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)』「2015/11/16 13:48:51」(JST)
[Wiki en表示]
Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors.
There are five known members of the melanocortin receptor system[1] each with differing specificities for melanocortins:[2][3][4]
- MC1R. MC1R is associated with pigmentation genetics.
- MC2R. MC2R is also known as the ACTH receptor or corticotropin receptor because it is specific for ACTH alone.
- MC3R. MC3R
- MC4R. Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity.[5]
- MC5R. MC5R
These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide,[6] and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones.[7]
Contents
- 1 Selective ligands
- 1.1 Agonists
- 1.2 Antagonists and inverse agonists
- 1.3 Unknown
- 2 References
- 3 External links
Selective ligands
Several selective ligands for the melanocortin receptors are known,[8][9][10][11] and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1,[12] while anorectic and aphrodisiac effects appear to involve both MC3 and MC4.[13] MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.[14][15][16][17]
Agonists
- Non-selective
- α-MSH
- β-MSH
- γ-MSH
- ACTH
- Afamelanotide
- Bremelanotide
- Melanotan II
- Modimelanotide
- Setmelanotide
- MC1-selective
- MC4-selective
- Unknown (but for certain MC2-acting)
Antagonists and inverse agonists
- Non-selective
- Agouti-related peptide
- Agouti signalling peptide
- MC4-selective
- HS-014
- HS-024
- MCL-0042[18]
- MCL-0129[19]
- MPB-10
- SHU-9119 (agonist at MC1 and MC5, antagonist at MC3 and MC4)
Unknown
References
- ^ Melanocortins and the Melanocortin Receptor
- ^ Voisey J, Carroll L, van Daal A (October 2003). "Melanocortins and their receptors and antagonists". Current Drug Targets 4 (7): 586–97. doi:10.2174/1389450033490858. PMID 14535656.
- ^ Hadley ME, Dorr RT (April 2006). "Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization". Peptides 27 (4): 921–30. doi:10.1016/j.peptides.2005.01.029. PMID 16412534.
- ^ Dores RM (April 2009). "Adrenocorticotropic hormone, melanocyte-stimulating hormone, and the melanocortin receptors: revisiting the work of Robert Schwyzer: a thirty-year retrospective". Annals of the New York Academy of Sciences 1163 (1): 93–100. doi:10.1111/j.1749-6632.2009.04434.x. PMID 19456331.
- ^ Farooqi IS, Keogh JM, Yeo GS, Lank EJ, Cheetham T, O'Rahilly S (2003). "Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene". N. Engl. J. Med. 348 (12): 1085–95. doi:10.1056/NEJMoa022050. PMID 12646665.
- ^ Chai B, Pogozheva I, Lai Y, Li J, Neubig R, Mosberg H, Gantz I (2005). "Receptor-antagonist interactions in the complexes of agouti and agouti-related protein with human melanocortin 1 and 4 receptors". Biochemistry 44 (9): 3418–31. doi:10.1021/bi0478704. PMID 15736952.
- ^ Pogozheva I, Chai B, Lomize A, Fong T, Weinberg D, Nargund R, Mulholland M, Gantz I, Mosberg H (2005). "Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists". Biochemistry 44 (34): 11329–41. doi:10.1021/bi0501840. PMC 2532597. PMID 16114870.
- ^ Balse-Srinivasan P, Grieco P, Cai M, Trivedi D, Hruby VJ (November 2003). "Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues". Journal of Medicinal Chemistry 46 (23): 4965–73. doi:10.1021/jm030119t. PMID 14584947.
- ^ Wilson KR, Todorovic A, Proneth B, Haskell-Luevano C (2006). "Overview of endogenous and synthetic melanocortin peptides". Cellular and Molecular Biology (Noisy-le-Grand, France) 52 (2): 3–20. PMID 16914082.
