Oxytocin receptor

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Oxytocin receptor
Identifiers
SymbolsOXTR; OT-R
External IDsOMIM: 167055 MGI: 109147 HomoloGene: 20255 IUPHAR: OT GeneCards: OXTR Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez502118430
EnsemblENSG00000180914ENSMUSG00000049112
UniProtP30559Q3UPP9
RefSeq (mRNA)NM_000916XM_001001627
RefSeq (protein)NP_000907XP_001001627
Location (UCSC)Chr 3:
8.77 - 8.79 Mb		Chr 6:
112.44 - 112.46 Mb
PubMed search[1][2]

The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin.[1][2] In humans, the oxytocin receptor is encoded by the OXTR gene.[3][4], which has been localized to human chromosome 3p25.[5]

Function and location

The OXTR protein belongs to the G-protein coupled receptor family, specifically Gq,[1] and acts as a receptor for oxytocin. Its activity is mediated by G proteins which activate several different second messenger systems.[6][7]

Oxytocin receptors are expressed by the myoepithelial cells of the mammary gland, and in both the myometrium and endometrium of the uterus at the end of pregnancy. The oxytocin-oxytocin receptor system plays an important role as an inducer of uterine contractions during parturition and of milk ejection.

Oxytocin receptors are also present in the central nervous system. These receptors modulate a variety of behaviors, including stress and anxiety, social memory and recognition, sexual and aggressive behaviors, bonding (affiliation) and maternal behavior.[8][9][10] (See the oxytocin article for more details.)

In some mammals, oxytocin receptors are also found in the kidney and heart.

Ligands

Several selective ligands for the oxytocin receptor have recently been developed, but close similarity between the oxytocin and related vasopressin receptors make it difficult to achieve high selectivity.[11][12]

Agonists

Peptide
Non-peptide

Antagonists

Peptide
Non-peptide
  • GSK-221,149
  • L-368,899 (CAS# 148927-60-0)[16][17]
  • L-371,257 (CAS# 162042-44-6)[18][19] – peripherally selective (i.e. poor blood brain barrier penetration, few central effects)[20]
  • L-372,662
  • SSR-126,768
  • WAY-162,720 – centrally active following peripheral administration

References

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External links

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
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)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
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)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
Hormone receptors
Other
Opioid receptors
Other neuropeptide receptors
  1. ↑ 1.0 1.1 Gimpl G, Fahrenholz F (2001). "The oxytocin receptor system: structure, function, and regulation". Physiological Reviews. 81 (2): 629–83. PMID 11274341. 
  2. ↑ Zingg HH, Laporte SA (2003). "The oxytocin receptor". Trends in Endocrinology and Metabolism. 14 (5): 222–7. doi:10.1016/S1043-2760(03)00080-8. PMID 12826328. 
  3. ↑ "Entrez Gene: OXTR oxytocin receptor". 
  4. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. ↑ Simmons CF Jr, Clancy TE, Quan R, Knoll JH (19965). "The oxytocin receptor gene (OXTR) localizes to human chromosome 3p25 by fluorescence in situ hybridization and PCR analysis of somatic cell hybrids". Genomics. 26 (3): 623–5. doi:10.1016/0888-7543(95)80188-R. ISSN 0888-7543. PMID 7607693.  Check date values in: |date= (help)
  6. ↑ Devost D, Wrzal P, Zingg HH. Oxytocin receptor signalling. Progress in Brain Research. 2008;170:167-76. PMID 18655881
  7. ↑ Gimpl G, Reitz J, Brauer S, Trossen C. Oxytocin receptors: ligand binding, signalling and cholesterol dependence. Progress in Brain Research. 2008;170:193-204. PMID 18655883
  8. ↑ Caldwell HK, Young WS 3rd (2006). "Oxytocin and Vasopressin: Genetics and Behavioral Implications". In Lajtha, Abel; Ramon Lim. Handbook of Neurochemistry and Molecular Neurobiology (3rd ed.). Berlin: Springer. pp. 573–607. ISBN 0-387-30348-0. 
  9. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  10. ↑ Veenema AH, Neumann ID (2008). "Central vasopressin and oxytocin release: regulation of complex social behaviours". Progress in Brain Research. 170: 261–76. doi:10.1016/S0079-6123(08)00422-6. PMID 18655888. 
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  12. ↑ 12.0 12.1 Manning M, Stoev S, Chini B, Durroux T, Mouillac B, Guillon G (2008). "Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents". Progress in Brain Research. 170: 473–512. doi:10.1016/S0079-6123(08)00437-8. PMID 18655903. 
  13. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  14. ↑ Rahman Z, Resnick L, Rosenzweig-Lipson SJ, Ring RH,"Methods of treatment using oxytocin receptor agonists", US patent application 2007/0117794, published 2007-05-24 , assigned to Wyeth Corp 
  15. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  16. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  17. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  18. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  19. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  20. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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