Melatonin receptor: Difference between revisions

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A '''melatonin receptor''' is a [[G protein-coupled receptor]] (GPCR) which binds [[melatonin]].<ref name="pmid9406026">{{cite journal | authors = Reppert SM | title = Melatonin receptors: molecular biology of a new family of G protein-coupled receptors | journal = J. Biol. Rhythms | volume = 12 | issue = 6 | pages = 528–31 | year = 1997 | pmid = 9406026 | doi = 10.1177/074873049701200606 }}</ref>
A '''melatonin receptor''' is a [[G protein-coupled receptor]] (GPCR) which binds [[melatonin]].<ref name="pmid9406026">{{cite journal | author4 = Reppert SM | title = Melatonin receptors: molecular biology of a new family of G protein-coupled receptors | journal = J. Biol. Rhythms | volume = 12 | issue = 6 | pages = 528–31 | year = 1997 | pmid = 9406026 | doi = 10.1177/074873049701200606 | last1 = Reppert | first1 = S. M. }}</ref>


Three types of melatonin receptor have been [[cloned]]. The MT<sub>1</sub> (or [[melatonin receptor 1A|Mel<sub>1A</sub>]] or MTNR1A) and MT<sub>2</sub> (or [[melatonin receptor 1B|Mel<sub>1B</sub>]] or MTNR1B) receptor subtypes are present in [[human]]s and other [[mammal]]s,<ref name="pmid8936344">{{cite journal | authors = Reppert SM, Weaver DR, Godson C | title = Melatonin receptors step into the light: cloning and classification of subtypes | journal = Trends Pharmacol. Sci. | volume = 17 | issue = 3 | pages = 100–2 | year = 1996 | pmid = 8936344 | doi = 10.1016/0165-6147(96)10005-5 }}</ref> while an additional melatonin receptor subtype MT<sub>3</sub> (or [[melatonin receptor 1C|Mel<sub>1C</sub>]] or MTNR1C) has been identified in [[amphibia]] and [[bird]]s.<ref name="Sugden_2004">{{cite journal | authors = Sugden D, Davidson K, Hough KA, Teh MT | title = Melatonin, melatonin receptors and melanophores: a moving story | journal = Pigment Cell Res. | volume = 17 | issue = 5 | pages = 454–60 | year = 2004 | pmid = 15357831 | doi = 10.1111/j.1600-0749.2004.00185.x }}</ref>
Three types of melatonin receptor have been [[cloned]]. The MT<sub>1</sub> (or [[melatonin receptor 1A|Mel<sub>1A</sub>]] or MTNR1A) and MT<sub>2</sub> (or [[melatonin receptor 1B|Mel<sub>1B</sub>]] or MTNR1B) receptor subtypes are present in [[human]]s and other [[mammal]]s,<ref name="pmid8936344">{{cite journal | author4 = Reppert SM, Weaver DR, Godson C | title = Melatonin receptors step into the light: cloning and classification of subtypes | journal = Trends Pharmacol. Sci. | volume = 17 | issue = 3 | pages = 100–2 | year = 1996 | pmid = 8936344 | doi = 10.1016/0165-6147(96)10005-5 | last1 = Reppart | first1 = Steven M. | last2 = Weaver | first2 = David R. | last3 = Godson | first3 = Catherine }}</ref> while an additional melatonin receptor subtype MT<sub>3</sub> (or [[melatonin receptor 1C|Mel<sub>1C</sub>]] or MTNR1C) has been identified in [[amphibia]] and [[bird]]s.<ref name="Sugden_2004">{{cite journal | author4 = Sugden D, Davidson K, Hough KA, Teh MT | title = Melatonin, melatonin receptors and melanophores: a moving story | journal = Pigment Cell Res. | volume = 17 | issue = 5 | pages = 454–60 | year = 2004 | pmid = 15357831 | doi = 10.1111/j.1600-0749.2004.00185.x | last1 = Sugden | first1 = David | last2 = Davidson | first2 = Kathryn | last3 = Hough | first3 = Kate A. }}</ref>


