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
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/06/26 18:49:29」(JST)
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| bradykinin receptor B1 |
| Identifiers |
| Symbol |
BDKRB1 |
| Entrez |
623 |
| HUGO |
1029 |
| OMIM |
600337 |
| RefSeq |
NM_000710 |
| UniProt |
P46663 |
| Other data |
| Locus |
Chr. 14 q32.1-32.2 |
| bradykinin receptor B2 |
| Identifiers |
| Symbol |
BDKRB2 |
| Entrez |
624 |
| HUGO |
1030 |
| OMIM |
113503 |
| RefSeq |
NM_000623 |
| UniProt |
P30411 |
| Other data |
| Locus |
Chr. 14 q32.1-32.2 |
The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin.
There are two Bradykinin receptors: the B1 receptor and the B2 receptor.[1]
|
Contents
- 1 B1 receptor
- 2 B2 receptor
- 3 References
- 4 External links
|
B1 receptor
Main article: bradykinin receptor B1
Bradykinin receptor B1 (B1) is a G-protein coupled receptor encoded by the BDKRB1 gene in humans. Its principal ligand is bradykinin, a 9 amino acid peptide generated in pathophysiologic conditions such as inflammation, trauma, burns, shock, and allergy. The B1 receptor is one of two of G protein-coupled receptors that have been found which bind bradykinin and mediate responses to these pathophysiologic conditions.
B1 protein is synthesized de novo following tissue injury and receptor binding leads to an increase in the cytosolic calcium ion concentration, ultimately resulting in chronic and acute inflammatory responses.
B2 receptor
Main article: bradykinin receptor B2
The B2 receptor is a G protein-coupled receptor, coupled to Gq and Gi. Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. Furthermore, the receptor stimulates the mitogen-activated protein kinase pathways. It is ubiquitously and constitutively expressed in healthy tissues.
The B2 receptor forms a complex with angiotensin converting enzyme (ACE), and this is thought to play a role in cross-talk between the renin-angiotensin system (RAS) and the kinin-kallikrein system (KKS). The heptapeptide angiotensin 1-7 (A1-7) also potentiates bradykinin action on B2 receptors.[2]
Icatibant is a second generation B2 receptor antagonist which has undergone limited clinical trials in pain and inflammation. FR 173657 is another orally active non-peptide B2 antagonist that has undergone limited trials as analgesic and antiinflammatory drug.
Kallidin also signals through the B2 receptor.
References
- ^ Leeb-Lundberg LM, Marceau F, Müller-Esterl W, Pettibone DJ, Zuraw BL (2005). "International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences". Pharmacol. Rev. 57 (1): 27–77. DOI:10.1124/pr.57.1.2. PMID 15734727.
- ^ Fernandes L, Fortes ZB, Nigro D, Tostes RC, Santos RA, Catelli De Carvalho MH (2001). "Potentiation of bradykinin by angiotensin-(1-7) on arterioles of spontaneously hypertensive rats studied in vivo". Hypertension 37 (2 Part 2): 703–9. PMID 11230360. http://hyper.ahajournals.org/cgi/content/abstract/37/2/703.
External links
- "Bradykinin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1330.
- Bradykinin+receptor at the US National Library of Medicine Medical Subject Headings (MeSH)
|
Cell surface receptor: G protein-coupled receptors
|
|
Class A:
Rhodopsin like |
|
|
| Class B: Secretin like |
|
Orphan
|
- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
|
|
|
Other
|
- Brain-specific angiogenesis inhibitor (1
- 2
- 3)
- Cadherin (1
- 2
- 3)
- Calcitonin
- CALCRL
- CD97
- Corticotropin-releasing hormone (1
- 2)
- EMR (1
- 2
- 3)
- Glucagon (GR
- GIPR
- GLP1R
- GLP2R)
- Growth hormone releasing hormone
- PACAPR1
- GPR
- Latrophilin (1
- 2
- 3
- ELTD1)
- Methuselah-like proteins
- Parathyroid hormone (1
- 2)
- Secretin
- Vasoactive intestinal peptide (1
- 2)
|
|
|
Class C: Metabotropic
glutamate / pheromone |
|
Taste
|
- TAS1R (1
- 2
- 3)
- TAS2R (1
- 3
- 4
- 5
- 8
- 9
- 10
- 12
- 13
- 14
- 16
- 19
- 20
- 30
- 31
- 38
- 39
- 40
- 41
- 42
- 43
- 45
- 46
- 50)
|
|
|
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
|
|
|
|
|
B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
|
|
|
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
|
Delta · Kappa · Mu · Nociceptin
|
|
|
Other neuropeptide receptors
|
Angiotensin · Bradykinin (B1, B2) / Tachykinin (TACR1) · Calcitonin gene-related peptide · Galanin · GPCR neuropeptide (B/W, FF, S, Y) · Neurotensin
|
|
|
| Type I cytokine receptor |
GH · Prolactin
|
|
| Enzyme-linked receptor |
Atrial natriuretic factor (NPR1, NPR2)
|
|
| Other |
Sigma (1, 2)
|
|
|
B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
|
|
UpToDate Contents
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English Journal
- Effect of Retro-Inverso Isomer of Bradykinin on Size-Dependent Penetration of Blood-Brain Tumor Barrier.
- Su B1, Wang R1, Xie Z1, Ruan H1, Li J1, Xie C1, Lu W1, Wang J1, Wang D1, Liu M1.
- Small (Weinheim an der Bergstrasse, Germany).Small.2018 Jan 2. doi: 10.1002/smll.201702331. [Epub ahead of print]
- PMID 29292579
- Kinin B1 receptors as a therapeutic target for inflammation.
- Qadri F1, Bader M1,2,3,4,5.
- Expert opinion on therapeutic targets.Expert Opin Ther Targets.2018 Jan;22(1):31-44. doi: 10.1080/14728222.2018.1409724. Epub 2017 Nov 30.
- PMID 29168929
- Ex vivo study of human visceral nociceptors.
- McGuire C1, Boundouki G2, Hockley JRF2, Reed D2, Cibert-Goton V1, Peiris M2, Kung V1, Broad J1, Aziz Q2, Chan C1, Ahmed S1, Thaha MA1, Sanger GJ1, Blackshaw LA2, Knowles CH1, Bulmer DC1.
- Gut.Gut.2018 Jan;67(1):86-96. doi: 10.1136/gutjnl-2016-311629. Epub 2016 Sep 21.
- PMID 27654583
Japanese Journal
- Gangliosides stimulate bradykinin B2 receptors to promote calmodulin kinase ？-mediated neuronal differentiation
- Kanatsu Yoshinori,Chen Nai Hong,Mitoma Junya [他]
- Journal of Biochemistry 152(1), 63-72, 2012-07
- NAID 40019351059
- 小分子プローブによるタンパク質の特異的ラベル化技術の開発
- 王子田 彰夫
- 薬学雑誌 132(2), 195-199, 2012
- … This labeling system, so-called reactive tag system, was successfully applied to the fluorescence imaging of tag-fused GPCRs such as bradykinin receptor (B2R) and acetylcholine receptor (m1AchR) expressing on HEK293 cells. …
- NAID 130001872008
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