Biological descriptionSelective, potent, full 5-HT1F agonist (EC50 = 3 nM). Selectivity is 80-fold greater than for other 5-HT receptor subtypes, Ki values are 0.53 (5-HT1A), 0.549 (5-HT1B), 0.575 (5-HT1D), 1.415 (5-HT1E), 3.935 (5-HT2A), 1.695 (5-HT2B), 3.499 (5-HT2C) and 4.851 (5-HT7). Able to reduce central sensitization and dural inflammation in vivo.
General notesSold under license from Eli Lilly and company
Chemical nameN-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide hydrochloride
Storage instructionsStore at +4°C. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in water to 5 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.
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Mitsikostas DD et al. 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia22:384-94 (2002).
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Phebus LA et al. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci61:2117-26 (1997).
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