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

Homo sapiens

 
 
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Disease relevance of HTR2B

  • Chronic exposure to 5-HT can contribute to pulmonary hypertension through activation of constrictor 5-HT1B receptors and proliferative 5-HT2B receptors, and possibly through direct intracellular effects [1].
  • Finally, we detected expression of the 5-HT2B receptor in spontaneous human and Mastomys natalensis carcinoid tumors and, similar to the 5-HT2B receptor transfected cells, the Mastomys tumor cells are also responsive to serotonin with similar coupling to p21ras activation [2].
  • The selective 5-HT2C/2B receptor antagonist, SB-228357 (0.32-10 mg kg(-1) p.o.) significantly reversed haloperidol-induced catalepsy whereas the 5-HT2A and 5-HT2B receptor antagonists, MDL-100907 (0.003-0.1 mg kg(-1) p.o.) and SB-215505 (0.1-3.2 mg kg(-1) p.o.) respectively did not reverse haloperidol-induced catalepsy [3].
  • Finally, this study reveals the antagonistic roles of 5-HT2A and 5-HT2B receptors in regulating the function of 5-HT1B/1D, a receptor involved in neuropsychiatric disorders and migraine pathogenesis [4].
  • BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats [5].
 

Psychiatry related information on HTR2B

 

High impact information on HTR2B

 

Chemical compound and disease context of HTR2B

  • Our review of the literature strongly suggests that m-CPP and fenfluramine provoke migraine attacks by stimulating, directly or indirectly, the 5HT2C/5HT2B receptors, although there is no total agreement with this interpretation [12].
  • 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 [13].
  • MT-500 (formerly RS-127445) is a 5-HT2B antagonist being developed for the prophylactic treatment of migraine [14].
 

Biological context of HTR2B

  • Sequences of a putative promoter region and splice regions were first elucidated, then sequenced along with HTR2B coding regions [7].
  • Probands from seven families included in a previous genome scan in which one of the strongest linkage findings was to a region including HTR2B, along with two genomic DNA pools of 10 unrelated control subjects and 10 unrelated autism probands were screened [7].
  • We also found novel isoforms for MT2, MRR, and 5HT2B and documented the process of RNA editing for 5HT2C [15].
  • The 5-HT2B receptor has been shown to couple to phosphoinositide hydrolysis as do the other two members of this subfamily when expressed in AV12-664 cells [16].
  • 2. PCR amplification was used to determine the tissue distribution of human 5-HT2B receptor mRNA. mRNA encoding the 5-HT2B receptor was expressed with greatest abundance in human liver and kidney [17].
 

Anatomical context of HTR2B

 

Associations of HTR2B with chemical compounds

  • OBJECTIVE AND METHODS: 5-Hydroxytryptamine (serotonin) receptor 2B (HTR2B) is involved in brain development [6].
  • On the basis of a higher affinity for ketanserin and a lower affinity for yohimbine the human 5-HT2B receptor also appeared to differ from the rat 5-HT2B receptor.(ABSTRACT TRUNCATED AT 250 WORDS)[17]
  • The ligand specificity of the human 5-HT2B receptor (5-HT > ritanserin > SB 204741 > spiperone) was distinct from that of the human 5-HT2A (ritanserin > spiperone > 5-HT > SB 204741) and 5-HT2C (ritanserin > 5-HT > spiperone = SB 204741) receptors [17].
  • The agonist-induced [Ca2+]i mobilization in h-CM cells was potently blocked by the 5-HT2A-selective antagonist M-100907 (IC50=1.2+/-0.4 nM) but less potently by the antagonists for 5-HT2B (RS-127445, IC50>10 microM) and 5-HT2C (RS-102221, IC50=5.8+/-2.3 microM) receptors [20].
  • Cortical perfusion with M100907, or the atypical antipsychotic drug risperidone, but not the 5-HT2B/C ligand SB 206553, also decreased dopamine release induced physiologically by stress [21].
 

