WordNet
- the secretion of an endocrine gland that is transmitted by the blood to the tissue on which it has a specific effect (同)endocrine, internal_secretion
- insoluble pigments that account for the color of e.g. skin and scales and feathers
PrepTutorEJDIC
- ホルモン
- メラニン(皮膚・毛髪などに見られる黒色色素)
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/07/30 11:28:41」(JST)
[Wiki en表示]
Melanin-concentrating hormone |
Identifiers |
Symbol |
PMCH |
CAS number |
67382-96-1 |
Entrez |
5367 |
HUGO |
9109 |
OMIM |
176795 |
RefSeq |
NM_002674 |
UniProt |
P20382 |
Other data |
Locus |
Chr. 12 q23.2 |
Melanin-concentrating hormone (MCH) is a cyclic 19-amino acid orexigenic hypothalamic peptide originally isolated from the pituitary gland of teleost fish where it controls skin pigmentation.
In mammals it is involved in the regulation of feeding behavior, mood, sleep-wake cycle[1] and energy balance. MCH expressing neurons are located within the lateral hypothalamus and zona incerta. Despite this restricted distribution MCH neurons project widely throughout the brain. MCH knockout mice are hypophagic (eat less) and are lean. When administered centrally it increases food intake and weight gain.
See also
- Melanin-concentrating hormone receptor (MCHR)
References
- ^ Verret L, Goutagny R, Fort P, Cagnon L, Salvert D, Léger L, Boissard R, Salin P, Peyron C, Luppi PH. (2003). "A role of melanin-concentrating hormone producing neurons in the central regulation of paradoxical sleep". BMC Neurosci 4 (19). doi:10.1186/1471-2202-4-19. PMID 12964948.
|
This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (August 2012) |
External links
- Melanin-concentrating hormone at the US National Library of Medicine Medical Subject Headings (MeSH)
- Endocrine system:
- hormones
- Peptide hormones
- Steroid hormones
|
|
Endocrine
glands |
Hypothalamic-
pituitary
|
Hypothalamus
|
- GnRH
- TRH
- Dopamine
- CRH
- GHRH/Somatostatin
- Melanin concentrating hormone
|
|
Posterior pituitary
|
|
|
Anterior pituitary
|
- α
- FSH
- FSHB
- LH
- LHB
- TSH
- TSHB
- CGA
- Prolactin
- POMC
- CLIP
- ACTH
- MSH
- Endorphins
- Lipotropin
- GH
|
|
|
Adrenal axis
|
Adrenal cortex:
|
- aldosterone
- cortisol
- DHEA
|
|
Adrenal medulla:
|
- epinephrine
- norepinephrine
|
|
|
Thyroid axis
|
Thyroid:
|
- thyroid hormone
- calcitonin
|
|
Parathyroid:
|
|
|
|
Gonadal axis
|
Testis::
|
|
|
Ovary:
|
- estradiol
- progesterone
- activin and inhibin
- relaxin (pregnancy)
|
|
Placenta:
|
- hCG
- HPL
- estrogen
- progesterone
|
|
|
Islet-Acinar
Axis
|
Pancreas:
|
- glucagon
- insulin
- amylin
- somatostatin
- pancreatic polypeptide
|
|
|
Pineal gland
|
|
|
|
Other
glands |
Thymus:
|
- Thymosins
- Thymosin α1
- Beta thymosins
- Thymopoietin
- Thymulin
|
|
Digestive system:
|
Stomach:
|
|
|
Duodenum:
|
- CCK
- Incretins
- secretin
- motilin
- VIP
|
|
Ileum:
|
- enteroglucagon
- peptide YY
|
|
Liver/other
|
- Insulin-like growth factor
|
|
|
Adipose tissue:
|
- leptin
- adiponectin
- resistin
|
|
Skeleton::
|
|
|
Kidney:
|
- JGA (renin)
