WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/10/14 17:28:13」(JST)
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tachykinin receptor 1 |
Identifiers |
Symbol |
TACR1 |
Alt. symbols |
TAC1R |
Entrez |
6869 |
HUGO |
11526 |
OMIM |
162323 |
RefSeq |
NM_001058 |
UniProt |
P25103 |
Other data |
Locus |
Chr. 2 p13.1-p12 |
tachykinin receptor 2 |
Identifiers |
Symbol |
TACR2 |
Alt. symbols |
TAC2R, NKNAR |
Entrez |
6865 |
HUGO |
11527 |
OMIM |
162321 |
RefSeq |
NM_001057 |
UniProt |
P21452 |
Other data |
Locus |
Chr. 10 q11-q21 |
tachykinin receptor 3 |
Identifiers |
Symbol |
TACR3 |
Entrez |
6870 |
HUGO |
11528 |
OMIM |
162332 |
RefSeq |
NM_001059 |
UniProt |
P29371 |
Other data |
Locus |
Chr. 4 q25 |
There are three known mammalian tachykinin receptors termed NK1, NK2 and NK3. All are members of the 7 transmembrane G-protein coupled receptor family and induce the activation of phospholipase C, producing inositol triphosphate (so called Gq-coupled).
Contents
- 1 Binding
- 2 See also
- 3 References
- 4 External links
Binding
The genes and receptor ligands are as follows:[1]
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)
See also
- Substance P
- G protein coupled receptors
References
- ^ Maggi CA (1995). "The mammalian tachykinin receptors". Gen. Pharmacol. 26 (5): 911–44. doi:10.1016/0306-3623(94)00292-U. PMID 7557266.
External links
- "Tachykinin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Tachykinin Receptor at the US National Library of Medicine Medical Subject Headings (MeSH)
Neuropeptide receptors
|
|
G protein-coupled receptor |
Hormone receptors |
Hypothalamic |
- CRH
- FSH
- LHRH
- TRH
- Somatostatin
|
|
Pituitary |
- Vasopressin
- Oxytocin
- LHCG
- TSH
|
|
Other |
- Atrial natriuretic factor
- Calcitonin
- Cholecystokinin
- VIP
|
|
|
Opioid receptors |
- Delta
- Kappa
- Mu
- Nociceptin
|
|
Other neuropeptide receptors |
- Angiotensin
- Bradykinin
- Tachykinin
- Calcitonin gene-related peptide
- Galanin
- GPCR neuropeptide
- Neurotensin
|
|
|
Type I cytokine receptor |
|
|
Enzyme-linked receptor |
- Atrial natriuretic factor
|
|
Other |
|
|
Index of signal transduction
|
|
Description |
- Intercellular
- neuropeptides
- growth factors
- cytokines
- hormones
- Cell surface receptors
- ligand-gated
- enzyme-linked
- G protein-coupled
- immunoglobulin superfamily
- integrins
- neuropeptide
- growth factor
- cytokine
- Intracellular
- adaptor proteins
- GTP-binding
- MAP kinase
- Calcium signaling
- Lipid signaling
- Pathways
- hedgehog
- Wnt
- TGF beta
- MAPK ERK
- notch
- JAK-STAT
- apoptosis
- hippo
- TLR
|
|
|
Neuropeptidergics
|
|
CGRP |
- Agonists: Amylin
- CGRP
- Pramlintide
- Antagonists: BI 44370 TA
- BMS-927711
- CGRP (8-37)
- MK-3207
- Olcegepant
- Rimegepant
- SB-268262
- Telcagepant
- Ubrogepant
|
|
Cholecystokinin |