- ^ Hruby VJ, Cai M, Cain JP, Mayorov AV, Dedek MM, Trivedi D (2007). "Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor". Current Topics in Medicinal Chemistry 7 (11): 1107–19. doi:10.2174/156802607780906645. PMC 2274922. PMID 17584128.
- ^ Mayorov AV, Cai M, Palmer ES, Dedek MM, Cain JP, Van Scoy AR, Tan B, Vagner J, Trivedi D, Hruby VJ (January 2008). "Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor". Journal of Medicinal Chemistry 51 (2): 187–95. doi:10.1021/jm070461w. PMC 2587288. PMID 18088090.
- ^ Kadekaro AL, Kanto H, Kavanagh R, Abdel-Malek ZA (June 2003). "Significance of the melanocortin 1 receptor in regulating human melanocyte pigmentation, proliferation, and survival". Annals of the New York Academy of Sciences 994 (1): 359–65. doi:10.1111/j.1749-6632.2003.tb03200.x. PMID 12851336.
- ^ King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H (2007). "Melanocortin receptors, melanotropic peptides and penile erection". Current Topics in Medicinal Chemistry 7 (11): 1098–1106. doi:10.2174/1568026610707011111. PMC 2694735. PMID 17584130.
- ^ Cragnolini AB, Schiöth HB, Scimonelli TN (June 2006). "Anxiety-like behavior induced by IL-1beta is modulated by alpha-MSH through central melanocortin-4 receptors". Peptides 27 (6): 1451–6. doi:10.1016/j.peptides.2005.10.020. PMID 16325304.
- ^ Catania A (July 2008). "Neuroprotective actions of melanocortins: a therapeutic opportunity". Trends in Neurosciences 31 (7): 353–60. doi:10.1016/j.tins.2008.04.002. PMID 18550183.
- ^ Lasaga M, Debeljuk L, Durand D, Scimonelli TN, Caruso C (October 2008). "Role of alpha-melanocyte stimulating hormone and melanocortin 4 receptor in brain inflammation". Peptides 29 (10): 1825–35. doi:10.1016/j.peptides.2008.06.009. PMID 18625277.
- ^ Gonzalez PV, Schiöth HB, Lasaga M, Scimonelli TN (March 2009). "Memory impairment induced by IL-1beta is reversed by alpha-MSH through central melanocortin-4 receptors". Brain, Behavior, and Immunity 23 (6): 817–22. doi:10.1016/j.bbi.2009.03.001. PMID 19275930.
- ^ Chaki S, Oshida Y, Ogawa S, Funakoshi T, Shimazaki T, Okubo T, Nakazato A, Okuyama S (December 2005). "MCL0042: a nonpeptidic MC4 receptor antagonist and serotonin reuptake inhibitor with anxiolytic- and antidepressant-like activity". Pharmacology, Biochemistry, and Behavior 82 (4): 621–6. doi:10.1016/j.pbb.2005.11.001. PMID 16337261.
- ^ Chaki S, Hirota S, Funakoshi T, Suzuki Y, Suetake S, Okubo T, Ishii T, Nakazato A, Okuyama S (February 2003). "Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor". The Journal of Pharmacology and Experimental Therapeutics 304 (2): 818–26. doi:10.1124/jpet.102.044826. PMID 12538838.
External links
- "Melanocortin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Melanocortin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
- Calculated spatial position of melanocortin-4 receptor in the lipid bilayer, inactive state with antagonist and active state with agonist
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 FF |
- Agonists: Neuropeptide AF
- Neuropeptide FF
- Neuropeptide SF (RFRP-1)
- Neuropeptide VF (RFRP-3)
- Antagonists: BIBP-3226
- RF9
|
|
Neuropeptide S |
- Antagonists: ML-154
- SHA-68
|
|
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
- c-Fos expression during the modulation of sexual behavior by an alarm pheromone.
- Kobayashi T, Kiyokawa Y, Arata S, Takeuchi Y, Mori Y.SourceLaboratory of Veterinary Ethology, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan.