- peritubular cells
- calcitriol
- prostaglandin
|
|
Heart:
|
|
|
|
|
|
noco (d)/cong/tumr, sysi/epon
|
proc, drug (A10/H1/H2/H3/H5)
|
|
|
|
Neuropeptidergics
|
|
Cholecystokinin |
CCKA
|
- Agonists: Cholecystokinin
- CCK-4
Antagonists: Asperlicin
- Proglumide
- Lorglumide
- Devazepide
- Dexloxiglumide
|
|
CCKB
|
- Agonists: Cholecystokinin
- CCK-4
- Gastrin
Antagonists: Proglumide
- CI-988
|
|
|
CRH |
CRF1
|
- Agonists: Corticotropin releasing hormone
Antagonists: Antalarmin
- CP-154,526
- Pexacerfont
|
|
CRF2
|
- Agonists: Corticotropin releasing hormone
|
|
|
Galanin |
GAL1
|
- Agonists: Galanin
- Galanin-like peptide
- Galmic
- Galnon
|
|
GAL2
|
- Agonists: Galanin
- Galanin-like peptide
- Galmic
- Galnon
|
|
GAL3
|
- Agonists: Galanin
- Galmic
- Galnon
|
|
|
Ghrelin |
- Agonists: Ghrelin
- Capromorelin
- MK-677
- Sermorelin
- SM-130,686
- Tabimorelin
|
|
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
|
|
MCH2
|
- Agonists: Melanin concentrating hormone
|
|
|
Melanocortin |
MC1
|
- Agonists: alpha-MSH
- Afamelanotide
- BMS-470,539
- Bremelanotide
- Melanotan II
Antagonists: Agouti signalling peptide
|
|
MC2
|
- Agonists: ACTH
- Cosyntropin
- Tetracosactide
|
|
MC3
|
- Agonists: alpha-MSH
- Bremelanotide
- Melanotan II
|
|
MC4
|
- Agonists: alpha-MSH
- Bremelanotide
- Melanotan II
- PF-00446687
- THIQ
Antagonists: Agouti-related peptide
|
|
MC5
|
- Agonists: alpha-MSH
- Melanotan II
|
|
|
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
|
|
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
|
|
|
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
|
|
NK2
|
- Agonists: Neurokinin A
Antagonists: GR-159,897
- Ibodutant
- Saredutant
|
|
NK3
|
- Agonists: Neurokinin B
Antagonists: Osanetant
- Talnetant
|
|
|
Vasopressin |
V1A
|
- Agonists: Desmopressin
- Felypressin
- Ornipressin
- Terlipressin
- Vasopressin
Antagonists: Conivaptan
- Demeclocycline
- Relcovaptan
|
|
V1B
|
- Agonists: Felypressin
- Ornipressin
- Terlipressin
- Vasopressin
Antagonists: Demeclocycline
- Nelivaptan
|
|
V2
|
- Agonists: Desmopressin
- Ornipressin
- Vasopressin
Antagonists: Conivaptan
- Demeclocycline
- Lixivaptan
- Mozavaptan
- Satavaptan
- Tolvaptan
|
|
|
Orexigenics (A15)
|
|
Exogenous |
- Amitriptyline
- Clonidine
- Cyproheptadine
- Dexamethasone
- Dronabinol/Tetrahydrocannabinol (Cannabis)
- Medroxyprogesterone acetate
- Megestrol acetate
- Mirtazapine
- Nabilone
- Nandrolone
- Olanzapine
- Omega-3 fatty acid
- Oxandrolone
- Pentoxifylline
- Prednisone
- Sugars
- Testosterone
- Thalidomide
|
|
Endogenous |
- ACTH/Corticotropin
- Adiponectin
- Agouti-related peptide
- Anandamide
- Cortisol/Hydrocortisone
- Cortisone
- Ghrelin
- Melanin-concentrating hormone
- Melatonin
- Neuropeptide Y
- Orexin/Hypocretin
|
|
UpToDate Contents
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English Journal
- Fighting Obesity with a Sugar-Based Library: Discovery of Novel MCH-1R Antagonists by a New Computational-VAST Approach for Exploration of GPCR Binding Sites.
