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

• Synthesis, affinity at 5-HT2A, 5-HT2B and 5-HT2C serotonin receptors and structure-activity relationships of a series of cyproheptadine analogues [5].

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

• 5-HT contracts bovine, ovine, canine, caprine, feline, rabbit, guinea-pig and rat isolated pulmonary arteries mainly by activation of 5-HT2A receptors but relaxes porcine pulmonary artery through activation of endothelial 5-HT2B receptors [6].

References