PF-05212377 (SAM-760; WYE-103760) is an orally available, high-affinity, selective 5-hydroxytryptamine (5-HT; serotonin) receptor 5-HT6 antagonist (Ki/IC50 = 0.53/1.06 nM against 3 nM [3H]-LSD for binding human 5-HT6). PF-05212377 modulates glutamate and acetylcholine release in the cerebral cortex and hippocampus in rodents with in vivo pro-cognitive efficacy.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Alzheimer's research & therapy, 10(1), 38-38 (2018-04-07)
Symptomatic benefits have been reported for 5-HT6 receptor antagonists in Alzheimer's disease (AD) trials. SAM-760 is a potent and selective 5-HT6 receptor antagonist that has demonstrated central 5-HT6 receptor saturation in humans at a dose of 30 mg. This was
Drug metabolism and disposition: the biological fate of chemicals, 46(7), 934-942 (2018-04-27)
SAM-760 [(2-methyl-1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-benzo[d]imidazole)], a 5HT6 antagonist, was investigated in humans for the treatment of Alzheimer's disease. In liver microsomes and recombinant cytochrome P450 (P450) isozymes, SAM-760 was predominantly metabolized by CYP3A (∼85%). Based on these observations and an expectation of a
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