5-HT2B receptor

5-hidroksitriptaminski (serotoninski) receptor 2B
Identifikatori
Simboli	HTR2B; 5-HT(2B); 5-HT2B
Vanjski ID	OMIM: 601122 MGI: 109323 HomoloGene: 55492 IUPHAR: 5-HT2B GeneCards: HTR2B Gene
Ontologija gena
Molekularna funkcija	• aktivnost rodopsinu-sličnog receptora • receptorska aktivnost • aktivnost serotoninskog receptora
Celularna komponenta	• integralno sa ćelijskom membranom • membrana
Biološki proces	• prenos signala • G-proteinska signalizacija, spregnuta sa IP3 sekundarnim glasnikom (aktivacija fosfolipaze C) • razvoj srca • cirkulacija • pozitivna regulacija I-kapaB kinaze/NF-kapaB kaskade
Pregled RNK izražavanja
	podaci
Ortolozi

edit

5-HT2B receptor (5-hidroksitriptaminski (serotoninski) receptor 2B, HTR2B) je 5-HT₂ receptor. On je kodiran istoimenim humanim genom.^[1]^[2]

Funkcija

5-HT₂ receptori posreduju mnogobrojne centralne i periferne fiziološke funkcije serotonina. Kardiovaskularni efekti obuhvataju kontrakciju krvnih sudova i promene oblika trombocita; efekti na centralni nervni sistem su neuronska senzitizacija na dodirne stimuluse i posredovanje dejstva fenilisopropilamin halucinogena.

5-HT_2B receptor učestvuje u:

CNS: presinaptičkoj inhibiciji, utiče na ponašanje^[3]
Pulmonarna vazokonstrikcija^[4]
5-HT_2B receptor reguliše srčanu strukturu i funkciju. Demonstrirano je da dolazi do abnormalnog srčanog razvoja kod miševa bez 5-HT_2B receptora.^[5] Stimulacija 5-HT_2B receptora može da dovede do patološke proliferacije fibroblasta srčanih sudova,^[6] koja kod hronične prekomerne stimulacije može da dovede do ozbiljne valvulopatije. Za 5-HT_2B receptore je nedavno pokazano da su prekomerno izraženi u human obolelom srcu, i za antagoniste 5-HT_2B receptora je nađeno da sprečavanju angiotenzinom II ili beta-adrenergičkim agonistima-indukovanu patološku srčanu hipertropiju kod miševa.^[7]^[8]^[9]
5-HT_2B receptori regulišu otpuštanje serotonina putem serotoninskih transportera. Oni su važni za normalnu fiziološku regulaciju nivoa serotonina u krvnoj plazmi,^[10] kao i za abnormalno akutno otpuštanje serotonina proizvedenog lekovima kao što je MDMA.^[11]^[12]

Ligandi

Mali broj visoko selektivnih liganda 5-HT_2B receptora je poznat, a isto tako i brojna potentna neselektivna jedinjenja su dostupna, posebno agensi koji deluju i na 5-HT_2C receptor. Istraživanja u ovoj oblasti su bila ograničena kardiotoksičnošću 5HT_2B agonista, i nedostatkom jasno definisane terapeutske primene 5HT_2B antagonista.^[13]

Agonisti

Selektivni

BW-723C86:^[14] znatno funkcionalno selektivan; skoro pun agonist. Anksiolitik in vivo.^[15]
Ro60-0175 ^[14] funkcionalno selektivan u odnosu na 5-HT_2A, potentan agonist 5-HT_2B i 5-HT_2C receptora
VER-3323: selektivan za 5-HT_2B/2C u odnosu na 5-HT_2A
α-Methyl-5-HT - umereno selektivan u odnosu na 5-HT_2A i 5-HT_2C

Neselektivni

Antagonisti

Sarpogrelat (mešoviti 5-HT_2A / 5-HT_2B antagonist)
Lisurid (primarno dopaminski agonist, ali deluje i kao 5-HT_2B antagonist)^[19]
Tegaserod (primarno 5-HT₄ agonist, ali isto tako 5-HT_2B antagonist)^[20]
RS-127,445:^[21] visok afinitet; selektivan u odnosu na druge 5-HTR tipove; oralno bioraspoloživ.
SDZ SER-082: mešoviti 5-HT_2B/2C antagonist
EGIS-7625: visoko selektivan u odnosu na 5-HT_2A^[22]
PRX-08066
SB-200,646
SB-204,741
SB-206,553: mešoviti 5-HT_2B / 5-HT_2C antagonist i PAM na α7 nAChR^[23]
SB-215,505 ^[24]
SB-228,357
LY-272,015