CCKA
|
- Agonists: Cholecystokinin
- CCK-4
- Antagonists: Amiglumide
- Asperlicin
- Devazepide
- Dexloxiglumide
- Lintitript
- Lorglumide
- Loxiglumide
- Pranazepide
- Proglumide
- Tarazepide
- Tomoglumide
|
|
CCKB
|
- Agonists: Cholecystokinin
- CCK-4
- Gastrin
- Antagonists: CI-988 (PD-134,308)
- Itriglumide
- L-365,360
- Netazepide
- Proglumide
- Spiroglumide
|
|
Unsorted
|
- Antagonists: Nastorazepide
|
|
|
CRH |
CRF1
|
- Agonists: Cortagine
- Corticorelin
- Corticotropin releasing hormone
- Sauvagine
- Stressin I
- Urocortin
- Antagonists: Antalarmin
- Astressin-B
- CP-154,526
- Emicerfont
- Hypericin
- LWH-234
- NBI-27914
- Pexacerfont
- R-121,919
- TS-041
- Verucerfont
|
|
CRF2
|
- Agonists: Corticorelin
- Corticotropin releasing hormone
- Sauvagine
- Urocortin
|
|
|
Galanin |
GAL1
|
- Agonists: Galanin
- Galanin (1-15)
- Galanin-like peptide
- Galmic
- Galnon
- Antagonists: C7
- Dithiepine-1,1,4,4-tetroxide
- Galantide (M15)
- M32
- M35
- M40
- SCH-202596
|
|
GAL2
|
- Agonists: Galanin
- Galanin (1-15)
- Galanin (2-11)
- Galanin-like peptide
- Galmic
- Galnon
- J18
- Antagonists: C7
- Galantide (M15)
- M32
- M35
- M40
- M871
|
|
GAL3
|
- Agonists: Galanin
- Galanin (1-15)
- Galmic
- Galnon
- Antagonists: C7
- Galantide (M15)
- GalR3ant
- HT-2157
- M32
- M35
- M40
- SNAP-37889
- SNAP-398299
|
|
|
Ghrelin/GHS |
- Agonists: Adenosine
- Alexamorelin
- Anamorelin
- Capromorelin
- CP-464709
- Cortistatin-14
- Examorelin (hexarelin)
- Ghrelin (lenomorelin)
- GHRP-1
- GHRP-3
- GHRP-4
- GHRP-5
- GHRP-6
- Ibutamoren (MK-677)
- Ipamorelin
- L-692,585
- LY-426410
- LY-444711
- Macimorelin
- Pralmorelin (GHRP-2)
- Relamorelin
- SM-130,686
- Tabimorelin
- Ulimorelin
- Antagonists: A-778,193
- Cortistatin-8
- (D-Lys3)-GHRP-6
- YIL-781
|
|
MCH |
MCH1
|
- Agonists: Melanin concentrating hormone
- Antagonists: ATC-0065
- ATC-0175
- GW-803,430
- NGD-4715
- SNAP-7941
- SNAP-94847
|
|
MCH2
|
- Agonists: Melanin concentrating hormone
|
|
|
Melanocortin |
MC1
|
- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- BMS-470,539
- Bremelanotide
- HS-014
- HS-024
- Melanotan II
- Modimelanotide
- PL-8177
- SHU-8914
- SHU-9005
- SHU-9119
- SNAP-7941
|
|
MC2
|
- Agonists: ACTH (corticotropin)
- Alsactide
- Codactide
- Giractide
- Norleusactide (pentacosactride)
- Seractide
- Tetracosactide (tetracosactrin, cosyntropin)
- Tosactide (octacosactrin)
- Tricosactide
- Tridecactide
|
|
MC3
|
- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- Bremelanotide
- Melanotan II
- Modimelanotide
- PG-931
- Antagonists: AGRP
- ASIP
- HS-014
- ML-00253764
- PG-106
- SHU-8914
- SHU-9005
- SHU-9119
|
|
MC4
|
- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- AZD2820
- BIM-22493
- Bremelanotide
- LY-2112688
- Melanotan II
- MK-0493
- Modimelanotide
- PF-00446687
- PG-931
- PL-6983
