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Chemical Compound Review

Lopac-M-109     3-(2-aminoethyl)-2-methyl-1H- indol-5-ol

Synonyms: Tocris-0558, CHEMBL266591, SureCN399028, CHEBI:31085, CCG-204897, ...
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Disease relevance of Lopac-M-109


Psychiatry related information on Lopac-M-109

  • 2-Methyl-5-HT produced forward locomotion, rearing, and increased wakefulness, but did not appreciably alter circling, grooming or sniffing [6].
  • Methiothepin pretreatment had no effect on the hyperlocomotor response to 2-methyl-5-HT, although methiothepin itself produced an initial increase in spontaneous locomotor activity (for the 60-120 min period) [6].

High impact information on Lopac-M-109


Chemical compound and disease context of Lopac-M-109


Biological context of Lopac-M-109


Anatomical context of Lopac-M-109

  • 7. The capacity of the 5-HT3 receptor agonist, 2 methyl-5-HT, to enhance the electrically evoked release of tritium was not altered in hypothalamus, hippocampus, and frontal cortex slices prepared from befloxatone-treated guinea-pigs, but was significantly attenuated in the paroxetine group also treated for 21 days.(ABSTRACT TRUNCATED AT 400 WORDS)[20]
  • 5-HT and 2-methyl-5-HT induced dose-dependent depolarizations of rat isolated vagus nerve with EC50 values of 2.53 (1.93-3.33) x 10(-6) and 4.03 (2.87-5.66) x 10(-6) M, respectively [21].
  • 3. In hypothalamus slices, this response was lost when 2-methyl-5-HT was introduced 20 min before the stimulation, thus indicating that these 5-HT3 receptors desensitize rapidly [22].
  • 2-methyl-5-HT had no effect on the tracheal smooth muscle [17].
  • 1. Despite the fact that 5-hydroxytryptamine (5-HT)-induced contractions of the rabbit isolated renal artery are mediated by a receptor belonging to the heterogeneous 5-HT1-like category, we observed that the so-called selective 5-HT3 receptor agonist, 2-methyl-5-HT, caused a concentration-dependent contraction of this vessel [23].

