55099-31-5Relevant articles and documents
Amantadine hapten and preparing method and application thereof
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Paragraph 0065; 0068; 0071, (2019/10/01)
The invention relates to the field of preparation of haptens, in particular to an amantadine hapten and a preparing method and application thereof. When the amantadine hapten is prepared, amantadine and bromine polyhydroxyalkanoate serve as raw materials, and through a nucleophilic substitution reaction, amidogen groups in amantadine molecules are connected with the bromine polyhydroxyalkanoate; then through a hydrolysis reaction, carboxyl groups are introduced to obtain a corresponding product. The amantadine hapten can be coupled with a carrier protein to prepare an artificial antigen, the artificial antigen is prepared into a monoclonal antibody or a polyclonal antibody through an immune animal, and then the monoclonal antibody or the polyclonal antibody can be used for quickly detecting residues of the amantadine in an animal product.
Synthesis and Characterization of Novel Acyl-Glycine Inhibitors of GlyT2
Mostyn, Shannon N.,Carland, Jane E.,Shimmon, Susan,Ryan, Renae M.,Rawling, Tristan,Vandenberg, Robert J.
, p. 1949 - 1959 (2017/09/26)
It has been demonstrated previously that the endogenous compound N-arachidonyl-glycine inhibits the glycine transporter GlyT2, stimulates glycinergic neurotransmission, and provides analgesia in animal models of neuropathic and inflammatory pain. However, it is a relatively weak inhibitor with an IC50 of 9 μM and is subject to oxidation via cyclooxygenase, limiting its therapeutic value. In this paper we describe the synthesis and testing of a novel series of monounsaturated C18 and C16 acyl-glycine molecules as inhibitors of the glycine transporter GlyT2. We demonstrate that they are up to 28 fold more potent that N-arachidonyl-glycine with no activity at the closely related GlyT1 transporter at concentrations up to 30 μM. This novel class of compounds show considerable promise as a first generation of GlyT2 transport inhibitors.
Antiproliferative and antimigratory actions of synthetic long chain n-3 monounsaturated fatty acids in breast cancer cells that overexpress cyclooxygenase-2
Cui, Pei H.,Kirsi Bourget, Tristan Rawing,Kim, Terry,Duke, Colin C.,Doddareddy, Munikumar R.,Hibbs, David E.,Zhou, Fanfan,Tattam, Bruce N.,Petrovic, Nenad,Murray, Michael
, p. 7163 - 7172 (2012/11/07)
Cyclooxygenase-2 (COX-2) is overexpressed in many human cancers and converts the n-6 polyunsaturated fatty acid (PUFA) arachidonic acid to prostaglandin E2 (PGE2), which drives tumorigenesis; in contrast, n-3 PUFA inhibit tumorigenesis. We tested the hypothesis that these antitumor actions of n-3 PUFA may involve the n-3 olefinic bond. n-3 Monounsaturated fatty acids (MUFAs) of chain length C16-C22 were synthesized and evaluated in MDA-MB-468 breast cancer cells that stably overexpressed COX-2 (MDA-COX-2 cells). Longer chain (C19-C22) n-3 MUFAs inhibited proliferation, activated apoptosis, decreased PGE2 formation, and decreased cell invasion; C16-C18 analogues were less active. Molecular modeling showed that interactions of Arg120, Tyr355, and several hydrophobic amino acid residues in the COX-2 active site with C19-C22 MUFA analogues were favored. Thus, longer-chain n-3 MUFAs may be prototypes of novel anticancer agents that decrease the formation of PGE2 in tumor cells that contain high levels of COX-2.
4-[diaryl)hydroxymethyl]-1-piperidinealkylcarboxylic acids, salts and esters useful in the treatment of allergic disorders
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, (2008/06/13)
Novel compounds useful in the treatment of allergic disorders and having the formula: STR1 where Ar and Ar1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O? M≈ m,--O--loweralkyl, --O--Aryl, or NR1 R2 (R1, R2 =H, loweralkyl, aryl) are herein disclosed.