- Heifetz A, Barker O, Verquin GP, Wimmer N, Meutermans W, Pal S, Law RJ, Whittaker M.AbstractObesity is an increasingly common disease. While antagonism of the melanin-concentrating hormone-1 receptor (MCH-1R) has been widely reported as a promising therapeutic avenue for obesity treatment, no MCH-1R antagonists have reached the market. Discovery and optimization of new chemical matter targeting MCH-1R is hindered by reduced HTS success rates and a lack of structural information about the MCH-1R binding site. X-ray crystallography and NMR, the major experimental sources of structural information, are very slow processes for membrane proteins, and are not currently feasible for every GPCR or GPCR-ligand complex. This situation significantly limits the ability of these methods to impact the drug discovery process for GPCR targets in "real-time" and hence there is an urgent need for other practical and cost-efficient alternatives. We present here a conceptually pioneering approach that integrates GPCR modeling with design, synthesis and screening of a diverse library of sugar-based compounds from the VAST technology (Versatile Assembly on Stable Templates), to provide structural insights on the MCH-1R binding site. This approach creates a cost-efficient new avenue for structure-based drug discovery (SBDD) against GPCR targets. In our work, a primary VAST hit was used to construct a high-quality MCH-1R model. Following model validation, a structure-based virtual screen yielded a 14% hit rate and 10 novel chemotypes of potent MCH-1R antagonists, including EOAI3367472 (IC50 = 131 nM) and EOAI3367474 (IC50 = 213 nM).
- Journal of chemical information and modeling.J Chem Inf Model.2013 Apr 16. [Epub ahead of print]
- Obesity is an increasingly common disease. While antagonism of the melanin-concentrating hormone-1 receptor (MCH-1R) has been widely reported as a promising therapeutic avenue for obesity treatment, no MCH-1R antagonists have reached the market. Discovery and optimization of new chemical matter targ
- PMID 23590178
- Lateral hypothalamus as a sensor-regulator in respiratory and metabolic control.
- Burdakov D, Karnani MM, Gonzalez A.SourceKing's College London, MRC Center for Developmental Neurobiology, London, UK; MRC National Institute for Medical Research, London, UK. Electronic address: denis.burdakov@kcl.ac.uk.
- Physiology & behavior.Physiol Behav.2013 Apr 3. pii: S0031-9384(13)00099-1. doi: 10.1016/j.physbeh.2013.03.023. [Epub ahead of print]
- Physiological fluctuations in the levels of hormones, nutrients, and gasses are sensed in parallel by interacting control systems distributed throughout the brain and body. We discuss the logic of this arrangement and the definitions of "sensing"; and then focus on lateral hypothalamic (LH) control
- PMID 23562864
Japanese Journal
- Synthesis and Structure-Activity Relationship of Naphtho[1,2-b]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists
- Lim Chae Jo,Choi Jun Young,Lee Byung Ho [他]
- Chemical and pharmaceutical bulletin 61(12), 1239-1247, 2013-12
- NAID 40019889786
- Developmental changes in melanophores and their asymmetrical responsiveness to melanin-concentrating hormone during metamorphosis in barfin flounder (Verasper moseri).
- Yoshikawa Naoki,Matsuda Taihei,Takahashi Akiyoshi,Tagawa Masatomo
- General and comparative endocrinology 194, 118-123, 2013-09-21
- … In this study, we first assessed the changes in melanophores with development and then investigated their responsiveness to melanin-concentrating hormone (MCH) during metamorphosis. …
- NAID 120005341898
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Related Pictures
★リンクテーブル★
[★]
[★]
- 英
- melanin-concentrating hormone、MCH
- 関
- 平均赤血球血色素量、平均赤血球ヘモグロビン