Chemical Name:N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazo
l-6-yl]-4-fluorobenzamide hydrochloride
Biological Activity:
Potent,
selective 5-HT1F receptor agonist (EC50 = 3 nM). Displays
> 80-fold selectivity over other 5-HT receptors (Ki values are
0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μM for 5-HT1F, 5-HT1A,
5-HT1B, 5-HT1D, 5-HT1E, 5-HT2B,
5-HT2C, 5-HT2A and 5-HT7 receptors
respectively). Inhibits neurogenic dural inflammation in vivo following i.v.
and oral administration.
Leeet al (1997)
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 Science 61 2117. Ramadanet al (2003) 5-HT1F receptor agonists in acute migraine
treatment: a hypothesis. Cephalalgia 23 776. Goadsby and
Classey (2003) Evidence for serotonin (5-HT)1B, 5-HT1D
and 5-HT1F receptor inhibitory effects on trigeminal neurons with
craniovascular input. Neuroscience 122 491.
Atypical antipsychotic agent that displays 5-HT2A receptor antagonism. Also displays high affinity at D2 receptors (Ki values are 0.4 and 3.13 nM for 5-HT2A and D2 receptors respectively).
