr-Pro-Phe-Phe-OH Drug Info [58]
L-708568 Drug Info [67]
L-732138 Drug Info [68]
L-733060 Drug Info [59]
L-736281 Drug Info [69]
L-741671 Drug Info [69]
MDL-28163 Drug Info [70]
Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2 Drug Info [63]
R-226161 Drug Info [71]
SP-SAP Drug Info [72]
SPANTIDE Drug Info [73]
Substance P Drug Info [74]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Drug Info [75]
[Sar9,Met(O2)11]-SP Drug Info [76]
Antagonist Aprepitant Drug Info [77]
befetupitant Drug Info [78]
BL-1832 Drug Info [79]
Casopitant Drug Info [26]
CGP-49823 Drug Info [80]
CI-1021 Drug Info [81]
CJ 11,974-01 Drug Info [82]
CJ-12255 Drug Info [83], [4]
CP-100263 Drug Info [32]
CP-122721 Drug Info [84]
CP-99,994 Drug Info [81]
CS-003 Drug Info [31]
DAPITANT Drug Info [85], [4]
Ezlopitant Drug Info [32]
Figopitant Drug Info [86]
FK-355 Drug Info [87]
FK-888 Drug Info [88]
GR-82334 Drug Info [89]
GSK 679769 Drug Info [32]
GSK424887 Drug Info [90]
GW 597599 Drug Info [91]
L-703,606 Drug Info [92]
L-759274 Drug Info [26]
LANEPITANT Drug Info [93], [4]
LY-2590443 Drug Info [72]
LY-686017 Drug Info [94]
MEN-11149 Drug Info [95]
MEN-11467 Drug Info [96]
MK-869 Drug Info [84]
Netupitant Drug Info [97]
NKP 608 Drug Info [16]
Nolpitantium besilate Drug Info [98]
Orvepitant Drug Info [90]
R116031 Drug Info [99]
Rolapitant Drug Info [97]
RP-67580 Drug Info [100]
S-41744 Drug Info [72]
SCH 206272 Drug Info [101]
SCH-900978 Drug Info [102]
SDZ-NKT-343 Drug Info [103]
spantide II Drug Info [104]
SSR240600 Drug Info [105]
T2328 Drug Info [106]
TA-5538 Drug Info [107]
TAK-637 Drug Info [26]
TKA-731 Drug Info [20]
VESTIPITANT MESYLATE Drug Info [91], [4]
VOFOPITANT HYDROCHLORIDE Drug Info [108], [4]
WIN-64821 Drug Info [109]
Zunrisa/Rezonic Drug Info [90]
[125I]L703,606 Drug Info [110]
[18F]SPA-RQ Drug Info [72]
Modulator AVE-5883 Drug Info [111]
DNK-333 Drug Info
EU-C-001 Drug Info [72]
FK-224 Drug Info [87]
GSK1144814 Drug Info
SLV-323 Drug Info [32]
WIN-64745 Drug Info
WIN-66306 Drug Info
WIN-68577 Drug Info
ZD-6021 Drug Info
Agonist eledoisin Drug Info [92]
Homspera Drug Info [72]
kassinin Drug Info [92]
neurokinin A Drug Info [112]
physalaemin Drug Info [92]
Septide Drug Info [113]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Measles
PANTHER Pathway CCKR signaling map ST
Reactome G alpha (q) signalling events
WikiPathways SIDS Susceptibility Pathways
Gastrin-CREB signalling pathway via PKC and MAPK
Spinal Cord Injury
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
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