- Ro 27-3225
- Setmelanotide
- THIQ
- Antagonists: AGRP
- ASIP
- HS-014
- HS-024
- HS-131
- JKC-363
- MCL-0020
- MCL-0042
- MCL-0129
- ML-00253764
- MPB-10
- SHU-8914
- SHU-9005
- SHU-9119
|
|
MC5
|
- Agonists: α-MSH
- β-MSH
- γ-MSH
- ACTH (corticotropin)
- Afamelanotide
- Bremelanotide
- HS-014
- HS-024
- Melanotan II
- Modimelanotide
- SHU-8914
- SHU-9005
- SHU-9119
- Antagonists: ASIP
- ML-00253764
|
|
Unsorted
|
- Agonists: Alsactide
- Codactide
- Giractide
- Norleusactide (pentacosactride)
- Seractide
- Tetracosactide (tetracosactrin, cosyntropin)
- Tosactide (octacosactrin)
- Tricosactide
- Tridecactide
|
|
|
Neuropeptide S |
|
|
Neuropeptide Y |
Y1
|
- Agonists: Neuropeptide Y
- Peptide YY
- Antagonists: BIBO-3304
- BIBP-3226
- BVD-10
- GR-231,118
- PD-160,170
|
|
Y2
|
- Agonists: 2-Thiouridine 5'-triphosphate
- Neuropeptide Y
- Neuropeptide Y (13-36)
- Peptide YY
- Peptide YY (3-36)
- Antagonists: BIIE-0246
- JNJ-5207787
- SF-11
|
|
Y4
|
- Agonists: GR-231,118
- Neuropeptide Y
- Pancreatic polypeptide
- Peptide YY
|
|
Y5
|
- Agonists: BWX-46
- Neuropeptide Y
- Peptide YY
- Antagonists: CGP-71683
- FMS-586
- L-152,804
- Lu AA-33810
- MK-0557
- NTNCB
- Velneperit (S-2367)
|
|
|
Neurotensin |
NTS1
|
- Agonists: Neurotensin
- Neuromedin N
- Antagonists: Meclinertant
- SR-142,948
|
|
NTS2
|
- Antagonists: Levocabastine
- SR-142,948
|
|
|
Opioid |
See here instead.
|
|
Orexin |
OX1
|
- Agonists: Orexin-A
- Orexin-B
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- Filorexant
- Lemborexant
- SB-334,867
- SB-408,124
- SB-649,868
- Suvorexant
- TCS-1102
|
|
OX2
|
- Agonists: Orexin-A
- Orexin-B
- SB-668,875
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- EMPA
- Filorexant
- JNJ-10397049
- JNJ-42847922
- Lemborexant
- MK-1064
- SB-649,868
- Suvorexant
- TCS-1102
- TCS-OX2-29
|
|
|
Oxytocin |
- Agonists: Aspartocin
- Carbetocin
- Cargutocin
- Demoxytocin
- Lipo-oxytocin-1
- Merotocin
- Nacartocin
- Oxytocin
- TC OT 39
- TGOT
- Vasotocin (argiprestocin)
- WAY-267,464
- Antagonists: Atosiban
- Barusiban
- Epelsiban
- Erlosiban
- L-368,899
- L-371,257
- L-372,662
- OBE001
- Retosiban
- SSR-126,768
- Tocinoic acid
- WAY-162,720
- Metabolism inhibitors: Amastatin
- Bestatin (ubenimex)
- EDTA
- L-Methionine
- Leupeptin
- o-Phenanthroline
- Phosphoramidon
- Puromycin
|
|
Tachykinin |
NK1
|
- Antagonists: Aprepitant
- Befetupitant
- Burapitant
- Casopitant
- CI-1021
- CP-96,345
- CP-99,994
- CP-122,721
- Dapitant
- Ezlopitant
- Figopitant
- FK-888
- Fosaprepitant
- Fosnetupitant
- GR-203,040
- GW-597,599
- HSP-117
- L-733,060
- L-741,671
- L-743,310
- L-758,298
- Lanepitant
- LY-306,740
- Maropitant
- Netupitant
- NKP-608
- Nolpitantium besilate
- Orvepitant
- Rolapitant
- RP-67,580
- SDZ NKT 343
- Serlopitant
- Telmapitant
- Tradipitant
- Vestipitant