Povezano

5-HT receptor

Reference

↑ „Entrez Gene: HTR_2B 5-hydroxytryptamine (serotonin) receptor 2B”.
↑ Schmuck K, Ullmer C, Engels P, Lübbert H (March 1994). „Cloning and functional characterization of the human 5-HT_2B serotonin receptor”. FEBS Lett. 342 (1): 85–90. DOI:10.1016/0014-5793(94)80590-3. PMID 8143856.
↑ Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). „Serotonin 5-HT_2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro”. J. Neurosci. 28 (11): 2933–40. DOI:10.1523/JNEUROSCI.5723-07.2008. PMID 18337424.
↑ Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L (October 2002). „Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension”. Nat. Med. 8 (10): 1129–35. DOI:10.1038/nm764. PMID 12244304.
↑ Nebigil CG, Hickel P, Messaddeq N, Vonesch JL, Douchet MP, Monassier L, György K, Matz R, Andriantsitohaina R, Manivet P, Launay JM, Maroteaux L (June 2001). „Ablation of serotonin 5-HT(2B) receptors in mice leads to abnormal cardiac structure and function”. Circulation 103 (24): 2973–9. PMID 11413089.
↑ Elangbam CS, Job LE, Zadrozny LM, Barton JC, Yoon LW, Gates LD, Slocum N (August 2008). „5-hydroxytryptamine (5HT)-induced valvulopathy: compositional valvular alterations are associated with 5HT2B receptor and 5HT transporter transcript changes in Sprague-Dawley rats”. Exp. Toxicol. Pathol. 60 (4–5): 253–62. DOI:10.1016/j.etp.2008.03.005. PMID 18511249.
↑ Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L (August 2004). „Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts”. Circulation 110 (8): 969–74. DOI:10.1161/01.CIR.0000139856.20505.57. PMID 15302781.
↑ Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J (August 2008). „Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice”. Hypertension 52 (2): 301–7. DOI:10.1161/HYPERTENSIONAHA.107.105551. PMID 18591460.
↑ Jaffré F, Bonnin P, Callebert J, Debbabi H, Setola V, Doly S, Monassier L, Mettauer B, Blaxall BC, Launay JM, Maroteaux L (November 2008). „Serotonin and Angiotensin Receptors in Cardiac Fibroblasts Coregulate Adrenergic-Dependent Cardiac Hypertrophy”. Circ. Res. 104 (1): 113–23. DOI:10.1161/CIRCRESAHA.108.180976. PMID 19023134.
↑ Callebert J, Esteve JM, Hervé P, Peoc'h K, Tournois C, Drouet L, Launay JM, Maroteaux L (May 2006). „Evidence for a control of plasma serotonin levels by 5-hydroxytryptamine(2B) receptors in mice”. J. Pharmacol. Exp. Ther. 317 (2): 724–31. DOI:10.1124/jpet.105.098269. PMID 16461587.
↑ Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). „Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro”. J. Neurosci. 28 (11): 2933–40. DOI:10.1523/JNEUROSCI.5723-07.2008. PMID 18337424.
↑ Diaz SL, Maroteaux L (January 2011). „Implication of 5-HT(2B) receptors in the serotonin syndrome”. Neuropharmacology. DOI:10.1016/j.neuropharm.2011.01.025. PMID 21277875.
↑ Schuhmacher M (2007). [Chiral arylmethoxytryptamines as 5-HT_2B-receptor antagonists: synthesis, analysis and in-vitro pharmacology (German)]. Ph.D. Dissertation. University of Regensburg. pp. pages 6–17. Arhivirano iz originala na datum 2011-07-18. Pristupljeno 2008-08-11.
↑ ^14,0 ^14,1 ^14,2 Porter RH, Benwell KR, Lamb H, et al. (1999). „Functional characterization of agonists at recombinant human 5-HT_2A, 5-HT_2B and 5-HT_2C receptors in CHO-K1 cells”. Br. J. Pharmacol. 128 (1): 13–20. DOI:10.1038/sj.bjp.0702751. PMC 1571597. PMID 10498829.
↑ Kennett GA, Trail B, Bright F (December 1998). „Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated”. Neuropharmacology 37 (12): 1603–10. DOI:10.1016/S0028-3908(98)00115-4. PMID 9886683.
↑ ^16,0 ^16,1 Setola, Vincent; Sandra J Hufeisen, K Jane Grande-Allen, Ivan Vesely, Richard A Glennon, Bruce Blough, Richard B Rothman, Bryan L Roth (2003-01-07). „3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro”. Molecular pharmacology 63 (6): 1223–1229. DOI:10.1124/mol.63.6.1223. PMID 12761331.
↑ Ray TS; Manzoni, Olivier Jacques (2010). Manzoni, Olivier Jacques. ur. „Psychedelics and the human receptorome”. PLoS ONE 5 (2): e9019. DOI:10.1371/journal.pone.0009019. PMC 2814854. PMID 20126400.
↑ Görnemann T, Hübner H, Gmeiner P, et al. (2008). „Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine_2B and 5-Hydroxytryptamine_2A receptors”. J. Pharmacol. Exp. Ther. 324 (3): 1136–45. DOI:10.1124/jpet.107.133165. PMID 18096760.
↑ Hofmann C, Penner U, Dorow R, Pertz HH, Jähnichen S, Horowski R, Latté KP, Palla D, Schurad B (2006). „Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis”. Clin Neuropharmacol 29 (2): 80–6. DOI:10.1097/00002826-200603000-00005. PMID 16614540. Arhivirano iz originala na datum 2012-03-11. Pristupljeno 2014-05-02.
↑ Beattie DT, Smith JA, Marquess D, et al. (November 2004). „The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo”. Br. J. Pharmacol. 143 (5): 549–60. DOI:10.1038/sj.bjp.0705929. PMC 1575425. PMID 15466450.
↑ Bonhaus DW, Flippin LA, Greenhouse RJ, et al. (1999). „RS-127445: a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist”. Br. J. Pharmacol. 127 (5): 1075–82. DOI:10.1038/sj.bjp.0702632. PMC 1566110. PMID 10455251.
↑ Kovács A, Gacsályi I, Wellmann J, et al. (2003). „Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist”. Cardiovasc Drugs Ther 17 (5–6): 427–34. DOI:10.1023/B:CARD.0000015857.96371.43. PMID 15107597.
↑ Dunlop J, Lock T, Jow B, et al. (March 2009). „Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b'di pyrrole-1(2H)-carboxamide)”]. J. Pharmacol. Exp. Ther. 328 (3): 766–76. DOI:10.1124/jpet.108.146514. PMID 19050173.
↑ Reavill C, Kettle A, Holland V, Riley G, Blackburn TP (February 1999). „Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist”. Br. J. Pharmacol. 126 (3): 572–4. DOI:10.1038/sj.bjp.0702350. PMC 1565856. PMID 10188965.