Regulatory relationships of HTR2B

  • 1. SB 206553 (5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2 ,3-f]indole) displays a high affinity (pK1 7.9) for the cloned human 5-HT2C receptor expressed in HEK 293 cells and the 5-HT2B receptor (pA2 8.9) as measured in the rat stomach fundus preparation [22].
  • Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones [23].
 

Other interactions of HTR2B

 

Analytical, diagnostic and therapeutic context of HTR2B

  • 3. Northern blot analysis confirmed the presence of 5-HT2B receptor mRNA (a 2.4 kB sized band) in pancreas, liver and kidney [17].
  • RESULTS: By RT-PCR, 5-HT1b, 5-HT2A and 5-HT2B mRNAs were detected in all of the 14 patients [29].
  • As chronic fluoxetine and paroxetine did not reduce brain mCPP levels (determined by HPLC 30 min after 4 mg/kg i.p.) the results suggest that chronic SSRI's, but not desipramine, reduce 5-HT2C/5-HT2B receptor responsivity [30].

References

  1. 5-hydroxytryptamine receptors in the human cardiovascular system. Kaumann, A.J., Levy, F.O. Pharmacol. Ther. (2006) [Pubmed]
  2. Ras involvement in signal transduction by the serotonin 5-HT2B receptor. Launay, J.M., Birraux, G., Bondoux, D., Callebert, J., Choi, D.S., Loric, S., Maroteaux, L. J. Biol. Chem. (1996) [Pubmed]
  3. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Reavill, C., Kettle, A., Holland, V., Riley, G., Blackburn, T.P. Br. J. Pharmacol. (1999) [Pubmed]
  4. Cross-talk between 5-hydroxytryptamine receptors in a serotonergic cell line. Involvement of arachidonic acid metabolism. Tournois, C., Mutel, V., Manivet, P., Launay, J.M., Kellermann, O. J. Biol. Chem. (1998) [Pubmed]
  5. BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats. Kennett, G.A., Ainsworth, K., Trail, B., Blackburn, T.P. Neuropharmacology (1997) [Pubmed]
  6. The human serotonin receptor 2B: coding region polymorphisms and association with vulnerability to illegal drug abuse. Lin, Z., Walther, D., Yu, X.Y., Drgon, T., Uhl, G.R. Pharmacogenetics (2004) [Pubmed]
  7. Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder. Kim, S.J., Veenstra-VanderWeele, J., Hanna, G.L., Gonen, D., Leventhal, B.L., Cook, E.H. Mol. Cell. Probes (2000) [Pubmed]
  8. Serotonin receptor ligands and the treatment of obesity. Vickers, S.P., Dourish, C.T. Current opinion in investigational drugs (London, England : 2000) (2004) [Pubmed]
  9. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. Kantor, S., Jakus, R., Balogh, B., Benko, A., Bagdy, G. Br. J. Pharmacol. (2004) [Pubmed]
  10. 5-HT2B receptor-mediated serotonin morphogenetic functions in mouse cranial neural crest and myocardiac cells. Choi, D.S., Ward, S.J., Messaddeq, N., Launay, J.M., Maroteaux, L. Development (1997) [Pubmed]
  11. The serotonin binding site of human and murine 5-HT2B receptors: molecular modeling and site-directed mutagenesis. Manivet, P., Schneider, B., Smith, J.C., Choi, D.S., Maroteaux, L., Kellermann, O., Launay, J.M. J. Biol. Chem. (2002) [Pubmed]
  12. Headache induced by serotonergic agonists--a key to the interpretation of migraine pathogenesis? Panconesi, A., Sicuteri, R. Cephalalgia : an international journal of headache. (1997) [Pubmed]
  13. 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. Hofmann, C., Penner, U., Dorow, R., Pertz, H.H., Jähnichen, S., Horowski, R., Latté, K.P., Palla, D., Schurad, B. Clinical neuropharmacology. (2006) [Pubmed]
