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Gene Review

HTR2A  -  5-hydroxytryptamine (serotonin) receptor...

Bos taurus

Synonyms: 5HT2A, 5HTR2A
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Disease relevance of 5HTR2A


High impact information on 5HTR2A

  • These data suggest that the mitogenic effect of 5-HT on endothelial cells is mediated by the 5-HT2 receptor, which is coupled to a G protein [1].
  • Ketanserin, a high-affinity ligand for 5-HT2 type receptors, was ineffective in displacing [3H]5-HT binding at concentrations up to 4 microM indicating a 5-HT1 receptor as the primary receptor type isolated [3].
  • It has been shown previously that serotonin stimulates the production of prostacyclin by bovine aortic smooth muscle cells in culture, via 5-HT2 receptors (Coughlin SR, Moskowitz MA, Antoniades HN, Levine L. Proc Natl Acad Sci USA 1981;78:7134-7138) [4].
  • In addition, both 5-HT2- and 5-HT3-selective agents are essentially inactive at these binding sites [5].
  • These responses were effectively blocked by the 5-HT1B receptor antagonist, isamoltane, the 5-HT1B/5-HT2 receptor antagonist, methiothepin, and the eNOS selective antagonists (0.01-10 microM): L-Nomega -monomethyl-L-arginine (L-NMMA) and L-N omega-iminoethyl-L-ornithine (L-NIO) [6].

Biological context of 5HTR2A


Anatomical context of 5HTR2A


Associations of 5HTR2A with chemical compounds


  1. Mitogenic effect of serotonin on vascular endothelial cells. Pakala, R., Willerson, J.T., Benedict, C.R. Circulation (1994) [Pubmed]
  2. Pulmonary response to intravenous administration of 5-hydroxytryptamine after type-2 receptor blockade in healthy calves. Linden, A.S., Desmecht, D.J., Amory, H., Rollin, F.A., Michaux, C.L., Lekeux, P. Am. J. Vet. Res. (1993) [Pubmed]
  3. Purification and reconstitution of serotonin receptors from bovine brain. Gallaher, T.K., Wang, H.H. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
  4. Stimulation of aortic smooth muscle prostacyclin by serotonin: role of distinct receptors in contractile and synthetic states. Demolle, D., Van Coevorden, A., Boeynaems, J.M. Circ. Res. (1989) [Pubmed]
  5. Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes. Heuring, R.E., Peroutka, S.J. J. Neurosci. (1987) [Pubmed]
  6. 5-hydroxytryptamine evokes endothelial nitric oxide synthase activation in bovine aortic endothelial cell cultures. McDuffie, J.E., Coaxum, S.D., Maleque, M.A. Proc. Soc. Exp. Biol. Med. (1999) [Pubmed]
  7. A paradox: the 5-HT2-receptor antagonist ketanserin restores the 5-HT-induced contraction depressed by methysergide in large coronary arteries of calf. Allosteric regulation of 5-HT2-receptors. Kaumann, A.J., Frenken, M. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
  8. Evidence that ergovaline acts on serotonin receptors. Dyer, D.C. Life Sci. (1993) [Pubmed]
  9. Rapid desensitization and resensitization of 5-HT2 receptor mediated phosphatidyl inositol hydrolysis by serotonin agonists in quiescent calf aortic smooth muscle cells. Pauwels, P.J., Van Gompel, P., Leysen, J.E. Life Sci. (1990) [Pubmed]
  10. Characterization of 5-hydroxytryptamine receptors in bovine coronary arteries. Foy, R.A., Myles, J.L., Wilkerson, R.D. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  11. Serotonin-induced vasoconstriction in rabbit femoral artery: mediation by both 5-HT2 serotonergic and alpha 1-adrenoceptors. Grandaw, P.P., Purdy, R.E. J. Cardiovasc. Pharmacol. (1996) [Pubmed]
  12. Target size analysis of serotonin 5-HT1 and 5-HT2 receptors in bovine brain membranes. Nishino, N., Tanaka, C. Life Sci. (1985) [Pubmed]
  13. Reactivity of the bronchial artery to 5-hydroxytryptamine. Ei-Fawal, H.A., Ogunbiyi, P.O., Gordon, V., Eyre, P. Res. Commun. Chem. Pathol. Pharmacol. (1985) [Pubmed]
  14. Two classes of [3H]spiperone binding sites in bovine neurohypophysis: D-2 receptors and putative 5-HT2 receptors. Treiman, M., Andersen, P.H. J. Recept. Res. (1989) [Pubmed]
  15. Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Peroutka, S.J. Biol. Psychiatry (1985) [Pubmed]
  16. Clebopride enhances contractility of the guinea pig stomach by blocking peripheral D2 dopamine receptor and alpha-2 adrenoceptor. Takeda, K., Taniyama, K., Kuno, T., Sano, I., Ishikawa, T., Ohmura, I., Tanaka, C. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  17. Interconversion into a low active state protects vascular 5-HT2-receptors against irreversible antagonism by phenoxybenzamine. Frenken, M., Kaumann, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (1987) [Pubmed]
  18. Effects of tryptamine mediated through 2 states of the 5-HT2 receptor in calf coronary artery. Frenken, M., Kaumann, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (1988) [Pubmed]
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