- Muscarinic acetylcholine receptor binding affinities of pethidine analogs
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A series of pethidine analogs were synthesized and their affinities for the [3H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki = 0.67, 0.37, and 0.38 μM, respectively).
- Lee, Na-Ra,Zhang, Xuan,Darna, Mahesh,Dwoskin, Linda P.,Zheng, Guangrong
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- Duraglutin artificial antigen and preparation method thereof
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The invention provides a duramine artificial antigen and a preparation method thereof. The nitrile group of the 4-phenylpiperidine-4-carbonitrile is ingeniously reduced into the amino group; carboxylgroups capable of being used for crosslinking are introduced, so the characteristic original appearance of a duraglutin main ring is maintained; butanedioic anhydride is introduced, so acetyl functional groups on a duraglutin side chain is maintained on the said chain; the hapten synthesized by the process can maintain the characteristic group original appearance of duraglutin, and the synthesizedcorresponding artificial antigen has good specificity. The preparation process is simple, and the raw material source is not limited; the prepared artificial antigen can be used for animal immunization to obtain a corresponding duraglutin antibody, has strong antibody specificity, can be used in immunoassay, is suitable for research of various duraglutin immunoassay methods, and can be used as akey raw material for production of a duraglutin immunochromatographic kit.
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- THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS
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The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease
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- NAPHTHAMIDE DERIVATIVES AND THEIR USE
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Compounds having the following structure wherein R1, R2, R3, R4, m and n are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically-acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same.
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Page 40; 44-45
(2010/02/06)
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