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Chemical Compound Review

AC1NSKNR     1-[(3S)-3-(3,4- dichlorophenyl)-3-[2-(4...

Synonyms: SR140333
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Disease relevance of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone

  • Univariate analysis revealed increased radiation injury score, bowel wall thickening, and collagen III deposition after treatment with CGRP(8-37), whereas SR140333 ameliorated radiation injury score, loss of mucosal surface area, collagen III deposition, and mucosal inflammation [1].
  • The NK(1) receptor antagonists, SDZ NKT 343, RPR100893 and SR140333, reduced mechanical hyperalgesia by 68, 36 and 27% at a dose of 30 mg kg(-1) p.o., respectively [2].
  • NGF-induced edema was not reduced by the neurokinin-1 receptor antagonist SR140333, but attenuated by the CGRP receptor antagonist CGRP[8-37] [3].
  • Both stress-induced visceral hypersensitivity in intact rats and the hormonally-restored visceral hyper-responsiveness of OVX rats were antagonized by SR140333 [4].
  • Human colonic anti-secretory activity of the potent NK(1) antagonist, SR140333: assessment of potential anti-diarrhoeal activity in food allergy and inflammatory bowel disease [5].

Psychiatry related information on 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone

  • The same doses of SR140333 given post-trial had minor facilitative effects on inhibitory avoidance learning and open-field habituation, but did not have reinforcing effects in a conditioned place preference (CPP) task [6].

High impact information on 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone

  • The selective rNK1 antagonist SR140333 totally reversed the effect of SP on progesterone conversion into 5alpha-DHP and 3alpha,5alpha-THP [7].
  • This elevated plasma leak was attenuated by recombinant NEP or the NK1R antagonist SR140333, and is thus caused by diminished degradation of SP [8].
  • The exacerbated inflammation in knockout mice was prevented by recombinant NEP and SR140333 [8].
  • The carrageenin (500 microg)-induced response was inhibited (p < 0.05) by a NK1 receptor antagonist, SR140333 (480 nmol/kg i.v. at -5 min), in the wild-type group [9].
  • Histamine release was measured from colonic samples of control and stressed animals and the effect of SR140333, a NK1 receptor antagonist, on substance P induced histamine release was determined [10].

Biological context of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone


Anatomical context of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone


Associations of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone with other chemical compounds

  • EXPERIMENTAL DESIGN: Male rats received full-length CGRP, CGRP antagonist (CGRP(8-37)), a modified substance P peptide (GR73632), a small-molecule substance P receptor antagonist (neurokinin-1 receptor antagonist, SR140333), or vehicle for 2 weeks after localized X irradiation of a 4-cm loop of small bowel [1].
  • Therefore, in a guinea pig model of allergic asthma, we investigated the involvement of the NK1 receptor in allergen-induced early (EAR) and late (LAR) asthmatic reactions, airway hyperreactivity (AHR) after these reactions and airway inflammation, using the selective nonpeptide NK1 receptor antagonist SR140333 [11].
  • The NGF increase was suppressed by treatment of rats with the selective tachykinin NK1 receptor antagonist SR140333 (0.1 mg/kg), and by the beta adrenergic agonist terbutaline (0.3 mg/kg) [18].
  • (4) The contractile responses to PAR-1 and PAR-2 activation were concentration-dependently attenuated by SR140333 (0.1-1 micro M), NK(1) receptor antagonist, or by SR48968 (0.1-1 micro M), NK(2) receptor antagonist [19].
  • Capsaicin 0.5%, which stimulates release of endogenous substance P from sensory nerves, was also found to enhance synovial angiogenesis, [PCNA index 17% (95% CI, 14% to 19%)] compared with saline injected control knees [2% (95% CI, 1% to 3%), p < 0.05], and this also was inhibited by 1 micro mol of SR140333 [11% (95% CI, 8 to 16%)] [20].

