コルチコトロピン受容体、コルチコトロピンレセプター

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

[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]

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

BMS-470,539

MC₄-selective

PF-00446687
PL-6983
THIQ

Unknown (but for certain MC₂-acting)

Alsactide
Tetracosactide

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

Semax

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

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. コルチコトロピン-放出ホルモン（CRH）の生理学 physiology of corticotropin releasing hormone
2. 点頭てんかんのマネージメントおよび予後 management and prognosis of infantile spasms
3. コルチコトロピン-放出ホルモン（CRH）刺激試験 corticotropin releasing hormone stimulation test
4. インスリン様成長因子 Iの生理学 physiology of insulin like growth factor i
5. 薬理ゲノム学の概要 overview of pharmacogenomics

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

「コルチコトロピン受容体」

　　[★]

英: corticotropin receptor
関: コルチコトロピンレセプター

「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

[1] Melanocortins and the Melanocortin Receptor

[pmid14535656-2] 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.

[pmid16412534-3] 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.

[pmid19456331-4] 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.

[5] 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.

[6] 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.

[7] 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.

[pmid14584947-8] 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.

[pmid16914082-9] 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.

[pmid17584128-10] 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.

[pmid18088090-11] 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.

[pmid12851336-12] 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.

[pmid17584130-13] 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.

[pmid16325304-14] 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.

[pmid18550183-15] 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.

[pmid18625277-16] 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.

[pmid19275930-17] 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.

[pmid16337261-18] 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.

[pmid12538838-19] 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.

匿名

検索

案内

案内

corticotropin receptor