15375-56-1Relevant articles and documents
Design, synthesis, and validation of a novel [11c]promethazine pet probe for imaging abeta using autoradiography
Behof, William J.,Boules, Mariam I.,Haynes, Justin R.,Koktysh, Dmitry,Pham, Wellington,Rosenberg, Adam J.,Tantawy, Mohammed N.,Whitmore, Clayton A.
, (2021)
Promethazine, an antihistamine drug used in the clinical treatment of nausea, has been demonstrated the ability to bind Abeta in a transgenic mouse model of Alzheimer’s disease. However, so far, all of the studies were performed in vitro using extracted tissues. In this work, we report the design and synthesis of a novel [11C]promethazine PET radioligand for future in vivo studies. The [11C]promethazine was isolated by RP-HPLC with radiochemical purity >95% and molar activity of 48 TBq/mmol. The specificity of the probe was demonstrated using human hippocampal tissues via autoradiography.
AMYLOID-BINDING COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0078-0079, (2021/01/25)
A method of screening for amyloid-binding compounds, amyloid-binding compounds, and a method of detecting amyloid-β (Abeta) plaques in a subject are disclosed. The method of screening for amyloid-binding compounds includes combining amyloid, a dye, and at least one test compound to form a sample solution; equilibrating the sample solution; measuring a fluorescence signal of the sample solution; and comparing the measured fluorescence signal of the sample to a control; wherein attenuation of the fluorescence signal, as compared to the control, indicates that one or more of the test compounds bind amyloid. The amyloid-binding compound includes a compound detected by the screening method. The method of detecting amyloid-β (Abeta) plaques in a subject includes administering one or more of the amyloid-binding compounds to the subject, and detecting the compound within the subject.
Substituted or unsubstituted benzhydryl heteroalkyl-substituted aminophenol compounds and pharmaceutical compositions thereof
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, (2008/06/13)
Aminophenol derivatives of the following formula (I) STR1 wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.