- Behavioural brain research.Behav Brain Res.2013 Jan 15;237:230-7. doi: 10.1016/j.bbr.2012.09.042. Epub 2012 Sep 28.
- We previously demonstrated that an alarm pheromone released by male Wistar rats evokes several physiological and behavioral responses in other rats. In addition to these responses, the alarm pheromone increased the number of mounts needed for an ejaculation and decreased the hit rate (number of intr
- PMID 23026375
- Synaptic effects induced by alcohol.
- Lovinger DM, Roberto M.SourceLaboratory for Integrative Neuroscience, NIAAA, 5625 Fishers Lane, Room TS-13A, Rockville, MD 20852, USA. lovindav@mail.nih.gov
- Current topics in behavioral neurosciences.Curr Top Behav Neurosci.2013;13:31-86. doi: 10.1007/7854_2011_143.
- Ethanol (EtOH) has effects on numerous cellular molecular targets, and alterations in synaptic function are prominent among these effects. Acute exposure to EtOH activates or inhibits the function of proteins involved in synaptic transmission, while chronic exposure often produces opposing and/or co
- PMID 21786203
Japanese Journal
- ACTH response to desmopressin in a patient with acromegaly ; Expression of corticotropin-releasing factor, urocortins and vasopressin V1b receptor in GH-producing pituitary adenoma
- ARIHARA Zenei,SAKURAI Kanako,OSAKI Yoshinori,FUKAZAWA Hiroshi,YAMADA Shozo,INOSHITA Naoko,MURAKAMI Osamu,OHBA Koji,TAKAHASHI Kazuhiro
- Endocrine journal 58(12), 1029-1036, 2011-12-01
- NAID 10030392435
- ラット急性ストレス負荷による大腸運動亢進に対する中枢オキシトシンの抑制作用(シンポジウム:脳腸相関と腸管炎症,2010年,第51回日本心身医学会総会ならびに学術講演会(仙台))
- 金子 宏,松永 昌宏,坪井 宏仁 [他],川西 陽子
- 心身医学 51(4), 323-328, 2011-04-01
- … 不安,恐怖などのネガティブ感情やストレスは大腸運動を亢進させる.この作用機序として,ストレスによる中枢corticotropin-releasing factor(CRF)の増加の関与が示されている.われわれは,ラットの水回避ストレスモデルを用いて,ストレス緩和作用をもつオキシトシンの,ストレス負荷時の大腸運動への効果を明らかにすることを試みた.その結果,脳室内へのオキシトシン投与は,ストレスによる大腸運動の亢進,室傍核CRF発現および …
- NAID 110008593581
- L-Ornithine attenuates corticotropin-releasing factor-induced stress responses acting at GABA_A receptors in neonatal
- Kurata Koji,Shigemi Kazutaka,Tomonaga Shozo,Aoki Mami,Morishita Koji,Denbow D. Michael,Furuse Mitsuhiro,古瀬 充宏,クラタ コウジ,シゲミ カズタカ,トモナガ ショウゾウ,アオキ マミ,モリシタ コウジ,フルセ ミツヒロ
- Neuroscience 172, 226-231, 2011-01-13
- … To clarify the mechanism, we conducted three experiments under strengthened stressful conditions with corticotropin-releasing factor (CRF). … with either CRF, CRF plus L-ornithine (0.5 μmol), CRF plus the Y-aminobutyric acid (GABA)_A receptor antagonist picrotoxin or L-ornithine with picrotoxin. …
- NAID 120004951558
Related Links
- ^Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM (March 2003). "International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ...
- MC2R MC2R A gene on chromosome 18p11.2 that encodes ACTH receptor, the activity of which is mediated by G protein-activated adenylate cyclase. Molecular pathology Genetic variations in MC2R cause glucocorticoid deficiency ...
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★リンクテーブル★
[★]
- 英
- corticotropin receptor
- 関
- コルチコトロピンレセプター
[★]
- 英
- corticotropin receptor
- 関
- コルチコトロピン受容体