- Vofopitant
|
|
NK2
|
- Antagonists: GR-159,897
- Ibodutant
- Nepadutant
- Saredutant
|
|
NK3
|
- Antagonists: Osanetant
- Talnetant
|
|
|
Vasopressin |
V1A
|
- Agonists: Felypressin
- Lypressin
- Ornipressin
- Selepressin
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: Atosiban
- Conivaptan
- FR-218944
- JNJ-17079166
- JNJ-17308616
- LY-307174
- PF-184563
- Relcovaptan
- RG7314
- SRX246
- SRX251
- TC OT 39
- WAY-267,464
- YM-218
- YM-471
- YM-35471
|
|
V1B
|
- Agonists: Desmopressin
- Felypressin
- Lypressin
- Ornipressin
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: ABT-436
- Nelivaptan
- ORG-52186
|
|
V2
|
- Agonists: Desmopressin
- Felypressin
- Lypressin
- Ornipressin
- TC OT 39
- Terlipressin
- Vasopressin (argipressin)
- Vasotocin (argiprestocin)
- Antagonists: Conivaptan
- JNJ-17079166
- Lixivaptan
- Mozavaptan
- RWJ-351647
- Satavaptan
- Tolvaptan
- YM-471
- YM-35471
|
|
Unsorted
|
- Antagonists: Ribuvaptan
- RWJ-339489
- VMAX-367
- VMAX-372
- VMAX-382
- YM-222546
|
|
|
See also: Peptidergics
|
|
UpToDate Contents
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English Journal
- Remarkable similarities between the hemichordate (Saccoglossus kowalevskii) and vertebrate GPCR repertoire.
- Krishnan A, Almén MS, Fredriksson R, Schiöth HB.SourceDepartment of Neuroscience, Functional Pharmacology, Uppsala University, BMC, Box 593, 751 24 Uppsala, Sweden. Electronic address: arunkumar.krishnan@neuro.uu.se.
- Gene.Gene.2013 Sep 10;526(2):122-33. doi: 10.1016/j.gene.2013.05.005. Epub 2013 May 15.
- Saccoglossus kowalevskii (the acorn worm) is a hemichordate belonging to the superphylum of deuterostome bilateral animals. Hemichordates are sister group to echinoderms, and closely related to chordates. S. kowalevskii has chordate like morphological traits and serves as an important model organism
- PMID 23685280
- The neurokinin-3 receptor (NK3R) antagonist SB222200 prevents the apomorphine-evoked surface but not nuclear NK3R redistribution in dopaminergic neurons of the rat ventral tegmental area.
- Hether S, Misono K, Lessard A.SourceMaryland Psychiatric Research Center, University of Maryland School of Medicine, Baltimore, MD 21228, United States.
- Neuroscience.Neuroscience.2013 Sep 5;247:12-24. doi: 10.1016/j.neuroscience.2013.05.006. Epub 2013 May 11.
- Schizophrenia is a severe condition that has been associated with functional abnormalities in dopaminergic (DA) neurons of the ventral tegmental area (VTA). Neurokinin-3 receptors (NK3Rs) of the tachykinin family of neuropeptides modulate the activity of VTA DA neurons and might be involved in DA ab
- PMID 23673279
- Hypothalamic expression of mutant huntingtin contributes to the development of depressive-like behavior in the BAC transgenic mouse model of Huntington's disease.