  14. MT-500 (POZEN). Mucke, H.A. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
  15. Functional activity of serotoninergic and melatoninergic systems expressed in the skin. Slominski, A., Pisarchik, A., Zbytek, B., Tobin, D.J., Kauser, S., Wortsman, J. J. Cell. Physiol. (2003) [Pubmed]
  16. Molecular biology of serotonin receptors. Baez, M., Kursar, J.D., Helton, L.A., Wainscott, D.B., Nelson, D.L. Obes. Res. (1995) [Pubmed]
  17. The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Bonhaus, D.W., Bach, C., DeSouza, A., Salazar, F.H., Matsuoka, B.D., Zuppan, P., Chan, H.W., Eglen, R.M. Br. J. Pharmacol. (1995) [Pubmed]
  18. Serotonin receptor subtype mRNA expression in human ocular tissues, determined by RT-PCR. Sharif, N.A., Senchyna, M. Mol. Vis. (2006) [Pubmed]
  19. Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. Kursar, J.D., Nelson, D.L., Wainscott, D.B., Baez, M. Mol. Pharmacol. (1994) [Pubmed]
  20. Serotonin-2 (5-HT2) receptor-mediated signal transduction in human ciliary muscle cells: role in ocular hypotension. Sharif, N.A., Kelly, C.R., Crider, J.Y., Davis, T.L. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics (2006) [Pubmed]
  21. Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex. Pehek, E.A., Nocjar, C., Roth, B.L., Byrd, T.A., Mabrouk, O.S. Neuropsychopharmacology (2006) [Pubmed]
  22. In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. Kennett, G.A., Wood, M.D., Bright, F., Cilia, J., Piper, D.C., Gager, T., Thomas, D., Baxter, G.S., Forbes, I.T., Ham, P., Blackburn, T.P. Br. J. Pharmacol. (1996) [Pubmed]
  23. Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones. Holohean, A.M., Hackman, J.C. Br. J. Pharmacol. (2004) [Pubmed]
  24. Human trabecular meshwork cells express functional serotonin-2A (5HT2A) receptors: role in IOP reduction. Sharif, N.A., Kelly, C.R., McLaughlin, M. Invest. Ophthalmol. Vis. Sci. (2006) [Pubmed]
  25. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Beattie, D.T., Smith, J.A., Marquess, D., Vickery, R.G., Armstrong, S.R., Pulido-Rios, T., McCullough, J.L., Sandlund, C., Richardson, C., Mai, N., Humphrey, P.P. Br. J. Pharmacol. (2004) [Pubmed]
  26. Serotonergic 5-HT2C receptors as a potential therapeutic target for the design antiepileptic drugs. Isaac, M. Current topics in medicinal chemistry. (2005) [Pubmed]
  27. Histological, immunohistochemical, ultrastructural and biochemical study of human gastric composite tumor: expression of the serotonin-2B receptor by the neuroendocrine component. Brouland, J.P., Manivet, P., Brocheriou-Spelle, I., Wassef, M., Le Bodic, M.F., Lavergne, A., Launay, J.M. Endocr. Pathol. (2001) [Pubmed]
  28. 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. Setola, V., Hufeisen, S.J., Grande-Allen, K.J., Vesely, I., Glennon, R.A., Blough, B., Rothman, R.B., Roth, B.L. Mol. Pharmacol. (2003) [Pubmed]
  29. Identification of mRNA for 5-HT1 and 5-HT2 receptor subtypes in human coronary arteries. Ishida, T., Hirata, K., Sakoda, T., Kawashima, S., Akita, H., Yokoyama, M. Cardiovasc. Res. (1999) [Pubmed]
  30. Effect of chronic administration of selective 5-hydroxytryptamine and noradrenaline uptake inhibitors on a putative index of 5-HT2C/2B receptor function. Kennett, G.A., Lightowler, S., de Biasi, V., Stevens, N.C., Wood, M.D., Tulloch, I.F., Blackburn, T.P. Neuropharmacology (1994) [Pubmed]
 
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