Associations of Lopac-M-109 with other chemical compounds


Gene context of Lopac-M-109


Analytical, diagnostic and therapeutic context of Lopac-M-109


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  8. Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors. Michel, K., Zeller, F., Langer, R., Nekarda, H., Kruger, D., Dover, T.J., Brady, C.A., Barnes, N.M., Schemann, M. Gastroenterology (2005) [Pubmed]
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  11. Serotonergic signaling inhibits hyperalgesia induced by spinal cord damage. Horiuchi, H., Ogata, T., Morino, T., Takeba, J., Yamamoto, H. Brain Res. (2003) [Pubmed]
  12. The anti-emetic activity of GK-128 in Suncus murinus. Ito, C., Isobe, Y., Kijima, H., Kiuchi, Y., Ohtsuki, H., Kawamura, R., Tsuchida, K., Higuchi, S. Eur. J. Pharmacol. (1995) [Pubmed]
  13. New 5-HT3 (serotonin-3) receptor antagonists. IV. Synthesis and structure-activity relationships of azabicycloalkaneacetamide derivatives. Kato, M., Ito, K., Nishino, S., Yamakuni, H., Takasugi, H. Chem. Pharm. Bull. (1995) [Pubmed]
  14. Pharmacological effects of the new gastroprokinetic agent mosapride citrate and its metabolites in experimental animals. Yoshida, N., Omoya, H., Kato, S., Ito, T. Arzneimittel-Forschung. (1993) [Pubmed]
  15. Pharmacological characterization of 5-hydroxytryptamine3 receptors in murine brain and ileum using the novel radioligand [3H]RS-42358-197: evidence for receptor heterogeneity. Bonhaus, D.W., Wong, E.H., Stefanich, E., Kunysz, E.A., Eglen, R.M. J. Neurochem. (1993) [Pubmed]
  16. Serotonin3 receptor agonists attenuate glutamate-induced firing in rat hippocampal CA1 pyramidal cells. Zhang, J.Y., Zeise, M.L., Wang, R.Y. Neuropharmacology (1994) [Pubmed]
  17. Receptors mediating the effects of 5-hydroxytryptamine on the tracheal vasculature and smooth muscle of sheep. Webber, S.E., Salonen, R.O., Widdicombe, J.G. Br. J. Pharmacol. (1990) [Pubmed]
  18. Effects of 5-HT3 agonists on reproductive behaviors in rats. Tanco, S.A., Watson, N.V., Gorzalka, B.B. Psychopharmacology (Berl.) (1994) [Pubmed]
  19. The anti-emetic effects of CP-99,994 in the ferret and the dog: role of the NK1 receptor. Watson, J.W., Gonsalves, S.F., Fossa, A.A., McLean, S., Seeger, T., Obach, S., Andrews, P.L. Br. J. Pharmacol. (1995) [Pubmed]
  20. Modulation of 5-HT release in the guinea-pig brain following long-term administration of antidepressant drugs. Blier, P., Bouchard, C. Br. J. Pharmacol. (1994) [Pubmed]
  21. Comparative study of the affinities of the 5-HT3 receptor antagonists, YM060, YM114 (KAE-393), granisetron and ondansetron in rat vagus nerve and cerebral cortex. Ito, H., Akuzawa, S., Tsutsumi, R., Kiso, T., Kamato, T., Nishida, A., Yamano, M., Miyata, K. Neuropharmacology (1995) [Pubmed]
  22. Functional characterization of a 5-HT3 receptor which modulates the release of 5-HT in the guinea-pig brain. Blier, P., Bouchard, C. Br. J. Pharmacol. (1993) [Pubmed]
  23. Rabbit isolated renal artery contractions by some tryptamine derivatives, including 2-methyl-5-HT, are mediated by a 5-HT1-like receptor. Tadipatri, S., Feniuk, W., Saxena, P.R. Br. J. Pharmacol. (1992) [Pubmed]
  24. Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding. Hoyer, D., Neijt, H.C. Mol. Pharmacol. (1988) [Pubmed]
  25. 5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin. Ismaiel, A.M., Titeler, M., Miller, K.J., Smith, T.S., Glennon, R.A. J. Med. Chem. (1990) [Pubmed]
  26. Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Ireland, S.J., Tyers, M.B. Br. J. Pharmacol. (1987) [Pubmed]
  27. 5-HT3 and 5-HT4 receptor-mediated facilitation of the emptying phase of the peristaltic reflex in the marmoset isolated ileum. Tuladhar, B.R., Costall, B., Naylor, R.J. Br. J. Pharmacol. (1996) [Pubmed]
  28. Pharmacological characteristics and regulation of 5-HT receptor-stimulated phosphoinositide hydrolysis in the rat spinal cord. Toscano, E., Romero, G., Oset, C., Del Río, J. Gen. Pharmacol. (1999) [Pubmed]
  29. 5-Hydroxytryptamine contracts human uterine artery smooth muscle predominantly via 5-HT2 receptors. Karlsson, C., Bodelsson, G., Bodelsson, M., Stjernquist, M. Hum. Reprod. (1997) [Pubmed]
  30. Itch-associated response induced by intradermal serotonin through 5-HT2 receptors in mice. Yamaguchi, T., Nagasawa, T., Satoh, M., Kuraishi, Y. Neurosci. Res. (1999) [Pubmed]
  31. 5-HT receptor subtypes outside the central nervous system. Roles in the physiology of the gut. Gershon, M.D., Wade, P.R., Kirchgessner, A.L., Tamir, H. Neuropsychopharmacology (1990) [Pubmed]
  32. 5-hydroxytryptamine3 (5-HT3) receptors mediate spinal 5-HT antinociception: an antisense approach. Paul, D., Yao, D., Zhu, P., Minor, L.D., Garcia, M.M. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  33. Serotonergic modulation of L-glutamic acid-evoked release of endogenous norepinephrine from rat hypothalamus. Goldfarb, J., Walcott, J., Blandina, P. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
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