ArticleBritish journal of pharmacology2000
Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 90 citations in OpenAlex.
- Bilobalide increases SKBMC complementary medicine and therapies · 2026Article
- Discovery of a Novel, Potent, and Selective 5‑Hydroxytryptamine 2B Receptor Antagonist that Induces Mitochondrial Biogenesis in the Kidney.ACS pharmacology & translational science · 2025Article
- A 5-HT-mediated urethral defense against urinary tract infections.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Characterization of Vasoreactivity in a Semi-Arboreal Snake, the Tokara Habu (Animals : an open access journal from MDPI · 2023Article
- G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders.Signal transduction and targeted therapy · 2023Review
- Characterization of endothelium-dependent and -independent processes in occipital artery of the rat: relevance to control of blood flow to nodose sensory cells.Journal of applied physiology (Bethesda, Md. : 1985) · 2021Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Psychotropic Drugs for the Management of Chronic Pain and Itch.Pharmaceuticals (Basel, Switzerland) · 2019Review
- Enhancement by Hydrogen Peroxide of Calcium Signals in Endothelial Cells Induced by 5-HT1B and 5-HT2B Receptor Agonists.Oxidative medicine and cellular longevity · 2019Article
- Endothelial nitric oxide synthase in rat brain is downregulated by sub-chronic antidepressant treatment.Psychopharmacology · 2017Article
- Molecular interactions between general anesthetics and the 5HT2B receptor.Journal of biomolecular structure & dynamics · 2015Article
- Effects of intracerebroventricular injections of 5-HT on systemic vascular resistances of conscious rats.Microvascular research · 2014Article
- Serotonin mediation of early memory formation via 5-HT2B receptor-induced glycogenolysis in the day-old chick.Frontiers in pharmacology · 2014Article
- Synthesis of novel analogs of cabergoline: improving cardiovascular safety by removing 5-HT2B receptor agonism.ACS medicinal chemistry letters · 2013Article
- Characteristics of the actions by which 5-hydroxytryptamine affects electrical and mechanical activities in rabbit jugular vein graft.British journal of pharmacology · 2012Article
- Molecular targets for therapy in systemic sclerosis.Fibrogenesis & tissue repair · 2012Article
- Platelet-derived serotonin links vascular disease and tissue fibrosis.The Journal of experimental medicine · 2011Article
- Discriminative stimulus effects of serotonin agonists, neutral antagonists, and inverse agonists in pigeons: perspectives on intrinsic efficacy measurements in vivo.Psychopharmacology · 2010Article
- Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications.Naunyn-Schmiedeberg's archives of pharmacology · 2007Review
- Contribution of serotonin (5-HT) 5-HT2 receptor subtypes to the discriminative stimulus effects of cocaine in rats.Psychopharmacology · 2006Article
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2 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The endothelial 5-HT receptor mediating relaxation of pig pulmonary artery has been characterized using the selective 5-HT(2B) receptor agonist BW 723C86 and a variety of structurally diverse 5-HT receptor antagonists. If arterial rings with intact endothelium were precontracted with prostaglandin F(2alpha) (3 microM), BW 723C86 caused concentration-dependent relaxation with a pEC(50)=8.21+/-0.03 and E(max)=89+/-4% relative to 5-HT. The relaxant responses to BW 723C86 were inhibited by the 5-HT(2B) receptor antagonist SB 204741, the 5-HT(2B/2C) receptor antagonist SB 206553 and the antimigraine drug pizotifen, yielding pA(2) values of 6.68, 7.20 and 8.32, respectively. The pA(2) values against BW 723C86 were similar to those determined against 5-HT. The relaxant effect of 5-HT was antagonized by a variety of 22 compounds of diverse chemical structures. Based on the calculated mean pA(2) values the order of the most potent antagonists was ritanserin (9.38) > methysergide (8. 86) > pizotifen (8.47) >/= methiothepin (8.32) > LY 53857 (7.84) >/= amoxapine (7.80) >/= loxapine (7.73) >/= metergoline (7.64) >/= mianserin (7.51) >/= rauwolscine (7.39). Compounds with weak blocking potency were yohimbine (6.37), spiperone (5.88) and ketanserin (5.85). Correlation analysis between the affinities of the antagonists in pig pulmonary artery and those from radioligand binding studies at human and rat 5-HT(2B) receptors showed a highly significant correlation (r=0.95 and 0.84, P<0.002 and <0.005). Correlation with 5-HT(2C) receptors was much lower (r=0.57, P=0.035), and no correlations were obtained with 5-ht(6) and 5-HT(7) receptors. It is concluded that the 5-HT receptor mediating endothelium-dependent relaxation of pig pulmonary artery is of the 5-HT(2B) subtype.
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