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Gene Review

5-HT3R  -  5-hydroxytryptamine receptor 3

Sus scrofa

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Disease relevance of 5-HT3R


High impact information on 5-HT3R


Biological context of 5-HT3R


Anatomical context of 5-HT3R


Associations of 5-HT3R with chemical compounds


Regulatory relationships of 5-HT3R

  • (2) Both TEA 0.05-0.5 mmol.L-1 and 4-AP 1-10 mumol.L-1 enhanced GPI contractions induced by the selective 5-HT3 receptor agonists 2-methyl-5-HT in concentration-dependent manners [20].

Other interactions of 5-HT3R

  • CONCLUSION: The enhancement by TEA and 4-AP of 5-HT3 receptor-mediated GPI contractile responses was due to blocking K+ channels in prejunctional myenteric neurons [20].

Analytical, diagnostic and therapeutic context of 5-HT3R

  • Under reducing conditions, SDS-PAGE analysis of the affinity purified 5-HT3 receptor resulted in 3-6 silver stained bands at apparent molecular masses of 37, 44-50, 52, 57-61, 63 and 65-71 kDa (n = 12) [19].
  • Unlike protein bands at 45, 50, 60 and 66 kDa, the bands corresponding to proteins of 52, 57, 63 and 71 kDa consistently gave no reaction with an antiserum specific for the cloned A subunit of the 5-HT3 receptor in both a modified dot blot procedure and a Western blot procedure (n = 2-5) [19].
  • Using the technique of in vitro receptor autoradiography, we have determined the distribution of the [3H]-(S)-zacopride labelled 5-HT3 receptor in porcine brain [12].


  1. Repeated administration of the 5-HT3 receptor antagonist granisetron reduces the incidence of delayed cisplatin-induced emesis in the piglet. Grélot, L., Le Stunff, H., Milano, S., Blower, P.R., Romain, D. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  2. The novel 5-HT4 receptor antagonist DAU 6285 antagonizes 5-hydroxytryptamine-induced tachycardia in pigs. Van Meel, J.C., Diederen, W., Haigh, R., Wienen, W., Pairet, M., Turconi, M., Doods, H.N. Eur. J. Pharmacol. (1993) [Pubmed]
  3. Inhibitory influence via 5-HT3 receptors on the induction of LTP in mossy fiber-CA3 system of guinea-pig hippocampal slices. Maeda, T., Kaneko, S., Satoh, M. Neurosci. Res. (1994) [Pubmed]
  4. Secretory pathways in Salmonella Typhimurium-induced fluid accumulation in the porcine small intestine. Grøndahl, M.L., Jensen, G.M., Nielsen, C.G., Skadhauge, E., Olsen, J.E., Hansen, M.B. J. Med. Microbiol. (1998) [Pubmed]
  5. 5-HT3 receptors are membrane ion channels. Derkach, V., Surprenant, A., North, R.A. Nature (1989) [Pubmed]
  6. Effects of cisapride on cholinergic neurotransmission and propulsive motility in the guinea pig ileum. Tonini, M., Galligan, J.J., North, R.A. Gastroenterology (1989) [Pubmed]
  7. Evidence for a 5-HT3 receptor involvement in the facilitation of peristalsis on mucosal application of 5-HT in the guinea pig isolated ileum. Tuladhar, B.R., Kaisar, M., Naylor, R.J. Br. J. Pharmacol. (1997) [Pubmed]
  8. Binding interactions of antagonists with 5-hydroxytryptamine3A receptor models. Maksay, G., Bikádi, Z., Simonyi, M. J. Recept. Signal Transduct. Res. (2003) [Pubmed]
  9. Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Rizzi, C.A., Sagrada, A., Schiavone, A., Schiantarelli, P., Cesana, R., Schiavi, G.B., Ladinsky, H., Donetti, A. Naunyn Schmiedebergs Arch. Pharmacol. (1994) [Pubmed]
  10. Effect of 5-hydroxytryptamine on vagal C-fiber subtypes in guinea pig lungs. Chuaychoo, B., Lee, M.G., Kollarik, M., Undem, B.J. Pulmonary pharmacology & therapeutics. (2005) [Pubmed]
  11. Distribution and characterisation of the [3H](S)-zacopride labelled 5-HT3 receptor in pig forebrain. Fletcher, S., Barnes, N.M. Brain Res. (1996) [Pubmed]
  12. Autoradiographic localization of the [3H]-(S)-zacopride labelled 5-HT3 receptor in porcine brain. Fletcher, S., Barnes, N.M. Neurosci. Lett. (1999) [Pubmed]
  13. Inhibition of noradrenaline release in the pig coronary artery via a novel serotonin receptor. Molderings, G.J., Göthert, M., Fink, K., Roth, E., Schlicker, E. Eur. J. Pharmacol. (1989) [Pubmed]
  14. 5-HT3 receptors augment neuronal, cholinergic contractions in guinea pig trachea. Rizzo, C.A., Kreutner, W., Chapman, R.W. Eur. J. Pharmacol. (1993) [Pubmed]
  15. The interaction of antidepressant drugs with central and peripheral (enteric) 5-HT3 and 5-HT4 receptors. Lucchelli, A., Santagostino-Barbone, M.G., Barbieri, A., Candura, S.M., Tonini, M. Br. J. Pharmacol. (1995) [Pubmed]
  16. Benzimidazolone derivatives: a new class of 5-hydroxytryptamine4 receptor agonists with prokinetic and acetylcholine releasing properties in the guinea pig ileum. Rizzi, C.A., Coccini, T., Onori, L., Manzo, L., Tonini, M. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  17. Comparison of the 5-HT3 receptor antagonist properties of ICS 205-930, GR38032F and zacopride. Cohen, M.L., Bloomquist, W., Gidda, J.S., Lacefield, W. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  18. Cisapride stimulates motility of the intestine via the 5-hydroxytryptamine receptors. Taniyama, K., Nakayama, S., Takeda, K., Matsuyama, S., Shirakawa, J., Sano, I., Tanaka, C. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  19. Purification of 5-hydroxytryptamine3 receptors from porcine brain. Fletcher, S., Barnes, N.M. Br. J. Pharmacol. (1997) [Pubmed]
  20. Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro. Yuan, Y.M., Yang, H.H., Hu, G.Y. Zhongguo yao li xue bao = Acta pharmacologica Sinica. (1998) [Pubmed]
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