==Expression patterns==
==Expression patterns==
In mammals, melatonin receptors are found in the [[brain]] and some peripheral organs. However, there is considerable variation in the density and location of MT receptor expression between species.<ref name="pmid8161940">{{cite journal | authors = Morgan PJ, Barrett P, Howell HE, Helliwell R | title = Melatonin receptors: localization, molecular pharmacology and physiological significance | journal = Neurochem. Int. | volume = 24 | issue = 2 | pages = 101–46 | year = 1994 | pmid = 8161940 | doi = 10.1016/0197-0186(94)90100-7 }}</ref>
In mammals, melatonin receptors are found in the [[brain]] and some peripheral organs. However, there is considerable variation in the density and location of MT receptor expression between species.<ref name="pmid8161940">{{cite journal | author4 = Morgan PJ, Barrett P, Howell HE, Helliwell R | title = Melatonin receptors: localization, molecular pharmacology and physiological significance | journal = Neurochem. Int. | volume = 24 | issue = 2 | pages = 101–46 | year = 1994 | pmid = 8161940 | doi = 10.1016/0197-0186(94)90100-7 | last1 = Morgan | first1 = Peter J. | last2 = Barrett | first2 = Perry | last3 = Howell | first3 = H.Edward }}</ref>
===MT<sub>1</sub>===
===MT<sub>1</sub>===
In humans, The MT<sub>1</sub> subtype is expressed in the [[pars tuberalis]] of the [[pituitary gland]] and the [[suprachiasmatic nuclei]] of the [[hypothalamus]].
In humans, The MT<sub>1</sub> subtype is expressed in the [[pars tuberalis]] of the [[pituitary gland]] and the [[suprachiasmatic nuclei]] of the [[hypothalamus]].
===MT<sub>2</sub>===
===MT<sub>2</sub>===
The MT<sub>2</sub> subtype is expressed in the [[retina]]. MT<sub>2</sub> receptor mRNA has not been detected by in situ hybridization in the rat suprachiasmatic nucleo or pars tubealis.<ref name="Reppert_1995">{{cite journal | authors = Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF | title = Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 92 | issue = 19 | pages = 8734–8 | year = 1995 | month = September | pmid = 7568007 | pmc = 41041 | doi = }}</ref>
The MT<sub>2</sub> subtype is expressed in the [[retina]]. MT<sub>2</sub> receptor mRNA has not been detected by in situ hybridization in the rat suprachiasmatic nucleo or pars tubealis.<ref name="Reppert_1995">{{cite journal | author4 = Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF | title = Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 92 | issue = 19 | pages = 8734–8 | year = 1995 | month = September | pmid = 7568007 | pmc = 41041 | doi = 10.1073/pnas.92.19.8734| bibcode = 1995PNAS...92.8734R | author1 = Reppert | first1 = Steven M. | last2 = Godson | first2 = Catherine | last3 = Mahle | first3 = Cathy D. | last5 = Slaugenhaupt | first5 = Susan A. | last6 = Gusella | first6 = James F. }}</ref>


===MT<sub>3</sub>===
===MT<sub>3</sub>===
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===MT<sub>2</sub>===
===MT<sub>2</sub>===
In humans, the MT<sub>2</sub> subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine.<ref name="Reppert_1995"/> Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.<ref name="pmid6828862">{{cite journal | authors = Besharse JC, Dunis DA | title = Methoxyindoles and photoreceptor metabolism: activation of rod shedding | journal = Science | volume = 219 | issue = 4590 | pages = 1341–3 | year = 1983 | month = March | pmid = 6828862 | doi = }}</ref>
In humans, the MT<sub>2</sub> subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine.<ref name="Reppert_1995"/> Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.<ref name="pmid6828862">{{cite journal | author4 = Besharse JC, Dunis DA | title = Methoxyindoles and photoreceptor metabolism: activation of rod shedding | journal = Science | volume = 219 | issue = 4590 | pages = 1341–3 | year = 1983 | month = March | pmid = 6828862 | doi = 10.1126/science.6828862| bibcode = 1983Sci...219.1341B | author1 = Besharse | first1 = Joseph C. | last2 = Dunis | first2 = Daiga A. }}</ref>


===MT<sub>3</sub>===
===MT<sub>3</sub>===
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===Agonists===
===Agonists===
* [[Agomelatine]]
* [[Agomelatine]]
* [[LY-156,735]]<ref name="pmid12405554">{{cite journal | authors = Nickelsen T, Samel A, Vejvoda M, Wenzel J, Smith B, Gerzer R | title = Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: results of a placebo-controlled trial | journal = Chronobiol. Int. | volume = 19 | issue = 5 | pages = 915–36 | year = 2002 | month = September | pmid = 12405554 | doi = }}</ref>
* [[LY-156,735]]<ref name="pmid12405554">{{cite journal | author4 = Nickelsen T, Samel A, Vejvoda M, Wenzel J, Smith B, Gerzer R | title = Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: results of a placebo-controlled trial | journal = Chronobiol. Int. | volume = 19 | issue = 5 | pages = 915–36 | year = 2002 | month = September | pmid = 12405554 | doi = }}</ref>
* [[Melatonin]]
* [[Melatonin]]
* [[Piromelatine]]
* [[Piromelatine]]