- Hult Lundh S, Nilsson N, Soylu R, Kirik D, Petersén A.AbstractPsychiatric symptoms such as depression and anxiety are important clinical features of Huntington's disease (HD). However, the underlying neurobiological substrate for the psychiatric features is not fully understood. In order to explore the biological origin of depression and anxiety in HD, we used a mouse model that expresses the human full-length mutant huntingtin, the BACHD mouse. We found that the BACHD mice displayed depressive- and anxiety-like features as early as at 2 months of age as assessed using the Porsolt forced swim test (FST), the sucrose preference test and the elevated plus maze (EPM). BACHD mice subjected to chronic treatment with the anti-depressant sertraline were not different to vehicle-treated BACHD mice in the FST and EPM. The behavioral manifestations occurred in the absence of reduced hippocampal cell proliferation/neurogenesis or upregulation of the hypothalamic-pituitary-adrenal axis. However, alterations in anxiety- and depression-regulating genes were present in the hypothalamus of BACHD mice including reduced mRNA expression of neuropeptide Y, tachykinin receptor 3 and vesicular monoamine transporter type 2 as well as increased expression of cocaine and amphetamine regulated transcript. Interestingly, the orexin neuronal population in the hypothalamus was increased and showed cellular atrophy in old BACHD mice. Furthermore, inactivation of mutant huntingtin in a subset of the hypothalamic neurons prevented the development of the depressive features. Taken together, our data demonstrate that the BACHD mouse recapitulates clinical HD with early psychiatric aspects and point to the role of hypothalamic dysfunction in the development of depression and anxiety in the disease.
- Human molecular genetics.Hum Mol Genet.2013 Sep 1;22(17):3485-97. doi: 10.1093/hmg/ddt203. Epub 2013 May 22.
- Psychiatric symptoms such as depression and anxiety are important clinical features of Huntington's disease (HD). However, the underlying neurobiological substrate for the psychiatric features is not fully understood. In order to explore the biological origin of depression and anxiety in HD, we used
- PMID 23697793
Japanese Journal
- Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
- Misu Ryosuke,Noguchi Taro,Ohno Hiroaki,Oishi Shinya,Fujii Nobutaka
- Bioorganic & medicinal chemistry 21(8), 2413-2417, 2013-04-15
- … Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). … NKB with the consensus sequence of the tachykinin peptide family also binds to other tachykinin receptors [neurokinin-1 receptor (NK1R) and neurokinin-2 receptor (NK2R)] with low selectivity. …
- NAID 120005244454
- Pharmacological Properties of FK886, a New, Centrally Active Neurokinin-1 Receptor Antagonist
- Yoshino-Furukawa Takako,Maeda Yasue,Kikuchi Aya [他],Sakuma Hiroyuki,Imazumi Katsunori,Yamakuni Hisashi,Sogabe Hajime,Matsuo Masahiko,Manda Toshitaka,Uchida Wataru
- Biological and Pharmaceutical Bulletin 36(1), 76-81, 2013
- … The pharmacological properties of the novel neurokinin-1 (NK1) receptor antagonist FK886, ([3,5-bis(trifluoromethyl)phenyl][(2R)-2-(3-hydroxy-4-methylbenzyl)-4-{2-[(2S)-2-(methoxymethyl)morpholin-4-yl]ethyl}piperazin-1-yl]methanone dihydrochloride), were studied. … It also possessed high affinities for dog, ferret, gerbil and guinea pig NK1 receptors, but not for rat NK1 receptor. …
- NAID 130003361350
- ドラッグライクテンプレートの開発研究 : 新規ニューロキニン-3 受容体選択的アゴニストの開発を目的としたタキキニン類ペプチドの構造活性相関研究
Related Links
- ^Takeda Y, Chou KB, Takeda J, Sachais BS, Krause JE (1991). "Molecular cloning, structural characterization and functional expression of the human substance P receptor". Biochem. Biophys. Res. Commun. 179 (3): 1232–1240. doi: ...
- This gene belongs to a gene family of tachykinin receptors. These tachykinin receptors are characterized by interactions with G proteins and contain seven hydrophobic transmembrane regions. This gene encodes the ...
Related Pictures
★リンクテーブル★
[★]
- 英
- tachykinin receptor
- 関
- タキキニンレセプター
[★]
- 英
- tachykinin receptor
- 関
- タキキニン受容体
[★]
タキキニン、タヒキニン