Gene context of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone

  • The present studies used mdr1a-/- mice, a spontaneously occurring mutant that is deficient in P-gp, to examine the CNS penetration of SR140333 and GR205171 [21].
  • The contractile effect of ET-1 was not affected by tetrodotoxin (1 microM), atropine (1 microM), methysergide (100 nM), chloropyramine (100 nM) or SR140333 (100 nM) but was significantly inhibited or even abolished by the receptor antagonist BQ123 (3 microM) or BQ788 (3 microM) [22].
  • SR140333 less markedly attenuated the capsaicin-induced increase in phosphorylated STAT3: whereas in the sciatic nerve the difference was significant when the data at 3 h and 6 h were combined (p < 0.05), no such treatment effect of SR140333 was observed in the DRG [15].
  • The NK1 receptor antagonist SR140333 inhibits capsaicin-induced ERK phosphorylation in sensory neurons [15].
  • Cold-storage denervation, tetrodotoxin-TTX (1 mM), spantide (100 mM) and NK1-3 receptor antagonists SR140333, 48968, 142801 (up to 10 mM) notably diminished M15, galanin(1-14)-[Abu8]Scy-I, SP(5-11) and [Abu8]-Scy-I evoked contractions without affecting activities of galanin and galanin(1-15)-NH2 [23].

Analytical, diagnostic and therapeutic context of 1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]oct-1-yl)ethyl]-1-piperidyl]-2-(3-isopropoxyphenyl)ethanone


