In Vitro and in Vivo Metabolism of Lu-AMBA, a GRP-Receptor Binding Compound, and the Synthesis and Characterization of Its Metabolites

2009 ◽  
Vol 20 (6) ◽  
pp. 1171-1178 ◽  
Author(s):  
Karen E. Linder ◽  
Edmund Metcalfe ◽  
Thangavel Arunachalam ◽  
Jianqing Chen ◽  
Stephen M. Eaton ◽  
...  
2009 ◽  
Vol 114 (2) ◽  
pp. 734-740 ◽  
Author(s):  
Anthony W. Musumeci ◽  
Tara L. Schiller ◽  
Zhi Ping Xu ◽  
Rodney F. Minchin ◽  
Darren J. Martin ◽  
...  

2011 ◽  
Vol 100 (11) ◽  
pp. 4877-4887 ◽  
Author(s):  
İpek Özcan ◽  
Kawthar Bouchemal ◽  
Freimar Segura‐Sánchez ◽  
Özgen Özer ◽  
Tamer Güneri ◽  
...  

2010 ◽  
Vol 63 (1) ◽  
pp. 116 ◽  
Author(s):  
Ben Capuano ◽  
Ian T. Crosby ◽  
Fiona M. McRobb ◽  
Anna Podloucka ◽  
David A. Taylor ◽  
...  

Herein we report the synthesis, characterization, and preliminary pharmacological activity of a new series of substituted 4′-phenoxypropyl tricyclic analogues of clozapine as potential antipsychotic agents for the treatment of schizophrenia. The lead compound (3) for this investigation was designed based on a revised model derived from the structural hybridization of the commercial therapeutics clozapine (1) and haloperidol (2). The compounds described in this paper probe the biochemical effects of introducing a variety of electron-withdrawing and electron-donating substituents with the primary focus on the para-position of the introduced distal aromatic ring. The target compounds were readily prepared in three steps using the key intermediate lactam (8-chloro-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepine-11-one, 9), piperazine and commercially available substituted phenols. The chemistry and structural characterization of this series of substituted 4′-phenoxypropyl analogues of clozapine are described. Preliminary in vitro results on the pharmacological effects of the ring substituents on affinity for dopamine D4 and serotonin 5-HT2A receptors are discussed. Psychosis-related in vivo animal behavioural data for compounds identified with potential from the receptor binding screen are also presented.


Life Sciences ◽  
1988 ◽  
Vol 43 (14) ◽  
pp. 1151-1160 ◽  
Author(s):  
Robert D. McQuade ◽  
Richard Chipkin ◽  
Nordine Amlaiky ◽  
Marc Caron ◽  
Louis Iorio ◽  
...  

2012 ◽  
Vol 40 (7) ◽  
pp. 1345-1356 ◽  
Author(s):  
Hong Su ◽  
David W. Boulton ◽  
Anthony Barros ◽  
Lifei Wang ◽  
Kai Cao ◽  
...  

RSC Advances ◽  
2017 ◽  
Vol 7 (48) ◽  
pp. 29998-30007 ◽  
Author(s):  
Xijing Liu ◽  
Peijiang Zhou ◽  
Hongju Zhan ◽  
Hongyu Liu ◽  
Jianwei Zhang ◽  
...  

In this article, highly photoluminescent near-infrared (NIR)-emitting quantum dots (QDs) were directly synthesized in water by a fast, inexpensive and facile method.


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