22932-27-0Relevant articles and documents
Novel potent and selective θ ligands: Evaluation of their agonist and antagonist properties
Marrazzo, Agostino,Cobos, Enrique J.,Parenti, Carmela,Aricò, Giuseppina,Marrazzo, Giuseppina,Ronsisvalle, Simone,Pasquinucci, Lorella,Prezzavento, Orazio,Colabufo, Nicola A.,Contino, Marialessandra,González, Luis G.,Scoto, Giovanna M.,Ronsisvalle, Giuseppe
supporting information; experimental part, p. 3669 - 3673 (2011/06/28)
Novel enantiomers and diastereoisomers structurally related to θ ligand (+)-MR200 were synthesized to improve θ1/θ 2 subtype selectivity. The selective θ1 ligand (-)-8 showed an antagonist profile determined by phenytoin differential modulation of binding affinity in vitro, confirmed in vivo by an increase of κ opioid analgesia. The θ2 ligand (-)-9 displayed agonist properties in an in vitro isolated organ bath assay and antiproliferative effects on LNCaP and PC3 prostate cancer cell lines.
Azabicycloalkane derivatives for use as serotonin reuptake inhibitors and 5ht2a antagonists
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Example 50, (2010/01/31)
The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, Y, U, W, k, A, E, V, R4 and R5 are as defined herein, pharmaceutical compositions thereof, and methods of use thereof in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of compounds of formula (I) and intermediates useful therefor.
8-azabicyclo[3.2.1.]oct-2-ene derivatives, their preparation and use
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, (2008/06/13)
PCT No. PCT/EP96/04449 Sec. 371 Date May 18, 1998 Sec. 102(e) Date May 18, 1998 PCT Filed Oct. 11, 1996 PCT Pub. No. WO97/13770 PCT Pub. Date Apr. 17, 1997A compound having the formula, or any of its enantiomers or any mixture thereof, or a pharmaceutical