Biological descriptionHighly potent, selective 5-HT2B receptor antagonist (Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors, respectively). Displays antihypertensive activity in vivo.
Chemical name1-[(3,4-Dimethoxyphenyl)methy]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole hydrochloride
Storage instructionsStore at +4°C. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 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.
Russell A et al. 5-Hydroxytryptamine(2B) receptor function is enhanced in the N(omega)-nitro-L-arginine hypertensive rat. J Pharmacol Exp Ther303:179-87 (2002).
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Watts SW & Fink GD 5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats. Am J Physiol276:H944-52 (1999).
Read more (PubMed: 10070078) »
Audia JE et al. Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus. J Med Chem39:2773-80 (1996).
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