Literatura

Raymond JR, Mukhin YV, Gelasco A, et al. (2002). „Multiplicity of mechanisms of serotonin receptor signal transduction”. Pharmacol. Ther. 92 (2–3): 179–212. DOI:10.1016/S0163-7258(01)00169-3. PMID 11916537.
Bonhaus DW, Bach C, DeSouza A, et al. (1995). „The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors”. Br. J. Pharmacol. 115 (4): 622–8. PMC 1908489. PMID 7582481.
Choi DS, Birraux G, Launay JM, Maroteaux L (1994). „The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors”. FEBS Lett. 352 (3): 393–9. DOI:10.1016/0014-5793(94)00968-6. PMID 7926008.
Kursar JD, Nelson DL, Wainscott DB, Baez M (1994). „Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor”. Mol. Pharmacol. 46 (2): 227–34. PMID 8078486.
Schmuck K, Ullmer C, Engels P, Lübbert H (1994). „Cloning and functional characterization of the human 5-HT2B serotonin receptor”. FEBS Lett. 342 (1): 85–90. DOI:10.1016/0014-5793(94)80590-3. PMID 8143856.
Launay JM, Birraux G, Bondoux D, et al. (1996). „Ras involvement in signal transduction by the serotonin 5-HT2B receptor”. J. Biol. Chem. 271 (6): 3141–7. DOI:10.1074/jbc.271.6.3141. PMID 8621713.
Le Coniat M, Choi DS, Maroteaux L, et al. (1996). „The 5-HT2B receptor gene maps to 2q36.3-2q37.1”. Genomics 32 (1): 172–3. DOI:10.1006/geno.1996.0101. PMID 8786115.
Kim SJ, Veenstra-VanderWeele J, Hanna GL, et al. (2000). „Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder”. Mol. Cell. Probes 14 (1): 47–52. DOI:10.1006/mcpr.1999.0281. PMID 10722792.
Manivet P, Mouillet-Richard S, Callebert J, et al. (2000). „PDZ-dependent activation of nitric-oxide synthases by the serotonin 2B receptor”. J. Biol. Chem. 275 (13): 9324–31. DOI:10.1074/jbc.275.13.9324. PMID 10734074.
Becamel C, Figge A, Poliak S, et al. (2001). „Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1”. J. Biol. Chem. 276 (16): 12974–82. DOI:10.1074/jbc.M008089200. PMID 11150294.
Manivet P, Schneider B, Smith JC, et al. (2002). „The serotonin binding site of human and murine 5-HT2B receptors: molecular modeling and site-directed mutagenesis”. J. Biol. Chem. 277 (19): 17170–8. DOI:10.1074/jbc.M200195200. PMID 11859080.
Borman RA, Tilford NS, Harmer DW, et al. (2002). „5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro”. Br. J. Pharmacol. 135 (5): 1144–51. DOI:10.1038/sj.bjp.0704571. PMC 1573235. PMID 11877320.
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences”. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. DOI:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
Matsuda A, Suzuki Y, Honda G, et al. (2003). „Large-scale identification and characterization of human genes that activate NF-kappaB and MAPK signaling pathways”. Oncogene 22 (21): 3307–18. DOI:10.1038/sj.onc.1206406. PMID 12761501.
Slominski A, Pisarchik A, Zbytek B, et al. (2003). „Functional activity of serotoninergic and melatoninergic systems expressed in the skin”. J. Cell. Physiol. 196 (1): 144–53. DOI:10.1002/jcp.10287. PMID 12767050.
Gerhard DS, Wagner L, Feingold EA, et al. (2004). „The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)”. Genome Res. 14 (10B): 2121–7. DOI:10.1101/gr.2596504. PMC 528928. PMID 15489334.
Lin Z, Walther D, Yu XY, et al. (2005). „The human serotonin receptor 2B: coding region polymorphisms and association with vulnerability to illegal drug abuse”. Pharmacogenetics 14 (12): 805–11. DOI:10.1097/00008571-200412000-00003. PMID 15608559.
Hillier LW, Graves TA, Fulton RS, et al. (2005). „Generation and annotation of the DNA sequences of human chromosomes 2 and 4”. Nature 434 (7034): 724–31. DOI:10.1038/nature03466. PMID 15815621.

