Tahikininski receptor 1

Osobine

Klinički značaj

Selektivni ligandi

• GR-73632 - potentan i selektivan agonist, EC₅₀ 2nM, polipeptid sa pet aminokiselina

• Aprepitant
• Kasopitant
• Ezlopitant
• Fosaprepitant
• Lanepitant
• Maropitant
• Vestipitant
• L-733,060
• L-741,671
• L-742,694
• RP-67580 - potentan i selektivan antagonist, Ki 2.9nM, (3aR,7aR)-oktahidro-2-[1-imino-2-(2-metoksifenil)etil ]-7,7-difenil-4H-izoindol
• RPR-100,893
• CP-96345
• CP-99994
• GR-205,171
• TAK-637
• T-2328

Vidi još

Literatura

1. ↑ Takeda Y, Chou KB, Takeda J, Sachais BS, Krause JE (1991). „Molecular cloning, structural characterization and functional expression of the human substance P receptor”. Biochem. Biophys. Res. Commun. 179 (3): 1232–40. DOI:10.1016/0006-291X(91)91704-G. PMID 1718267. 
2. ↑ ^{2,0 2,1 2,2} Ho W. Z., Douglas S. D. (December 2004). „Substance P and neurokinin-1 receptor modulation of HIV”. Journal of Neuroimmunology 157 (1–2): 48–55. DOI:10.1016/j.jneuroim.2004.08.022. PMID 15579279. Arhivirano iz originala na datum 2009-09-01. Pristupljeno 2014-05-08. 
3. ↑ ^{3,0 3,1} Page N. M. (August 2005). „New challenges in the study of the mammalian Tachykinins”. Peptides 26 (8): 1356–1368. DOI:10.1016/j.peptides.2005.03.030. PMID 16042976. 
4. ↑ ^{4,0 4,1} Datar P., Srivastava S., Coutinho E., Govil G. (2004). „Substance P: Structure, Function, and Therapeutics”. Current Topics in Medicinal Chemistry 4 (1): 75–103. DOI:10.2174/1568026043451636. PMID 14754378. Arhivirano iz originala na datum 2009-09-18. Pristupljeno 2014-05-08. 
5. ↑ ^{5,0 5,1} Satake H., Kawada T. (August 2006). „Overview of the primary structure, tissue-distribution, and functions of tachykinins and their receptors”. Current Drug Targets 7 (8): 963–974. DOI:10.2174/138945006778019273. Arhivirano iz originala na datum 2009-09-03. Pristupljeno 2014-05-08. 
6. ↑ ^{6,0 6,1} Almeida T. A., Rojo J., Nieto P. M., Hernandez M., Martin J. D., Candenas M. L. (August 2004). „Tachykinins and Tachykinins Receptors: Structure and Activity Relationships”. Current Medicinal Chemistry 11 (15): 2045–2081. PMID 15279567. 
7. ↑ Humphrey JM (2003). „Medicinal chemistry of selective neurokinin-1 antagonists”. Current topics in medicinal chemistry 3 (12): 1423–35. DOI:10.2174/1568026033451925. PMID 12871173. 
8. ↑ Yu YJ, Arttamangkul S, Evans CJ, Williams JT, von Zastrow M (January 2009). „Neurokinin 1 receptors regulate morphine-induced endocytosis and desensitization of mu-opioid receptors in CNS neurons”. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 29 (1): 222–33. DOI:10.1523/JNEUROSCI.4315-08.2009. PMC 2775560. PMID 19129399. 
9. ↑ Perlis RH, Purcell S, Fagerness J, Kirby A, Petryshen TL, Fan J, Sklar P (January 2008). „Family-based association study of lithium-related and other candidate genes in bipolar disorder”. Arch. Gen. Psychiatry 65 (1): 53–61. DOI:10.1001/archgenpsychiatry.2007.15. PMID 18180429. 
10. ↑ George DT, Gilman J, Hersh J, Thorsell A, Herion D, Geyer C, Peng X, Kielbasa W, Rawlings R, Brandt JE, Gehlert DR, Tauscher JT, Hunt SP, Hommer D, Heilig M (March 2008). „Neurokinin 1 receptor antagonism as a possible therapy for alcoholism”. Science (journal) 319 (5869): 1536–9. DOI:10.1126/science.1153813. PMID 18276852. 
11. ↑ Jordan K (2006). „Neurokinin-1-receptor antagonists: a new approach in antiemetic therapy”. Onkologie 29 (1-2): 39–43. DOI:10.1159/000089800. PMID 16514255. 