Revision as of 19:56, 7 March 2014

melatonin receptor 1A
Identifiers
SymbolMTNR1A
NCBI gene4543
HGNC7463
OMIM600665
RefSeqNM_005958
UniProtP48039
Other data
LocusChr. 4 q35.1
Search for
StructuresSwiss-model
DomainsInterPro
melatonin receptor 1B
Identifiers
SymbolMTNR1B
NCBI gene4544
HGNC7464
OMIM600804
RefSeqNM_005959
UniProtP49286
Other data
LocusChr. 11 q21-q22
Search for
StructuresSwiss-model
DomainsInterPro

A melatonin receptor is a G protein-coupled receptor (GPCR) which binds melatonin.[1]

Three types of melatonin receptor have been cloned. The MT1 (or Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other mammals,[2] while an additional melatonin receptor subtype MT3 (or Mel1C or MTNR1C) has been identified in amphibia and birds.[3]

Expression patterns

In mammals, melatonin receptors are found in the brain and some peripheral organs. However, there is considerable variation in the density and location of MT receptor expression between species.[4]

MT1

In humans, The MT1 subtype is expressed in the pars tuberalis of the pituitary gland and the suprachiasmatic nuclei of the hypothalamus.

MT2

The MT2 subtype is expressed in the retina. MT2 receptor mRNA has not been detected by in situ hybridization in the rat suprachiasmatic nucleo or pars tubealis.[5]

MT3

The MT3 subtype of many non-mammalian vertebrates is expressed in various brain areas.[3]

MT Receptor function

MT1

In humans, The MT1 subtype's expression in the pars tuberalis of the pituitary gland and suprachiamatic nuclei of the hypothalamus is indicative of melatonin's circadian and reproductive functional involvement.

MT2

In humans, the MT2 subtype's expression in the retina is suggestive of melatonin's effect on the mammalian retina occurring through this receptor. Research suggests that melatonin acts to inhibit the Ca2+-dependent release of dopamine.[5] Melatonin's action in the retina is believed to affect several light-dependent functions, including phagocytosis and photopigment disc shedding.[6]

MT3

Selective Ligands

Agonists

Antagonists

See also

References

  1. ^ Reppert, S. M. (1997). "Melatonin receptors: molecular biology of a new family of G protein-coupled receptors". J. Biol. Rhythms. 12 (6): 528–31. doi:10.1177/074873049701200606. PMID 9406026.
  2. ^ Reppart, Steven M.; Weaver, David R.; Godson, Catherine; 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. doi:10.1016/0165-6147(96)10005-5. PMID 8936344.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  3. ^ a b Sugden, David; Davidson, Kathryn; Hough, Kate A.; Sugden D, Davidson K, Hough KA, Teh MT (2004). "Melatonin, melatonin receptors and melanophores: a moving story". Pigment Cell Res. 17 (5): 454–60. doi:10.1111/j.1600-0749.2004.00185.x. PMID 15357831.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. ^ Morgan, Peter J.; Barrett, Perry; Howell, H.Edward; Morgan PJ, Barrett P, Howell HE, Helliwell R (1994). "Melatonin receptors: localization, molecular pharmacology and physiological significance". Neurochem. Int. 24 (2): 101–46. doi:10.1016/0197-0186(94)90100-7. PMID 8161940.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  5. ^ a b Reppert, Steven M.; Godson, Catherine; Mahle, Cathy D.; Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF; Slaugenhaupt, Susan A.; Gusella, James F. (1995). "Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor". Proc. Natl. Acad. Sci. U.S.A. 92 (19): 8734–8. Bibcode:1995PNAS...92.8734R. doi:10.1073/pnas.92.19.8734. PMC 41041. PMID 7568007. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  6. ^ Besharse, Joseph C.; Dunis, Daiga A.; Besharse JC, Dunis DA (1983). "Methoxyindoles and photoreceptor metabolism: activation of rod shedding". Science. 219 (4590): 1341–3. Bibcode:1983Sci...219.1341B. doi:10.1126/science.6828862. PMID 6828862. {{cite journal}}: Missing |author3= (help); Unknown parameter |month= ignored (help)
  7. ^ "Chronobiotic effects of the melatonin agonist LY 156735 following a simulated 9h time shift: results of a placebo-controlled trial". Chronobiol. Int. 19 (5): 915–36. 2002. PMID 12405554. {{cite journal}}: Unknown parameter |month= ignored (help)

External links


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