Vanjske veze

„5-HT_2B”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2017-02-02.

[entrez_3357-1] „Entrez Gene: HTR_2B 5-hydroxytryptamine (serotonin) receptor 2B”.

[pmid8143856-2] Schmuck K, Ullmer C, Engels P, Lübbert H (March 1994). „Cloning and functional characterization of the human 5-HT_2B serotonin receptor”. FEBS Lett. 342 (1): 85–90. DOI:10.1016/0014-5793(94)80590-3. PMID 8143856.

[pmid18337424-3] Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). „Serotonin 5-HT_2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro”. J. Neurosci. 28 (11): 2933–40. DOI:10.1523/JNEUROSCI.5723-07.2008. PMID 18337424.

[pmid12244304-4] Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L (October 2002). „Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension”. Nat. Med. 8 (10): 1129–35. DOI:10.1038/nm764. PMID 12244304.

[pmid11413089-5] Nebigil CG, Hickel P, Messaddeq N, Vonesch JL, Douchet MP, Monassier L, György K, Matz R, Andriantsitohaina R, Manivet P, Launay JM, Maroteaux L (June 2001). „Ablation of serotonin 5-HT(2B) receptors in mice leads to abnormal cardiac structure and function”. Circulation 103 (24): 2973–9. PMID 11413089.

[pmid18511249-6] Elangbam CS, Job LE, Zadrozny LM, Barton JC, Yoon LW, Gates LD, Slocum N (August 2008). „5-hydroxytryptamine (5HT)-induced valvulopathy: compositional valvular alterations are associated with 5HT2B receptor and 5HT transporter transcript changes in Sprague-Dawley rats”. Exp. Toxicol. Pathol. 60 (4–5): 253–62. DOI:10.1016/j.etp.2008.03.005. PMID 18511249.

[pmid15302781-7] Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L (August 2004). „Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts”. Circulation 110 (8): 969–74. DOI:10.1161/01.CIR.0000139856.20505.57. PMID 15302781.

[pmid18591460-8] Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J (August 2008). „Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice”. Hypertension 52 (2): 301–7. DOI:10.1161/HYPERTENSIONAHA.107.105551. PMID 18591460.

[pmid19023134-9] Jaffré F, Bonnin P, Callebert J, Debbabi H, Setola V, Doly S, Monassier L, Mettauer B, Blaxall BC, Launay JM, Maroteaux L (November 2008). „Serotonin and Angiotensin Receptors in Cardiac Fibroblasts Coregulate Adrenergic-Dependent Cardiac Hypertrophy”. Circ. Res. 104 (1): 113–23. DOI:10.1161/CIRCRESAHA.108.180976. PMID 19023134.

