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Gene Review

Tacr1  -  tachykinin receptor 1

Rattus norvegicus

Synonyms: NK-1 receptor, NK-1R, SPR, Substance-P receptor, Tac1r, ...
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Disease relevance of Tacr1


Psychiatry related information on Tacr1


High impact information on Tacr1


Chemical compound and disease context of Tacr1


Biological context of Tacr1


Anatomical context of Tacr1

  • Overexpression of Rab5a promoted NK1R translocation to perinuclear sorting endosomes, whereas the GTP binding-deficient mutant Rab5aS34N caused retention of the NK1R in superficial early endosomes [15].
  • The aim of the study was to test whether the synthesis of substance P (SP) and that of its receptor (also known as NK1 receptor) are coordinately regulated after chronic pharmacologic intervention in two neural systems, the spinal cord and basal ganglia [19].
  • Compared with control rats, NK1R messenger RNA (mRNA) was increased by 2-fold in uteri from rats treated with E2, was decreased by 3.3-fold in rats treated with P4, and was decreased by 1.8-fold in rats treated with both E2 and P4 [16].
  • In cells expressing NK1R, the selective agonist Sar-Met-substance P induced rapid translocation of beta-arrestins 1 and 2 from the cytosol to the plasma membrane and then endosomes, indicative of interaction with both isoforms [20].
  • Immunoreactive bands were observed specifically in the NKR-CHO cells, hypothalamus, and cerebral cortex but not in the SPR- or SKR-CHO cells, nor in the cerebellum [21].

Associations of Tacr1 with chemical compounds


Physical interactions of Tacr1


Co-localisations of Tacr1

  • However, in the Sprague-Dawley rat, NK1 receptor immunoreactivity was only co-localized with calcitonin gene-related peptide immunoreactivity in a minority of fibers of the circular muscle [25].

