G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139gene.[5][6] Research has shown that mice with loss of GCP139 experience schizophrenia-like symptomatology that is rescued with the dopamine receptor antagonist haloperidol and the μ-opioid receptor antagonist naltrexone.[7][8]
Zelatriazin (TAK-41), (NBI-1065846) a potent, and GPR139 receptor selective agonist [9] which was in clinical trials to gauge the efficacy for treating psychiatric conditions such as major depressive disorder and the negative symptoms of schizophrenia, but was later dropped from development.
^"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
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^Dao M, Stoveken HM, Cao Y, Martemyanov KA (March 2022). "The role of orphan receptor GPR139 in neuropsychiatric behavior". Neuropsychopharmacology. 47 (4): 902–913. doi:10.1038/s41386-021-00962-2. PMC8882194. PMID33479510. S2CID231668867.902-913&rft.date=2022-03&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8882194#id-name=PMC&rft_id=https://api.semanticscholar.org/CorpusID:231668867#id-name=S2CID&rft_id=info:pmid/33479510&rft_id=info:doi/10.1038/s41386-021-00962-2&rft.aulast=Dao&rft.aufirst=M&rft.au=Stoveken, HM&rft.au=Cao, Y&rft.au=Martemyanov, KA&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8882194&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
^Vedel L, Nøhr AC, Gloriam DE, Bräuner-Osborne H. Pharmacology and function of the orphan GPR139 G protein-coupled receptor. Basic Clin Pharmacol Toxicol. 2020 Jun;126 Suppl 6(Suppl 6):35-46. doi:10.1111/bcpt.13263PMID31132229
^Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, et al. (August 2021). "Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia". Journal of Medicinal Chemistry. 64 (15): 11527–11542. doi:10.1021/acs.jmedchem.1c00820. PMID34260228. S2CID235908256.11527-11542&rft.date=2021-08&rft_id=https://api.semanticscholar.org/CorpusID:235908256#id-name=S2CID&rft_id=info:pmid/34260228&rft_id=info:doi/10.1021/acs.jmedchem.1c00820&rft.aulast=Reichard&rft.aufirst=HA&rft.au=Schiffer, HH&rft.au=Monenschein, H&rft.au=Atienza, JM&rft.au=Corbett, G&rft.au=Skaggs, AW&rft.au=Collia, DR&rft.au=Ray, WJ&rft.au=Serrats, J&rft.au=Bliesath, J&rft.au=Kaushal, N&rft.au=Lam, BP&rft.au=Amador-Arjona, A&rft.au=Rahbaek, L&rft.au=McConn, DJ&rft.au=Mulligan, VJ&rft.au=Brice, N&rft.au=Gaskin, PL&rft.au=Cilia, J&rft.au=Hitchcock, S&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
Vanti WB, Nguyen T, Cheng R, Lynch KR, George SR, O'Dowd BF (May 2003). "Novel human G-protein-coupled receptors". Biochemical and Biophysical Research Communications. 305 (1): 67–71. doi:10.1016/S0006-291X(03)00709-5. PMID12732197.67-71&rft.date=2003-05&rft_id=info:doi/10.1016/S0006-291X(03)00709-5&rft_id=info:pmid/12732197&rft.aulast=Vanti&rft.aufirst=WB&rft.au=Nguyen, T&rft.au=Cheng, R&rft.au=Lynch, KR&rft.au=George, SR&rft.au=O'Dowd, BF&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
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Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (June 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters. 520 (1–3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID12044878. S2CID7116392.1–3&rft.pages=97-101&rft.date=2002-06&rft_id=https://api.semanticscholar.org/CorpusID:7116392#id-name=S2CID&rft_id=info:pmid/12044878&rft_id=info:doi/10.1016/S0014-5793(02)02775-8&rft.aulast=Takeda&rft.aufirst=S&rft.au=Kadowaki, S&rft.au=Haga, T&rft.au=Takaesu, H&rft.au=Mitaku, S&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
Gloriam DE, Schiöth HB, Fredriksson R (April 2005). "Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship". Biochimica et Biophysica Acta (BBA) - General Subjects. 1722 (3): 235–246. doi:10.1016/j.bbagen.2004.12.001. PMID15777626.235-246&rft.date=2005-04&rft_id=info:doi/10.1016/j.bbagen.2004.12.001&rft_id=info:pmid/15777626&rft.aulast=Gloriam&rft.aufirst=DE&rft.au=Schiöth, HB&rft.au=Fredriksson, R&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
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