5-HT2B serotonin receptor

Schmuck K, Ullmer C, Engels P, Lubbert H. Cloning and functional characterization of the human 5-HT2B serotonin receptor. FEBS Lett 1994 342 85-90. 

Fig. 9.8 Examples of rule-of-three compliant molecules that have biological activity better than 10 nM. Under each molecule, the following information is included molecule name, MW, ClogP, the biological activity type, value and target. Target names are as follows D3 and D4 - dopaminergic receptor types 2 and 3 AChE and BChE - acetyl- and butyryl-choline esterases PRa and PRb - progesterone receptor types A and B H] and H3, histamine receptor types 1 and 3 5-HT2a, 5-HT2b, 5-HT2c, 5-HT3, 5-HT4 - serotonin receptor subtypes 2A, 2B, 2C, and types 3 and 4 DAT, NET, 5-HTT - dopamine, norepinephrine and serotonin transporter proteins /X], /x.2, S, ki, ks - opioid receptor types mu-1, mu-2, delta, kappa-1 and kappa-3 5a-Rl and 5o -R2 - 5-alpha-reductase isozymes 1 and 2 Flt-1-fms-like tyrosine kinase receptor.

Ismaiel AM, Dukat M, Nelson DL, Lucaites VL, Glennon RA. Binding of N2-substituted pyrido[4,3-b]indole analogs of spiperone at human 5-HT2A, 5-HT2B, and 5-HT2C serotonin receptors. Med Chem Res 1996 6 197-211. 

The Emergence of Serotonin 5-HT2B Receptors as Drug Antitargets... 

Perhaps, the most significant success of receptorome screening was the implication of the serotonin 5-HT2B receptor in the VHD associated with fenfluramine use. The anorexigen fenfluramine was widely used in the 1990s as an adjunct to diet and exercise, with great success [8]. Originally, racemic fenfluramine was used with... 

Da Prada, M. and Kellermann, O. (2006) Serotonin transport and serotonin transporter-mediated antidepressant recognition are controlled by 5-HT2B receptor signaling in serotonergic neuronal cells. FASEB Journal, 20 (11), 1843-1854. 

HT interacts with a large diversity of G-protein-coupled receptors, namely the 5-HTi,2,4,5,6 and 7 families, and in addition with a ligand-gated cationic channel, 5-HT3. The diversity has been explained by the fact that serotonin is one of the oldest neurotransmitters in evolution. The 5-HTi receptor family (5-HTia,ib,id,ie andiF) couples mainly to Gi/o. 5-1 I I oa, 5-HT2B and 5-HT2C receptors couple to Gq/11. 5-HT4, 5-HT6, and 5-HT7 receptors couple to Gs. The 5-HT5A receptor couples principally to Gi/o. The 5-HTsb receptor seems to occur only in rodents, and no transduction mechanism has been identified. 

De Lucchini S, Marracci S, Nardi I. The serotonin 5-HT2B receptor from the puffer fish Tetraodon fluviatilis cDNA cloning, genomic organization and alternatively spliced variants. Brain Res Mol Brain Res 2001 97 89-93. 

Manivet P, Schneider B, Smith JC, Choi DS, Maroteaux L, Kellermann O. The serotonin binding site of human and murine 5-HT2B receptors molecular modeling and site-directed mutagenesis. J Biol Chem 2002 277 17,170-17,178. 

Etienne N, et al. [The 5-HT2B receptor a main cardio-pulmonary target of serotonin], J Soc Biol 2004 198(l) 22-29. 

Launay JM, Birraux G, Bondoux D, et al. Ras involvement in signal transduction by the serotonin 5-HT2B receptor. J Biol Chem 1996 271 3141-3147. 

Choi DS, Ward SJ, Messaddeq N, Launay JM, Maroteaux L. 5-HT2B receptor-mediated serotonin morphogenetic functions in mouse cranial neural crest and myocardiac cells. Development 1997 124 1745-1755. 

Leung GP, Dun SL, Dun NJ, Wong PY. Serotonin via 5-HT1B and 5-HT2B receptors stimulates anion secretion in the rat epididymal epithelium. J Physiol... 

Nebigil CG, Etienne N, Messaddeq N, Maroteaux L. Serotonin is a novel survival factor of cardiomyocytes mitochondria as a target of 5-HT2B receptor signaling. FASEB J 2003 17 1373-1375. 

Nebigil CG, Etienne N, Schaerlinger B, Hickel P, Launay JM, Maroteaux L. Devel-opmentally regulated serotonin 5-HT2B receptors. Int J Dev Neurosci 2001 19 365-372. 

Choi D-S, Maroteaux L. Immunohistochemical localisation of the serotonin 5-HT2B receptor in mouse gut, cardiovascular system, and brain. FEBS Lett 1996 391 45-51. 

Choi DS, Birraux G, Launay JM, Maroteaux L. The human serotonin 5-HT2B receptor pharmacological link between 5-HT2 and 5-HT1D receptors. FEBS Lett 1994 352 393-399. 

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