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Chemical Compound Review

Kytril     1-methyl-N-(9-methyl-9...

Synonyms: AGN-PC-002JZD, APF530, CHEMBL289469, SureCN445223, AG-B-64422, ...
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Disease relevance of BRL 43694


Psychiatry related information on BRL 43694


High impact information on BRL 43694

  • Using these models, selective 5-HT3 receptor antagonists such as MDL 72222 (ref. 5), ICS 205-930 (ref. 6), GR38032F (ref. 7) and BRL 43694 (ref. 8) have been developed [11].
  • The 5-HT(3) antagonists, granisetron and ondansetron, are useful in combating the nausea associated with cancer chemotherapy, and alosetron is employed in the treatment of IBS with diarrhea [12].
  • The LGA flow responses to motilin were not inhibited by granisetron, C6, alpha-adrenergic, beta-adrenergic, or H2 blockers [13].
  • The effects of IV injection of 5-hydroxytryptamine 3 receptor antagonists (BRL 43694 and GR38032F) on gastrointestinal contractile activity were studied in dogs with vagally denervated fundic pouch in the conscious state by means of chronically implanted force transducers in the gastrointestinal tract and the pouch [14].
  • CONCLUSION: The administration of a 5-hydroxytryptamine3, receptor (5-HT3) antagonist, in this case granisetron, after 24 hours conferred no benefit [15].

Chemical compound and disease context of BRL 43694


Biological context of BRL 43694

  • We have used a homology model of the extracellular domain of the 5-HT(3) receptor to dock granisetron, a 5-HT(3) receptor antagonist, into the binding site using AUTODOCK [19].
  • The complete control rates were 92.9% in TT subjects (n = 14) in comparison to homozygote (47.6%, n = 21, P = .009) or heterozygote (56.1%, n = 41, P = .02) carriers of the 3435 C allele in granisetron-treated patients [20].
  • Scatchard analysis of [3H]granisetron binding resulted in KD values lower than the IC50 values of granisetron and a decreasing number of binding sites at higher temperatures [21].
  • METHOD: Thirty-one outpatients who were currently experiencing sexual dysfunction associated with SRIs were randomly assigned to double-blind treatment with granisetron (1-1.5 mg) or placebo for use 1 to 2 hours prior to sexual activity [22].
  • Granisetron was very well tolerated, and there were no clinically important changes in pulse rate, blood pressure or Holter electrocardiogram [23].