Regulatory relationships of Tacr1


Other interactions of Tacr1


Analytical, diagnostic and therapeutic context of Tacr1


  1. Interleukin-1beta upregulates functional expression of neurokinin-1 receptor (NK-1R) via NF-kappaB in astrocytes. Guo, C.J., Douglas, S.D., Gao, Z., Wolf, B.A., Grinspan, J., Lai, J.P., Riedel, E., Ho, W.Z. Glia (2004) [Pubmed]
  2. Combinations of neurokinin receptor antagonists reduce visceral hyperalgesia. Kamp, E.H., Beck, D.R., Gebhart, G.F. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  3. Nerve growth factor and nerve growth factor receptors in respiratory syncytial virus-infected lungs. Hu, C., Wedde-Beer, K., Auais, A., Rodriguez, M.M., Piedimonte, G. Am. J. Physiol. Lung Cell Mol. Physiol. (2002) [Pubmed]
  4. A neurokinin 1 receptor antagonist reduces an ongoing ileal pouch inflammation and the response to a subsequent inflammatory stimulus. Stucchi, A.F., Shebani, K.O., Leeman, S.E., Wang, C.C., Reed, K.L., Fruin, A.B., Gower, A.C., McClung, J.P., Andry, C.D., O'Brien, M.J., Pothoulakis, C., Becker, J.M. Am. J. Physiol. Gastrointest. Liver Physiol. (2003) [Pubmed]
  5. Relationship between overexpression of NK-1R, NK-2R and intestinal mucosal damage in acute necrotizing pancreatitis. Shi, X., Gao, N.R., Guo, Q.M., Yang, Y.J., Huo, M.D., Hu, H.L., Friess, H. World J. Gastroenterol. (2003) [Pubmed]
  6. Effects of supraspinal administration of PG-SPI and PG-KII, two amphibian tachykinin peptides, on nociception in the rat. Improta, G., Broccardo, M. Peptides (2000) [Pubmed]
  7. NKP608, an NK1 receptor antagonist, has an anxiolytic action in the social interaction test in rats. File, S.E. Psychopharmacology (Berl.) (2000) [Pubmed]
  8. Reinstatement of episodic-like memory in rats by neurokinin-1 receptor antagonism. Kart-Teke, E., Dere, E., Brandão, M.L., Huston, J.P., De Souza Silva, M.A. Neurobiology of learning and memory (2007) [Pubmed]
  9. NMDA-receptor regulation of substance P release from primary afferent nociceptors. Liu, H., Mantyh, P.W., Basbaum, A.I. Nature (1997) [Pubmed]
  10. Inhibition of hyperalgesia by ablation of lamina I spinal neurons expressing the substance P receptor. Mantyh, P.W., Rogers, S.D., Honore, P., Allen, B.J., Ghilardi, J.R., Li, J., Daughters, R.S., Lappi, D.A., Wiley, R.G., Simone, D.A. Science (1997) [Pubmed]
  11. Receptor endocytosis and dendrite reshaping in spinal neurons after somatosensory stimulation. Mantyh, P.W., DeMaster, E., Malhotra, A., Ghilardi, J.R., Rogers, S.D., Mantyh, C.R., Liu, H., Basbaum, A.I., Vigna, S.R., Maggio, J.E. Science (1995) [Pubmed]
  12. An isobolographic analysis of the effects of N-methyl-D-aspartate and NK1 tachykinin receptor antagonists on inflammatory hyperalgesia in the rat. Ren, K., Iadarola, M.J., Dubner, R. Br. J. Pharmacol. (1996) [Pubmed]
  13. Antinociceptive activity of the tachykinin NK1 receptor antagonist, CP-99,994, in conscious gerbils. Rupniak, N.M., Webb, J.K., Williams, A.R., Carlson, E., Boyce, S., Hill, R.G. Br. J. Pharmacol. (1995) [Pubmed]
  14. Pharmacological characterization of LY303870: a novel, potent and selective nonpeptide substance P (neurokinin-1) receptor antagonist. Gitter, B.D., Bruns, R.F., Howbert, J.J., Waters, D.C., Threlkeld, P.G., Cox, L.M., Nixon, J.A., Lobb, K.L., Mason, N.R., Stengel, P.W. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  15. Recycling and resensitization of the neurokinin 1 receptor. Influence of agonist concentration and Rab GTPases. Roosterman, D., Cottrell, G.S., Schmidlin, F., Steinhoff, M., Bunnett, N.W. J. Biol. Chem. (2004) [Pubmed]
  16. Tachykinin receptor and neutral endopeptidase gene expression in the rat uterus: characterization and regulation in response to ovarian steroid treatment. Pinto, F.M., Armesto, C.P., Magraner, J., Trujillo, M., Martín, J.D., Candenas, M.L. Endocrinology (1999) [Pubmed]
  17. Characterization of tachykinin receptors mediating plasma extravasation and vasodilatation in normal and acutely inflamed knee joints of the rat. Lam, F.Y., Wong, M.C. Br. J. Pharmacol. (1996) [Pubmed]
  18. Modulation of substance P-ergic system in the rat spinal cord by an opioid antagonist. Igwe, O.J. Brain Res. Mol. Brain Res. (1994) [Pubmed]
  19. Tachykinin systems in the spinal cord and basal ganglia: influence of neonatal capsaicin treatment or dopaminergic intervention on levels of peptides, substance P-encoding mRNAs, and substance P receptor mRNA. Sivam, S.P., Krause, J.E. J. Neurochem. (1992) [Pubmed]
  20. The third intracellular loop and carboxyl tail of neurokinin 1 and 3 receptors determine interactions with beta-arrestins. Schmidlin, F., Roosterman, D., Bunnett, N.W. Am. J. Physiol., Cell Physiol. (2003) [Pubmed]
  21. Localization of the neuromedin K receptor (NK3) in the central nervous system of the rat. Ding, Y.Q., Shigemoto, R., Takada, M., Ohishi, H., Nakanishi, S., Mizuno, N. J. Comp. Neurol. (1996) [Pubmed]
  22. Electrophysiological characterisation of tachykinin receptors in the rat nucleus of the solitary tract and dorsal motor nucleus of the vagus in vitro. Maubach, K.A., Jones, R.S. Br. J. Pharmacol. (1997) [Pubmed]
  23. Evidence that tachykinin NK2 receptors modulate resting tone in the rat isolated small intestine. Maggi, C.A., Giuliani, S. Br. J. Pharmacol. (1996) [Pubmed]
  24. [Pro9]SP and [pGlu6, Pro9]SP(6-11) interact with two different receptors in the guinea-pig ileum as demonstrated with new SP antagonists. Chassaing, G., Lavielle, S., Brunissen, A., Carruette, A., Garret, C., Petitet, F., Saffroy, M., Beaujouan, J.C., Torrens, Y., Glowinski, J. Neuropeptides (1992) [Pubmed]
  25. Cellular localization and distribution of neurokinin-1 receptors in the rat stomach. Yip, L., Kwok, Y.N., Buchan, A.M. Autonomic neuroscience : basic & clinical. (2003) [Pubmed]
  26. Tissue distribution and quantitation of the mRNAs for three rat tachykinin receptors. Tsuchida, K., Shigemoto, R., Yokota, Y., Nakanishi, S. Eur. J. Biochem. (1990) [Pubmed]
  27. Further evidence that central tachykinin NK-1 receptors mediate the inhibitory effect of tachykinins on angiotensin-induced drinking in rats. Polidori, C., Ciccocioppo, R., De Caro, G., Massi, M. Peptides (1998) [Pubmed]
  28. Heterologous regulation of trafficking and signaling of G protein-coupled receptors: beta-arrestin-dependent interactions between neurokinin receptors. Schmidlin, F., Déry, O., Bunnett, N.W., Grady, E.F. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  29. Effect of post-mortem delay on density of tachykinin receptors in rat peripheral tissues. Dias, L.S., Schell, D.N., Burcher, E. Peptides (1998) [Pubmed]
  30. NK1 receptor antagonist blocks angiotensin II responses in renin transgenic rat medulla oblongata. Diz, D.I., Westwood, B., Bosch, S.M., Ganten, D., Ferrario, C. Hypertension (1998) [Pubmed]
  31. The vanilloid receptor-1 (TRPV1) is expressed in some rat dorsal horn NK1 cells. Doly, S., Fischer, J., Conrath, M. Brain Res. (2004) [Pubmed]
  32. Corticotropin-releasing factor mRNA and substance P receptor binding in the paraventricular hypothalamic nucleus, central nucleus of the amygdala, and locus coeruleus of Sprague-Dawley rats following restraint-induced stress. Hwang, B.H., Katner, J., Iyengar, S. J. Mol. Neurosci. (2005) [Pubmed]
  33. Simultaneous quantitation of substance P-encoding preprotachykinin alternatively spliced mRNAs and substance P receptor NK-1 mRNA by an RNase protection assay. Gautreau, A., Kerdelhué, B. Brain Res. Brain Res. Protoc. (1998) [Pubmed]
  34. Noradrenergic neurons expressing substance P receptor (NK1) in the locus coeruleus complex: a double immunofluorescence study in the rat. Chen, L.W., Wei, L.C., Liu, H.L., Rao, Z.R. Brain Res. (2000) [Pubmed]
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