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HTR2B  -  5-hydroxytryptamine (serotonin) receptor...

Sus scrofa

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Disease relevance of 5-HT2B

  • These data are consistent with activation of peripheral 5-HT2B receptors initiating PPE and the theory that selective 5-HT2B antagonists might be effective prophylactic therapies for migraine [1].

High impact information on 5-HT2B

  • NO release has been linked to activation of the 5-HT2B receptor on the vascular endothelium [1].
  • This effect was inhibited by non-selective 5-HT2 receptor antagonists (methysergide, LY53857, LY215840), by a peripherally restricted 5-HT2 receptor antagonist (xylamidine) and by a 5-HT2B selective receptor antagonist (LY202146) [1].
  • Evidence for 5-HT2B and 5-HT7 receptor-mediated relaxation in pulmonary arteries of weaned pigs [2].
  • Restrictive cardiac valvulopathies observed in Parkinson patients treated with the ergoline dopamine agonist pergolide have recently been associated with the agonist efficacy of the drug at 5-hydroxytryptamine2B (5-HT2B) receptors [3].
  • Both in vitro and in vivo methods were used to examine the interaction of bucindolol with 5-HT receptors relevant to the cardiovascular system-the 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2B receptors-and with alpha1-adrenergic receptors [4].

Biological context of 5-HT2B


Anatomical context of 5-HT2B

  • Bucindolol also displayed no agonist activity at the 5-HT2A and 5-HT2B receptor (endothelium-denuded rat thoracic aorta and rat stomach fundus, respectively), but did act as a weak 5-HT2A-receptor antagonist (-log K(B) [M] = 5.4+/-0.1) and 5-HT2B-receptor antagonist (-log K(B) [M] = 7.8+/-0.1) [4].

Associations of 5-HT2B with chemical compounds


  1. Neurogenic dural protein extravasation induced by meta-chlorophenylpiperazine (mCPP) involves nitric oxide and 5-HT2B receptor activation. Johnson, K.W., Nelson, D.L., Dieckman, D.K., Wainscott, D.B., Lucaites, V.L., Audia, J.E., Owton, W.M., Phebus, L.A. Cephalalgia : an international journal of headache. (2003) [Pubmed]
  2. Evidence for 5-HT2B and 5-HT7 receptor-mediated relaxation in pulmonary arteries of weaned pigs. Jähnichen, S., Glusa, E., Pertz, H.H. Naunyn Schmiedebergs Arch. Pharmacol. (2005) [Pubmed]
  3. Agonism at 5-HT2B receptors is not a class effect of the ergolines. Jähnichen, S., Horowski, R., Pertz, H.H. Eur. J. Pharmacol. (2005) [Pubmed]
  4. Interaction of the beta adrenergic receptor antagonist bucindolol with serotonergic receptors. Watts, S.W., Fink, G.D., Silver, P.J., Cushing, D.J. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  5. Synthesis, affinity at 5-HT2A, 5-HT2B and 5-HT2C serotonin receptors and structure-activity relationships of a series of cyproheptadine analogues. Honrubia, M.A., Rodriguez, J., Dominguez, R., Lozoya, E., Manaut, F., Seijas, J.A., Villaverde, M.C., Calleja, J.M., Cadavid, M.I., Maayani, S., Sanz, F., Loza, M.I. Chem. Pharm. Bull. (1997) [Pubmed]
  6. Species differences in the responses of pulmonary vascular preparations to 5-hydroxytryptamine. Morcillo, E.J., Cortijo, J. Thérapie. (1999) [Pubmed]
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