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There are three knownmammaliantachykinin receptors termed NK₁, NK₂ and NK₃. All are members of the7 transmembrane G-protein coupled receptor family and induce the activation ofphospholipase C, producinginositol triphosphate (so called G_q-coupled).

Inhibitors of NK-1, known asNK-1 receptor antagonists, can be used asantiemetic agents, such as the drugaprepitant.^[1]

Binding

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The genes and receptor ligands are as follows:^[2]

Receptor	Gene	Preferred ligand
NK₁	TACR1	substance P
NK₂	TACR2	neurokinin A
NK₃	TACR3	neurokinin B

(Hökfelt et al., 2001; Page, 2004; Pennefather et al., 2004; Maggi, 2000)

References

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^"Aprepitant".NICE. Retrieved2020-05-10.
^Maggi CA (September 1995). "The mammalian tachykinin receptors".General Pharmacology.26 (5):911–44.doi:10.1016/0306-3623(94)00292-U.PMID 7557266.

External links

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"Tachykinin Receptors".IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Tachykinin+Receptor at the U.S. National Library of MedicineMedical Subject Headings (MeSH)

Cell surface receptor:G protein-coupled receptors

Class A:Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but5-HT3)5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2),EP (1 2 3 4),FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2,GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemerin
- 1
- 2
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin &Zeta, but notSigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	GPR (3 4 6 12 15 17 18 19 20 21 22 26 27 31 32 33 34 35 37 39 42 45 50 52 55 61 62 63 65 68 75 78 82 83 84 85 87 88 101 103 109A 119 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B:Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C:Metabotropic glutamate /pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	Calcium-sensing receptor GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F:Frizzled &Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

Neuropeptide receptors

G protein-coupled receptor

Hormone receptors

Hypothalamic	CRH FSH LHRH TRH Somatostatin
Pituitary	Vasopressin 1A 1B 2 Oxytocin LHCG TSH
Other	Atrial natriuretic factor NPR3 Calcitonin Cholecystokinin A B VIP

Opioid receptors

Other neuropeptide receptors

Type I cytokine receptor

Enzyme-linked receptor

Atrial natriuretic factor
- NPR1
- NPR2

Other

Sigma
- 1
- 2

v t e Neurokinin receptor modulators
NK₁	Agonists:Substance P Antagonists:Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Elinzanetant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists:Neurokinin A Antagonists:GR-159897 Ibodutant Nepadutant Saredutant Otilonium bromide
NK₃	Agonists:Neurokinin B Senktide Antagonists:Elinzanetant Fezolinetant Osanetant Pavinetant SB-218,795 SB-222,200 Talnetant

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Binding

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References

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