Anatomical context of BRL 43694


Associations of BRL 43694 with other chemical compounds


Gene context of BRL 43694


Analytical, diagnostic and therapeutic context of BRL 43694


  1. Reduction of cisplatin-induced emesis by a selective neurokinin-1-receptor antagonist. L-754,030 Antiemetic Trials Group. Navari, R.M., Reinhardt, R.R., Gralla, R.J., Kris, M.G., Hesketh, P.J., Khojasteh, A., Kindler, H., Grote, T.H., Pendergrass, K., Grunberg, S.M., Carides, A.D., Gertz, B.J. N. Engl. J. Med. (1999) [Pubmed]
  2. Role of 5-hydroxytryptamine in intestinal water and electrolyte movement during gut anaphylaxis. Mourad, F.H., O'Donnell, L.J., Ogutu, E., Dias, J.A., Farthing, M.J. Gut (1995) [Pubmed]
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  9. Effects of granisetron and lorazepam, alone and in combination, on psychometric performance. Leigh, T.J., Link, C.G., Fell, G.L. British journal of clinical pharmacology. (1991) [Pubmed]
  10. Lack of efficacy of the 5-HT3 receptor antagonist granisetron in the treatment of acute neuroleptic-induced akathisia. Poyurovsky, M., Weizman, A. International clinical psychopharmacology. (1999) [Pubmed]
  11. Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding. Kilpatrick, G.J., Jones, B.J., Tyers, M.B. Nature (1987) [Pubmed]
  12. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gershon, M.D., Tack, J. Gastroenterology (2007) [Pubmed]
  13. Motilin regulates interdigestive gastric blood flow in dogs. Jin, C., Naruse, S., Kitagawa, M., Ishiguro, H., Muxin, W., Nakajima, M., Yokohata, K., Ito, O., Hayakawa, T. Gastroenterology (2002) [Pubmed]
  14. Involvement of 5-hydroxytryptamine 3 receptors in regulation of interdigestive gastric contractions by motilin in the dog. Itoh, Z., Mizumoto, A., Iwanaga, Y., Yoshida, N., Torii, K., Wakabayashi, K. Gastroenterology (1991) [Pubmed]
  15. Use of dexamethasone and granisetron in the control of delayed emesis for patients who receive highly emetogenic chemotherapy. National Cancer Institute of Canada Clinical Trials Group. Latreille, J., Pater, J., Johnston, D., Laberge, F., Stewart, D., Rusthoven, J., Hoskins, P., Findlay, B., McMurtrie, E., Yelle, L., Williams, C., Walde, D., Ernst, S., Dhaliwal, H., Warr, D., Shepherd, F., Mee, D., Nishimura, L., Osoba, D., Zee, B. J. Clin. Oncol. (1998) [Pubmed]
  16. Comparative clinical trial of granisetron and ondansetron in the prophylaxis of cisplatin-induced emesis. The Granisetron Study Group. Navari, R., Gandara, D., Hesketh, P., Hall, S., Mailliard, J., Ritter, H., Friedman, C., Fitts, D. J. Clin. Oncol. (1995) [Pubmed]
  17. Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides. Youssefyeh, R.D., Campbell, H.F., Klein, S., Airey, J.E., Darkes, P., Powers, M., Schnapper, M., Neuenschwander, K., Fitzpatrick, L.R., Pendley, C.E. J. Med. Chem. (1992) [Pubmed]
  18. The utility of antiemetics in the prevention and treatment of postoperative nausea and vomiting in patients scheduled for laparoscopic cholecystectomy. Fujii, Y. Curr. Pharm. Des. (2005) [Pubmed]
  19. Locating an antagonist in the 5-HT3 receptor binding site using modeling and radioligand binding. Thompson, A.J., Price, K.L., Reeves, D.C., Chan, S.L., Chau, P.L., Lummis, S.C. J. Biol. Chem. (2005) [Pubmed]
  20. Association of the ABCB1 3435C>T polymorphism with antiemetic efficacy of 5-hydroxytryptamine type 3 antagonists. Babaoglu, M.O., Bayar, B., Aynacioglu, A.S., Kerb, R., Abali, H., Celik, I., Bozkurt, A. Clin. Pharmacol. Ther. (2005) [Pubmed]
  21. Distinct thermodynamic parameters of serotonin 5-HT3 agonists and antagonists to displace [3H]granisetron binding. Maksay, G. J. Neurochem. (1996) [Pubmed]
  22. A placebo-controlled, crossover trial of granisetron in SRI-induced sexual dysfunction. Nelson, E.B., Shah, V.N., Welge, J.A., Keck, P.E. The Journal of clinical psychiatry. (2001) [Pubmed]
  23. Efficacy and safety of granisetron in the prevention of chemotherapy-induced emesis in paediatric patients. Lemerle, J., Amaral, D., Southall, D.P., Upward, J., Murdoch, R.D. Eur. J. Cancer (1991) [Pubmed]
  24. Role of 5-hydroxytryptamine type 3 receptors in rat intestinal fluid and electrolyte secretion induced by cholera and Escherichia coli enterotoxins. Mourad, F.H., O'Donnell, L.J., Dias, J.A., Ogutu, E., Andre, E.A., Turvill, J.L., Farthing, M.J. Gut (1995) [Pubmed]
  25. Effects on muscle pain by intramuscular injection of granisetron in patients with fibromyalgia. Ernberg, M., Lundeberg, T., Kopp, S. Pain (2003) [Pubmed]
  26. Total body irradiation prior to bone marrow transplantation: efficacy and safety of granisetron in the prophylaxis and control of radiation-induced emesis. Belkacémi, Y., Ozsahin, M., Pène, F., Rio, B., Sutton, L., Laporte, J.P., Touboul, E., Gorin, N.C., Laugier, A. Int. J. Radiat. Oncol. Biol. Phys. (1996) [Pubmed]
  27. [3H]-BRL 43694 (Granisetron), a specific ligand for 5-HT3 binding sites in rat brain cortical membranes. Nelson, D.R., Thomas, D.R. Biochem. Pharmacol. (1989) [Pubmed]
  28. Efficacy and safety of granisetron, a selective 5-hydroxytryptamine-3 receptor antagonist, in the prevention of nausea and vomiting induced by high-dose cisplatin. Navari, R.M., Kaplan, H.G., Gralla, R.J., Grunberg, S.M., Palmer, R., Fitts, D. J. Clin. Oncol. (1994) [Pubmed]
  29. Review of the preclinical pharmacology and comparative efficacy of 5-hydroxytryptamine-3 receptor antagonists for chemotherapy-induced emesis. Perez, E.A. J. Clin. Oncol. (1995) [Pubmed]
  30. Resolution of fluoxetine-induced sexual dysfunction with the 5-HT3 antagonist granisetron. Nelson, E.B., Keck, P.E., McElroy, S.L. The Journal of clinical psychiatry. (1997) [Pubmed]
  31. Comparative involvement of 5-HT1, 5-HT2 and 5-HT3 receptors in stress-induced colonic motor alterations in rats. Gué, M., Alary, C., Rio-Lacheze, C.D., Junien, J.L., Buéno, L. Eur. J. Pharmacol. (1993) [Pubmed]
  32. Characterisation of the cytochrome P450 enzymes involved in the in vitro metabolism of granisetron. Bloomer, J.C., Baldwin, S.J., Smith, G.J., Ayrton, A.D., Clarke, S.E., Chenery, R.J. British journal of clinical pharmacology. (1994) [Pubmed]
  33. The effect of repeat dosing with cimetidine on the pharmacokinetics of intravenous granisetron in healthy volunteers. Youlten, L. J. Pharm. Pharmacol. (2004) [Pubmed]
  34. Structural features of the ligand-binding domain of the serotonin 5HT3 receptor. Yan, D., Schulte, M.K., Bloom, K.E., White, M.M. J. Biol. Chem. (1999) [Pubmed]
  35. A comparison of two dose levels of granisetron in patients receiving high-dose cisplatin. The Granisetron Study Group. Soukop, M. Eur. J. Cancer (1990) [Pubmed]
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