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Biological Activity:
Potent, selective and p.o. active 5-HT2A antagonist; functionally also an inverse agonist of 5-HT2A receptor; no affinity to dopamine, histamine and adrenergic receptors; therapeutic agent for the treatment of insomnia
References: online 1
M. Rinaldi-Carmona et al. Biochemical and Pharmacological Properties of SR 46349B, a New Potent and Selective 5-Hydroxytryptamine2 Receptor Antagonist. JPET 1992, 262(2), 759-768. [online]
F Chaouloff et al. Repeated DOI and SR 46349B treatments do not affect elevated plus-maze anxiety despite opposite effects on cortical 5-HT2A receptors. Eur J Pharmacol. 1997, 334(1), 25-29. [online]
BR Teergarden et al. 5-HT2A Inverse-Agonists for the Treatment of Insomnia. Current Topics Med. Chem. 2008, 8(11), 969–976. [abstract]
Chemical Name: (1Z,2E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime hemifumarate
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