Dodatna literatura

• Burcher E (1989). „The study of tachykinin receptors.”. Clin. Exp. Pharmacol. Physiol. 16 (6): 539–43. DOI:10.1111/j.1440-1681.1989.tb01602.x. PMID 2548782. 
• Kowall NW, Quigley BJ, Krause JE, et al. (1993). „Substance P and substance P receptor histochemistry in human neurodegenerative diseases.”. Regul. Pept. 46 (1-2): 174–85. DOI:10.1016/0167-0115(93)90028-7. PMID 7692486. 
• Patacchini R, Maggi CA (2002). „Peripheral tachykinin receptors as targets for new drugs.”. Eur. J. Pharmacol. 429 (1-3): 13–21. DOI:10.1016/S0014-2999(01)01301-2. PMID 11698023. 
• Saito R, Takano Y, Kamiya HO (2003). „Roles of substance P and NK(1) receptor in the brainstem in the development of emesis.”. J. Pharmacol. Sci. 91 (2): 87–94. DOI:10.1254/jphs.91.87. PMID 12686752. 
• Fong TM, Yu H, Huang RR, Strader CD (1992). „The extracellular domain of the neurokinin-1 receptor is required for high-affinity binding of peptides.”. Biochemistry 31 (47): 11806–11. DOI:10.1021/bi00162a019. PMID 1280161. 
• Fong TM, Huang RR, Strader CD (1993). „Localization of agonist and antagonist binding domains of the human neurokinin-1 receptor.”. J. Biol. Chem. 267 (36): 25664–7. PMID 1281469. 
• Fong TM, Anderson SA, Yu H, et al. (1992). „Differential activation of intracellular effector by two isoforms of human neurokinin-1 receptor.”. Mol. Pharmacol. 41 (1): 24–30. PMID 1310144. 
• Takahashi K, Tanaka A, Hara M, Nakanishi S (1992). „The primary structure and gene organization of human substance P and neuromedin K receptors.”. Eur. J. Biochem. 204 (3): 1025–33. DOI:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928. 
• Walsh DA, Mapp PI, Wharton J, et al. (1992). „Localisation and characterisation of substance P binding to human synovial tissue in rheumatoid arthritis.”. Ann. Rheum. Dis. 51 (3): 313–7. DOI:10.1136/ard.51.3.313. PMC 1004650. PMID 1374227. 
• Gerard NP, Garraway LA, Eddy RL, et al. (1991). „Human substance P receptor (NK-1): organization of the gene, chromosome localization, and functional expression of cDNA clones.”. Biochemistry 30 (44): 10640–6. DOI:10.1021/bi00108a006. PMID 1657150. 
• Hopkins B, Powell SJ, Danks P, et al. (1991). „Isolation and characterisation of the human lung NK-1 receptor cDNA.”. Biochem. Biophys. Res. Commun. 180 (2): 1110–7. DOI:10.1016/S0006-291X(05)81181-7. PMID 1659396. 
• Takeda Y, Chou KB, Takeda J, et al. (1991). „Molecular cloning, structural characterization and functional expression of the human substance P receptor.”. Biochem. Biophys. Res. Commun. 179 (3): 1232–40. DOI:10.1016/0006-291X(91)91704-G. PMID 1718267. 
• Giuliani S, Barbanti G, Turini D, et al. (1992). „NK2 tachykinin receptors and contraction of circular muscle of the human colon: characterization of the NK2 receptor subtype.”. Eur. J. Pharmacol. 203 (3): 365–70. DOI:10.1016/0014-2999(91)90892-T. PMID 1723045. 
• Ichinose H, Katoh S, Sueoka T, et al. (1991). „Cloning and sequencing of cDNA encoding human sepiapterin reductase--an enzyme involved in tetrahydrobiopterin biosynthesis.”. Biochem. Biophys. Res. Commun. 179 (1): 183–9. DOI:10.1016/0006-291X(91)91352-D. PMID 1883349. 
• Thöny B, Heizmann CW, Mattei MG (1995). „Human GTP-cyclohydrolase I gene and sepiapterin reductase gene map to region 14q21-q22 and 2p14-p12, respectively, by in situ hybridization.”. Genomics 26 (1): 168–70. DOI:10.1016/0888-7543(95)80101-Q. PMID 7782081. 
• Fong TM, Cascieri MA, Yu H, et al. (1993). „Amino-aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345.”. Nature 362 (6418): 350–3. DOI:10.1038/362350a0. PMID 8384323. 
• Derocq JM, Ségui M, Blazy C, et al. (1997). „Effect of substance P on cytokine production by human astrocytic cells and blood mononuclear cells: characterization of novel tachykinin receptor antagonists.”. FEBS Lett. 399 (3): 321–5. DOI:10.1016/S0014-5793(96)01346-4. PMID 8985172. 
• De Felipe C, Herrero JF, O'Brien JA, et al. (1998). „Altered nociception, analgesia and aggression in mice lacking the receptor for substance P.”. Nature 392 (6674): 394–7. DOI:10.1038/32904. PMID 9537323. 

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