- 関
- CCK receptor
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
- a gastrointestinal hormone that stimulates the secretion of pancreatic enzymes and the contraction and emptying of the gall bladder; its release is stimulated by the presence of fatty acids and amino acids in the small intestine
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)』「2013/05/21 14:37:05」(JST)
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cholecystokinin A receptor |
Identifiers |
Symbol |
CCKAR |
Entrez |
886 |
HUGO |
1570 |
OMIM |
118444 |
RefSeq |
NM_000730 |
UniProt |
P32238 |
Other data |
Locus |
Chr. 4 p15.2-p15.1 |
cholecystokinin B receptor |
Identifiers |
Symbol |
CCKBR |
Entrez |
887 |
HUGO |
1571 |
OMIM |
118445 |
RefSeq |
NM_176875 |
UniProt |
P32239 |
Other data |
Locus |
Chr. 11 p15.4 |
Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) or gastrin.[1] There are two different subtypes CCKA and CCKB which are ~50% homologous:[2] Various cholecystokinin antagonists have been developed and are used in research, although the only drug of this class that has been widely marketed to date is the anti-ulcer drug proglumide.
protein |
gene |
tissue distribution |
preferred ligand |
function |
CCKA (CCK1) |
CCKAR |
primarily gastrointestinal tract, lesser amounts in the CNS |
sulfated CCK >> nonsulfated CCK ≈ nonsulfated CCK |
stimulation of bicarb secretion, gall bladder emptying and inhibiting gut motility |
CCKB (CCK2) |
CCKBR |
primarily CNS, lesser amounts in the gastrointestinal tract |
gastrin ≈ CCK (receptor does not descriminate between sulfated and nonsulfated peptides) |
regulation of nociception, anxiety, memory and hunger |
References [edit]
- ^ Noble F, Wank SA, Crawley JN, Bradwejn J, Seroogy KB, Hamon M, Roques BP (December 1999). "International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors". Pharmacological Reviews 51 (4): 745–81. PMID 10581329.
- ^ Dufresne M, Seva C, Fourmy D (2006). "Cholecystokinin and gastrin receptors". Physiol. Rev. 86 (3): 805–47. doi:10.1152/physrev.00014.2005. PMID 16816139.
External links [edit]
- Cholecystokinin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
Cell surface receptor: G protein-coupled receptors
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Class A:
Rhodopsin like |
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Class B: Secretin like |
Orphan
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- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
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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)
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|
|
Class C: Metabotropic
glutamate / pheromone |
Taste
|
- TAS1R (1
- 2
- 3)
- 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)
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|
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)
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|
|
Class F:
Frizzled / Smoothened |
Frizzled
|
- Frizzled (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10)
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Smoothened
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|
|
|
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)
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Neuropeptide receptors
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|
G protein-coupled receptor |
Hormone receptors
|
Hypothalamic
|
CRH · FSH · LHRH · TRH · Somatostatin
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Pituitary
|
Vasopressin (1A, 1B, 2) · Oxytocin · LHCG · TSH
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Other
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Atrial natriuretic factor (NPR3) · Calcitonin · Cholecystokinin (A, B) · VIP
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Opioid receptors
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Delta · Kappa · Mu · Nociceptin
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Other neuropeptide receptors
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Angiotensin · Bradykinin (B1, B2) / Tachykinin (TACR1) · Calcitonin gene-related peptide · Galanin · GPCR neuropeptide (B/W, FF, S, Y) · Neurotensin
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Type I cytokine receptor |
GH · Prolactin
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Enzyme-linked receptor |
Atrial natriuretic factor (NPR1, NPR2)
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Other |
Sigma (1, 2)
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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)
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Neuropeptidergics
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Cholecystokinin |
