Melatoninski receptor

Melatoninski receptor 1A
Identifikatori
Simbol	MTNR1A
Entrez	4543
HUGO	7463
OMIM	600665
RefSeq	NM_005958
UniProt	P48039
Ostali podaci
Lokus	Hromozom 4 q35.1

Melatoninski receptor 1B
Identifikatori
Simbol	MTNR1B
Entrez	4544
HUGO	7464
OMIM	600804
RefSeq	NM_005959
UniProt	P49286
Ostali podaci
Lokus	Hromozom 11 q21-q22

Melatoninski receptor je G protein-spregnuti receptor koji vezuje melatonin.^[1]

Tri tipa melatoninskog receptora su bila klonirana. MT₁ (Mel_1A ili MTNR1A) i MT₂ (Mel_1B ili MTNR1B) receptorski tipovi su prisutni kod čoveka i drugih sisara^[2], dok je dodatni melatoninski receptor tipa MT₃ (Mel_1C ili MTNR1C) bio identifikovan kod vodozemaca u ptica.^[3]

Mod izražavanja

Kod sisara su melatoninski receptori nađeni u mozgu i pojedinim perifernim organima. Međutim, postoje znatne varijacije u gustini i lokaciji izražavanja melatoninskih receptora između vrsta.^[4] MT₁ tip je prisutan u pars tuberalis hipofize i suprahiazmatičnom jedru hipotalamusa. MT₂ tip je uglavnom prisutan u retini. MT₃ tip mnogih nižih kičmenjaka je izražen u raznim delovima mozga.^[3]

Selektivni ligandi

Agonisti

Antagonisti

Afobazol
Luzindol - N-acetil-2-benziltriptamin

Reference

^ Reppert, SM (1997). „Melatonin receptors: molecular biology of a new family of G protein-coupled receptors”. J. Biol. Rhythms. 12 (6): 528—31. PMID 9406026. doi:10.1177/074873049701200606.
^ Reppert SM, Weaver DR, Godson C (1996). „Melatonin receptors step into the light: cloning and classification of subtypes”. Trends Pharmacol. Sci. 17 (3): 100—2. PMID 8936344. doi:10.1016/0165-6147(96)10005-5.
^ ^а ^б Sugden D, Davidson K, Hough KA, Teh MT (2004). „Melatonin, melatonin receptors and melanophores: a moving story”. Pigment Cell Res. 17 (5): 454—60. PMID 15357831. doi:10.1111/j.1600-0749.2004.00185.x.
^ Morgan PJ, Barrett P, Howell HE, Helliwell R (1994). „Melatonin receptors: localization, molecular pharmacology and physiological significance”. Neurochem. Int. 24 (2): 101—46. PMID 8161940. doi:10.1016/0197-0186(94)90100-7.
^ Nickelsen, T.; Samel, A.; Vejvoda, M.; Wenzel, J.; Smith, B.; Gerzer, R. (2002). „Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: Results of a placebo-controlled trial”. Chronobiology International. 19 (5): 915—36. PMID 12405554. doi:10.1081/cbi-120014108.

Spoljašnje veze

„Melatonin Receptors”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 07. 03. 2014. г.
Melatonin+Receptors на US National Library of Medicine Medical Subject Headings (MeSH)

Transmembranski receptor: receptori spregnuti s G proteinom

Klasa A: Rodopsinu slični

Neurotransmiter

Adrenergički	α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Purinski	Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
Serotoninski	(svi osim 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Drugi	Acetilholin (M1, M2, M3, M4, M5) • Dopamin (D1, D2, D3, D4, D5) • Histamin (H1, H2, H3, H4) • Melatonin (1A, 1B, 1C) • TAAR (1, 2, 3, 5, 6, 8, 9)

Metaboliti i
signalni molekuli

Eikozanoidni	CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) • Prostaciklin • Tromboksan
Drugi	Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat • Lizofosfatidna kiselina (1, 2, 3, 4, 5, 6) • Lizofosfolipid (1, 2, 3, 4, 5, 6, 7, 8) • Niacin (1, 2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1, 2, 3, 4, 5) • Sukcinat

Peptid

Neuropeptidni

B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5) • Neuromedin (B, U (1, 2)) • Neurotenzin (1, 2)

