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Article: New findings reported from J.W. Adams and co-authors describe advances in pharmaceuticals.
- Article from:
- Blood Weekly
- Article date:
- November 19, 2009
CopyrightCOPYRIGHT 2009 NewsRX. This material is published under license from the publisher through the Gale Group, Farmington Hills, Michigan. All inquiries regarding rights should be directed to the Gale Group. (Hide copyright information)
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"We have evaluated the receptor pharmacology, antiplatelet activity, and vascular pharmacology of APD791 [3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide] a novel 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist. APD791 displayed high-affinity binding to membranes (K-i = 4.9 nM) and functional inverse agonism of inositol phosphate accumulation (IC50 = 5.2 nM) in human embryonic kidney cells stably expressing the human 5-HT2A receptor," researchers in the United States report (see also Pharmaceuticals).
"In competition binding assays, APD791 was greater than 2000-fold selective for the 5-HT2A receptor versus 5-HT2C and 5-HT2B ...