CCKA
|
- Agonists: Cholecystokinin
- CCK-4
Antagonists: Asperlicin
- Proglumide
- Lorglumide
- Devazepide
- Dexloxiglumide
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|
CCKB
|
- Agonists: Cholecystokinin
- CCK-4
- Gastrin
Antagonists: Proglumide
- CI-988
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|
|
CRH |
CRF1
|
- Agonists: Corticotropin releasing hormone
Antagonists: Antalarmin
- CP-154,526
- Pexacerfont
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CRF2
|
- Agonists: Corticotropin releasing hormone
|
|
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Galanin |
GAL1
|
- Agonists: Galanin
- Galanin-like peptide
- Galmic
- Galnon
|
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GAL2
|
- Agonists: Galanin
- Galanin-like peptide
- Galmic
- Galnon
|
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GAL3
|
- Agonists: Galanin
- Galmic
- Galnon
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|
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Ghrelin |
- Agonists: Ghrelin
- Capromorelin
- MK-677
- Sermorelin
- SM-130,686
- Tabimorelin
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GnRH |
- Agonists: Buserelin
- Deslorelin
- GnRH
- Goserelin
- Histrelin
- Leuprorelin
- Nafarelin
- Triptorelin
Antagonists: Abarelix
- Cetrorelix
- Degarelix
- Ganirelix
|
|
MCH |
MCH1
|
- Agonists: Melanin concentrating hormone
Antagonists: ATC-0175
- GW-803,430
- NGD-4715
- SNAP-7941
- SNAP-94847
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MCH2
|
- Agonists: Melanin concentrating hormone
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|
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Melanocortin |
MC1
|
- Agonists: alpha-MSH
- Afamelanotide
- BMS-470,539
- Bremelanotide
- Melanotan II
Antagonists: Agouti signalling peptide
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MC2
|
- Agonists: ACTH
- Cosyntropin
- Tetracosactide
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MC3
|
- Agonists: alpha-MSH
- Bremelanotide
- Melanotan II
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MC4
|
- Agonists: alpha-MSH
- Bremelanotide
- Melanotan II
- PF-00446687
- THIQ
Antagonists: Agouti-related peptide
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MC5
|
- Agonists: alpha-MSH
- Melanotan II
|
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Neuropeptide S |
- Agonists: Neuropeptide S
Antagonists: SHA-68
|
|
Neuropeptide Y |
Y1
|
- Agonists: Neuropeptide Y
- Peptide YY
Antagonists: BIBP-3226
|
|
Y2
|
- Agonists: Neuropeptide Y
- Peptide YY
Antagonists: BIIE-0246
|
|
Y4
|
- Agonists: Neuropeptide Y
- Pancreatic polypeptide
- Peptide YY
Antagonists: UR-AK49
|
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Y5
|
- Agonists: Neuropeptide Y
- Peptide YY
Antagonists: Lu AA-33810
|
|
|
Neurotensin |
NTS1
|
- Agonists: Neurotensin
- Neuromedin N
Antagonists: SR-48692
- SR-142,948
|
|
NTS2
|
- Agonists: Neurotensin
Antagonists: Levocabastine
- SR-142,948
|
|
|
Orexin |
OX1
|
- Agonists: Orexin-A
Antagonists: Almorexant
- SB-334,867
- SB-408,124
- SB-649,868
- Suvorexant
|
|
OX2
|
- Agonists: Orexin-A
Antagonists: Almorexant
- SB-649,868
- Suvorexant
- TCS-OX2-29
|
|
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Oxytocin |
- Agonists: Carbetocin
- Demoxytocin
- Oxytocin
- WAY-267,464
Antagonists: Atosiban
- Epelsiban
- L-371,257
- L-368,899
- Retosiban
|
|
Tachykinin |
NK1
|
- Agonists: Substance P
Antagonists: Aprepitant
- Befetupitant
- Casopitant
- CI-1021
- CP-96,345
- CP-99,994
- CP-122,721
- Dapitant
- Ezlopitant
- FK-888
- Fosaprepitant
- 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
- Orvepitant
- RP-67,580
- SDZ NKT 343
- Vestipitant
- Vofopitant
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NK2
|
- Agonists: Neurokinin A
Antagonists: GR-159,897
- Ibodutant
- Saredutant
|
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NK3
|
- Agonists: Neurokinin B
Antagonists: Osanetant
- Talnetant
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Vasopressin |
V1A
|
- Agonists: Desmopressin
- Felypressin
- Ornipressin
- Terlipressin
- Vasopressin
Antagonists: Conivaptan
- Demeclocycline
- Relcovaptan
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V1B
|
- Agonists: Felypressin
- Ornipressin
- Terlipressin
- Vasopressin
Antagonists: Demeclocycline
- Nelivaptan
|
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V2
|
- Agonists: Desmopressin
- Ornipressin
- Vasopressin
Antagonists: Conivaptan
- Demeclocycline
- Lixivaptan
- Mozavaptan
- Satavaptan
- Tolvaptan
|
|
|
UpToDate Contents
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English Journal
- Behavioral and cortical EEG evaluations confirm the roles of both CCK(A) and CCK(B) receptors in mouse CCK-induced anxiety.