Drugi

Anafilatoksin (C3a, C5a) • Angiotenzin (1, 2) • Apelin • Bombezin (BRS3, GRPR, NMBR) • Bradikinin (B1, B2) • Hemokin • Holecistokinin (A, B) • Endotelin (A, B) • Formil peptid (1, 2, 3) • FSH • Galanin (1, 2, 3) • GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanokortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Motilin • Opioidni (δ, κ, μ, Nociceptin & ζ, ali ne σ) • Oreksin (1, 2) • Oksitocin • Prokineticin (1, 2) • Prolaktin-oslobađajući peptid • Relaksin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • Tahikinin (1, 2, 3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A, 1B, 2)

Razno

Orfan	GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Drugi	Adrenomedulin • Mirisni • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Proteazom-aktivirani (1, 2, 3, 4) • SREB (1, 2, 3)

Klasa B: Sekretinu slični

Orfan	GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi	Moždano specifični angiogenezni inhibitor (1, 2, 3) • Kadherin (1, 2, 3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1, 2) • EMR (1, 2, 3) • Glukagon (GR, GIPR, GLP1R, GLP2R) • Hormon rasta • PACAPR1 • GPR • Latrofilin (1, 2, 3, ELTD1) • Metuzalemski protein • Paratiroidni hormon (1, 2) • Sekretin • Vazoaktivni intestinalni peptid (1, 2)

Klasa C: Metabotropni
glutamat / feromon

Ukus	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)
Drugi	Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • GPR (156, 158, 179) • RAIG (1, 2, 3, 4) • VNR (1, 2, 3, 5)

Klasa F:
Frizzled / Zaglađeni

Uvojiti	Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Zaglađeni	Zaglađeni

Hipnotici/sedativi (N05C)

GABA_A receptor

Barbiturati

Ultra kratkotrajni	Metoheksital Tiamilal Tiopental
Kratko/srednje trajni	Alobarbital Amobarbital Aprobarbital Butobarbital Pentobarbital Sekobarbital Talbutal
Dugotrajni	Barbital Mefobarbital Fenobarbital
Negrupisani	Ciklobarbital Etalobarbital Heptabarbital Heksobarbital Proksibarbital Reposal Vinilbital Vinbarbital

Benzodiazepini

Kratkotrajni	Brotizolam Cinolazepam Doksefazepam Loprazolam Midazolam Triazolam
Intermedijerno trajni	Estazolam Flunitrazepam Lormetazepam Nimetazepam Temazepam
Dugotrajni	Flurazepam Flutoprazepam Nitrazepam Kvanzepam

Dialkil-fenoli

Nebenzodijazepini

Piperidindioni

Hinazolinoni

Neuroaktivni steroidi

Alfa-2-adrenergički
receptor

Alfa-adrenergički agonisti	4-NEMD Klonidin Deksmedetomidin Lofeksidin Medetomidin Romifidin Tizanidin Ksilazin

Melatoninski receptor

Melatonin	Agomelatin Melatonin Ramelteon Tasimelteon

Histaminski receptor &
Acetilholinski receptor

Antihistamini & Antiholinergici	Amitriptilin Demenhidranat Doksilamin Hidroksizin Difenhidramin Bromodifenhidramin Karbinoksamin Doksepin Esmirtazapin Orfenadrin Mianserin Mirtazapin Finiltoloksamin Propiomazin Pirilamin Skopolamin

5-HT_2A &
α₁- adrenergički

Selektivni 5-HT_2A & α₁-adrenergički antagonisti	Etoperidon Nefozodon Niaprazin Trazodon

GABA_B receptor /
GHB receptor

GHB Tip	1,4-Butandiol Acebuterna keselina GABAB Gama-hidroksibuterna kiselina GBL gama-Balerolakton

Oreksinski receptori

Oreksinski antagonisti	Almoreksant SB-334,867 SB-408,124 SB-649,868 TCS-OX2-29

Drugi receptori/
negrupisani

Aldehidi	Acetilglicinamid hloral hidrat Hloral hidrat Hloralodol Dihloralfenazon Paraldehid Petrihloral
Alkini	Centalun Ethlorvinon Etinamat Heksapropimat Metilpentinol
Karbamati	Meprobamat Karisoprodol Tibamat Metokarbamol Procimat
Drugi	2-Metil-2-butanol Acekarbromal Acetofenon Apronal Bromidi Bromizoval Karbromal Hloralosa Klometiazol Embutramid Etomidat Evoksin Fenadiazol Gaboksadol Loreklezol Mefenoksalon Sulfonmetan Trihloroetanol Triklofos Valerian Valnoktamid

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