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4F 4PP is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 5.3 nM).1 It is selective for 5-HT2A receptors over 5-HT1C receptors (Ki = 620 nM). It inhibits 5-HT-induced currents in Xenopus oocytes expressing human 5-HT2A receptors (IC50 = 5.15 µM).2 Spinal superfusion of 4F 4PP (100 µM) reduces the area of electrically stimulated spinal field potentials in a rat model of neuropathic pain induced by spinal nerve ligation (SNL).3
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1. Ketanserin analogues: Structure-
2. Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-
3. Subtype-