  1. Calcitonin gene-related peptide and substance P regulate the intestinal radiation response. Wang, J., Qiu, X., Kulkarni, A., Hauer-Jensen, M. Clin. Cancer Res. (2006) [Pubmed]
  2. Oral anti-hyperalgesic and anti-inflammatory activity of NK(1) receptor antagonists in models of inflammatory hyperalgesia of the guinea-pig. Campbell, E.A., Gentry, C., Patel, S., Kidd, B., Cruwys, S., Fox, A.J., Urban, L. Pain (2000) [Pubmed]
  3. Intraplantar injection of nerve growth factor into the rat hind paw: local edema and effects on thermal nociceptive threshold. Amann, R., Schuligoi, R., Herzeg, G., Donnerer, J. Pain (1996) [Pubmed]
  4. Stress-induced visceral hypersensitivity in female rats is estrogen-dependent and involves tachykinin NK1 receptors. Bradesi, S., Eutamene, H., Garcia-Villar, R., Fioramonti, J., Bueno, L. Pain (2003) [Pubmed]
  5. Human colonic anti-secretory activity of the potent NK(1) antagonist, SR140333: assessment of potential anti-diarrhoeal activity in food allergy and inflammatory bowel disease. Moriarty, D., Goldhill, J., Selve, N., O'Donoghue, D.P., Baird, A.W. Br. J. Pharmacol. (2001) [Pubmed]
  6. Neurokinin-1 receptor antagonism by SR140333: enhanced in vivo ACh in the hippocampus and promnestic post-trial effects. Kart, E., Jocham, G., Müller, C.P., Schlömer, C., Brandão, M.L., Huston, J.P., de Souza Silva, M.A. Peptides (2004) [Pubmed]
  7. Substance P inhibits progesterone conversion to neuroactive metabolites in spinal sensory circuit: a potential component of nociception. Patte-Mensah, C., Kibaly, C., Mensah-Nyagan, A.G. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  8. Neutral endopeptidase (EC terminates colitis by degrading substance P. Sturiale, S., Barbara, G., Qiu, B., Figini, M., Geppetti, P., Gerard, N., Gerard, C., Grady, E.F., Bunnett, N.W., Collins, S.M. Proc. Natl. Acad. Sci. U.S.A. (1999) [Pubmed]
  9. Neurokinin-1 receptor agonists are involved in mediating neutrophil accumulation in the inflamed, but not normal, cutaneous microvasculature: an in vivo study using neurokinin-1 receptor knockout mice. Cao, T., Pintér, E., Al-Rashed, S., Gerard, N., Hoult, J.R., Brain, S.D. J. Immunol. (2000) [Pubmed]
  10. Acute restraint stress activates functional NK1 receptor in the colon of female rats: involvement of steroids. Bradesi, S., Eutamene, H., Fioramonti, J., Bueno, L. Gut (2002) [Pubmed]
  11. Involvement of tachykinin NK1 receptor in the development of allergen-induced airway hyperreactivity and airway inflammation in conscious, unrestrained guinea pigs. Schuiling, M., Zuidhof, A.B., Zaagsma, J., Meurs, H. Am. J. Respir. Crit. Care Med. (1999) [Pubmed]
  12. Role of tachykinin NK receptors on the local and remote injuries following ischaemia and reperfusion of the superior mesenteric artery in the rat. Souza, D.G., Mendonça, V.A., de A Castro, M.S., Poole, S., Teixeira, M.M. Br. J. Pharmacol. (2002) [Pubmed]
  13. An examination of neurogenic mechanisms involved in mustard oil-induced inflammation in the mouse. Grant, A.D., Pinter, E., Salmon, A.M., Brain, S.D. Eur. J. Pharmacol. (2005) [Pubmed]
  14. Characterisation of substance P-induced endocytosis of NK1 receptors on enteric neurons. Southwell, B.R., Woodman, H.L., Murphy, R., Royal, S.J., Furness, J.B. Histochem. Cell Biol. (1996) [Pubmed]
  15. The NK1 receptor antagonist SR140333 inhibits capsaicin-induced ERK phosphorylation in sensory neurons. Donnerer, J., Liebmann, I. Pharmacology (2006) [Pubmed]
  16. Post-stimulus potentiation of transmission in pelvic ganglia enhances sympathetic dilatation of guinea-pig uterine artery in vitro. Morris, J.L., Gibbins, I.L., Jobling, P. J. Physiol. (Lond.) (2005) [Pubmed]
  17. Mechanisms underlying the inhibitory effects of tachykinin receptor antagonists on eosinophil recruitment in an allergic pleurisy model in mice. Alessandri, A.L., Pinho, V., Souza, D.G., Castro, M.S., Klein, A., Teixeira, M.M. Br. J. Pharmacol. (2003) [Pubmed]
  18. Beta adrenergic inhibition of capsaicin-induced, NK1 receptor-mediated nerve growth factor biosynthesis in rat skin. Amann, R., Schuligoi, R. Pain (2004) [Pubmed]
  19. Involvement of nitric oxide and tachykinins in the effects induced by protease-activated receptors in rat colon longitudinal muscle. Mulè, F., Baffi, M.C., Capparelli, A., Pizzuti, R. Br. J. Pharmacol. (2003) [Pubmed]
  20. Enhancement of angiogenesis by endogenous substance P release and neurokinin-1 receptors during neurogenic inflammation. Seegers, H.C., Hood, V.C., Kidd, B.L., Cruwys, S.C., Walsh, D.A. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  21. P-Glycoprotein efflux reduces the brain concentration of the substance P (NK1 receptor) antagonists SR140333 and GR205171: a comparative study using mdr1a-/- and mdr1a+/+ mice. Rupniak, N.M., Fisher, A., Boyce, S., Clarke, D., Pike, A., O'Connor, D., Watt, A. Behavioural pharmacology. (2003) [Pubmed]
  22. Actions of endothelin and corticotropin releasing factor in the guinea-pig ileum: no evidence for an interaction with capsaicin-sensitive neurons. Lázár, Z., Benkó, R., Bölcskei, K., Rumbus, Z., Wolf, M., Holzer, P., Maggi, C.A., Barthó, L. Neuropeptides (2003) [Pubmed]
  23. Mechanism of the contractile effects of galantide and Galanin(1-14) [alpha-aminobutyric acid]scyliorhinin-I in rat isolated fundus strips. Korolkiewicz, R.P., Konstanski, Z., Rekowski, P., Szyk, A., Ruczyński, J., Dabrowski, J., Ujda, M., Korolkiewicz, K.Z., Petrusewicz, J. Med. Sci. Monit. (2002) [Pubmed]
  24. The role of neurokinin 1 receptors in the maintenance of visceral hyperalgesia induced by repeated stress in rats. Bradesi, S., Kokkotou, E., Simeonidis, S., Patierno, S., Ennes, H.S., Mittal, Y., McRoberts, J.A., Ohning, G., McLean, P., Marvizon, J.C., Sternini, C., Pothoulakis, C., Mayer, E.A. Gastroenterology (2006) [Pubmed]
  25. Bone marrow-derived mast cells in mice respond in co-culture to scorpion venom activation of superior cervical ganglion neurites according to level of expression of NK-1 receptors. Furuno, T., Ma, D., van der Kleij, H.P., Nakanishi, M., Bienenstock, J. Neurosci. Lett. (2004) [Pubmed]
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