[pmid16461587-10] Callebert J, Esteve JM, Hervé P, Peoc'h K, Tournois C, Drouet L, Launay JM, Maroteaux L (May 2006). „Evidence for a control of plasma serotonin levels by 5-hydroxytryptamine(2B) receptors in mice”. J. Pharmacol. Exp. Ther. 317 (2): 724–31. DOI:10.1124/jpet.105.098269. PMID 16461587.

[autogenerated1-11] Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). „Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro”. J. Neurosci. 28 (11): 2933–40. DOI:10.1523/JNEUROSCI.5723-07.2008. PMID 18337424.

[pmid21277875-12] Diaz SL, Maroteaux L (January 2011). „Implication of 5-HT(2B) receptors in the serotonin syndrome”. Neuropharmacology. DOI:10.1016/j.neuropharm.2011.01.025. PMID 21277875.

[Schuhmacher-13] Schuhmacher M (2007). [Chiral arylmethoxytryptamines as 5-HT_2B-receptor antagonists: synthesis, analysis and in-vitro pharmacology (German)]. Ph.D. Dissertation. University of Regensburg. pp. pages 6–17. Arhivirano iz originala na datum 2011-07-18. Pristupljeno 2008-08-11.

[pmid10498829-14] 14,0 ^14,1 ^14,2 Porter RH, Benwell KR, Lamb H, et al. (1999). „Functional characterization of agonists at recombinant human 5-HT_2A, 5-HT_2B and 5-HT_2C receptors in CHO-K1 cells”. Br. J. Pharmacol. 128 (1): 13–20. DOI:10.1038/sj.bjp.0702751. PMC 1571597. PMID 10498829.

[pmid9886683-15] Kennett GA, Trail B, Bright F (December 1998). „Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated”. Neuropharmacology 37 (12): 1603–10. DOI:10.1016/S0028-3908(98)00115-4. PMID 9886683.

[MDx-16] 16,0 ^16,1 Setola, Vincent; Sandra J Hufeisen, K Jane Grande-Allen, Ivan Vesely, Richard A Glennon, Bruce Blough, Richard B Rothman, Bryan L Roth (2003-01-07). „3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro”. Molecular pharmacology 63 (6): 1223–1229. DOI:10.1124/mol.63.6.1223. PMID 12761331.

[pmid20126400-17] Ray TS; Manzoni, Olivier Jacques (2010). Manzoni, Olivier Jacques. ur. „Psychedelics and the human receptorome”. PLoS ONE 5 (2): e9019. DOI:10.1371/journal.pone.0009019. PMC 2814854. PMID 20126400.

[pmid18096760-18] Görnemann T, Hübner H, Gmeiner P, et al. (2008). „Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine_2B and 5-Hydroxytryptamine_2A receptors”. J. Pharmacol. Exp. Ther. 324 (3): 1136–45. DOI:10.1124/jpet.107.133165. PMID 18096760.

[pmid16614540-19] Hofmann C, Penner U, Dorow R, Pertz HH, Jähnichen S, Horowski R, Latté KP, Palla D, Schurad B (2006). „Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis”. Clin Neuropharmacol 29 (2): 80–6. DOI:10.1097/00002826-200603000-00005. PMID 16614540. Arhivirano iz originala na datum 2012-03-11. Pristupljeno 2014-05-02.

[20] Beattie DT, Smith JA, Marquess D, et al. (November 2004). „The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo”. Br. J. Pharmacol. 143 (5): 549–60. DOI:10.1038/sj.bjp.0705929. PMC 1575425. PMID 15466450.

[pmid10455251-21] Bonhaus DW, Flippin LA, Greenhouse RJ, et al. (1999). „RS-127445: a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist”. Br. J. Pharmacol. 127 (5): 1075–82. DOI:10.1038/sj.bjp.0702632. PMC 1566110. PMID 10455251.

[pmid15107597-22] Kovács A, Gacsályi I, Wellmann J, et al. (2003). „Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist”. Cardiovasc Drugs Ther 17 (5–6): 427–34. DOI:10.1023/B:CARD.0000015857.96371.43. PMID 15107597.

[pmid19050173-23] Dunlop J, Lock T, Jow B, et al. (March 2009). „Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b'di pyrrole-1(2H)-carboxamide)”]. J. Pharmacol. Exp. Ther. 328 (3): 766–76. DOI:10.1124/jpet.108.146514. PMID 19050173.

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