- Li H, Ohta H, Izumi H, Matsuda Y, Seki M, Toda T, Akiyama M, Matsushima Y, Goto Y, Kaga M, Inagaki M.SourceDepartment of Developmental Disorders, National Institute of Mental Health, National Center of Neurology and Psychiatry, 4-1-1 Ogawa Higashi, Kodaira, Tokyo 187-8553, Japan.
- Behavioural brain research.Behav Brain Res.2013 Jan 15;237:325-32. doi: 10.1016/j.bbr.2012.09.051. Epub 2012 Oct 5.
- This study investigated the roles of cholecystokinin (CCK)(A) and CCK(B) receptors on CCK-4-induced anxiety-like behaviors in mice through behavioral and neural evaluations. Anxiety-like behaviors in mice were induced by an intracerebroventricular (i.c.v.) administration of CCK-4, which can bind to
- PMID 23043971
- Neuropeptide regulation of fear and anxiety: Implications of cholecystokinin, endogenous opioids, and neuropeptide Y.
- Bowers ME, Choi DC, Ressler KJ.SourceCenter for Behavioral Neuroscience, Department of Psychiatry and Behavioral Sciences, Emory University, Atlanta, GA, United States.
- Physiology & behavior.Physiol Behav.2012 Dec 5;107(5):699-710. doi: 10.1016/j.physbeh.2012.03.004. Epub 2012 Mar 10.
- The neural circuitry of fear likely underlies anxiety and fear-related disorders such as specific and social phobia, panic disorder, and posttraumatic stress disorder. The primary pharmacological treatments currently utilized for these disorders include benzodiazepines, which act on the GABAergic re
- PMID 22429904
Japanese Journal
- Obesity-Related Mechanism of Food Intake Suppression
- He Junfeng,Wong Siew Sun,Qu Yating,Xie Menzhou
- Journal of brain science 36, 61-80, 2011-03-30
- … Food intake suppression via the peripheral nervous system mainly focuses on cholecystokinin and enterostatin relaying to the central nervous system (CNS). …
- NAID 110008574016
- Pharmacological Evaluation of Analgesic Effects of the Cholecystokinin2 Receptor Antagonist Z-360 in Mouse Models of Formalin- and Cancer-Induced Pain
- Yoshinaga Koji,Horii Takayuki,Hamano Hiroki,Eta Runa,Ozaki Tomoko,Orikawa Yuki,Yoshii Kazuyoshi,Kawabata Yoshihiro,Hori Yuko,Seto Koichi,Takei Mineo,Kuraishi Yasushi
- Biological & Pharmaceutical Bulletin 33(2), 244-248, 2010
- … Z-360, a novel cholecystokinin2 (CCK2) receptor antagonist, has been developed as a therapeutic drug for pancreatic cancer and showed pain relief action in phase Ib/IIa clinical trial. … YF476, another CCK2 receptor antagonist, was without effects at 1 and 10 mg/kg. … In contrast, the CCK1 receptor antagonist devazepide inhibited the nociceptive responses to formalin. …
- NAID 130000156631
Related Links
- 製品名 カタログ番号 DESCRIPTION CITATIONS RANKING CI 988 sc-205244 CI-988 is a selective and effective antagonist of CCK-BR (CCK2, CCK-B) receptors. It is described to block the elevated levels of cytosolic Ca 2+ induced by ...
- This gene encodes a G-protein coupled receptor for gastrin and cholecystokinin (CCK), regulatory peptides of the brain and gastrointestinal tract. This protein is a type B gastrin receptor, which has a high affinity for both ...
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