Biological descriptionSelective 5-HT2B receptor antagonist. High affinity for 5-HT2B receptors (pKi = 7.85), some activity at 5-HT2C receptors (pKi = 5.8).
Storage instructionsStore at Room Temperature. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in ethanol to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Dergacheva O et al. 5-HT(2) receptor subtypes mediate different long-term changes in GABAergic activity to parasympathetic cardiac vagal neurons in the nucleus ambiguus. Neuroscience149:696-705 (2007).
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Shingala JR & Balaraman R Antihypertensive effect of 5-HT1A agonist buspirone and 5-HT2B antagonists in experimentally induced hypertension in rats. Pharmacology73:129-39 (2005).
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Knowles ID & Ramage AG Evidence that activation of central 5-HT(2B) receptors causes renal sympathoexcitation in anaesthetized rats. Br J Pharmacol129:177-83 (2000).
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Forbes IT et al. N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist. J Med Chem38:855-7 (1995).
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