139754-93-1Relevant academic research and scientific papers
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ1Receptor Antagonists for the Treatment of Pain
García, Mónica,Llorente, Virginia,Garriga, Lourdes,Christmann, Ute,Rodríguez-Escrich, Sergi,Virgili, Marina,Fernández, Bego?a,Bordas, Magda,Ayet, Eva,Burgue?o, Javier,Pujol, Marta,Dordal, Albert,Portillo-Salido, Enrique,Gris, Georgia,Vela, José Miguel,Almansa, Carmen
, p. 10139 - 10154 (2021/07/28)
A new series of propionamide derivatives was developed as dual μ-opioid receptor agonists and σ1receptor antagonists. Modification of a high-throughput screening hit originated a series of piperazinylcycloalkylmethyl propionamides, which were e
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1
Cioffi, Christopher L.,Liu, Shuang,Wolf, Mark A.,Guzzo, Peter R.,Sadalapure, Kashinath,Parthasarathy, Visweswaran,Loong, David T. J.,Maeng, Jun-Ho,Carulli, Edmund,Fang, Xiao,Karunakaran, Kalesh,Matta, Lakshman,Choo, Sok Hui,Panduga, Shailijia,Buckle, Ronald N.,Davis, Randall N.,Sakwa, Samuel A.,Gupta, Priya,Sargent, Bruce J.,Moore, Nicholas A.,Luche, Michele M.,Carr, Grant J.,Khmelnitsky, Yuri L.,Ismail, Jiffry,Chung, Mark,Bai, Mei,Leong, Wei Yee,Sachdev, Nidhi,Swaminathan, Srividya,Mhyre, Andrew J.
, p. 8473 - 8494 (2016/10/03)
We previously disclosed the discovery of rationally designed N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1), represented by analogues 10 and 11. We describe herein further structure-activit
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor
Chen, Caroline W.,Tran, Joe A.,Fleck, Beth A.,Tucci, Fabio C.,Jiang, Wanlong,Chen, Chen
, p. 6825 - 6831 (2008/09/16)
A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were i
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor
Tran, Joseph A.,Pontillo, Joseph,Arellano, Melissa,Fleck, Beth A.,Tucci, Fabio C.,Marinkovic, Dragan,Chen, Caroline W.,Saunders, John,Foster, Alan C.,Chen, Chen
, p. 3434 - 3438 (2007/10/03)
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity (Ki) of 4.2 and 1100 nM at MC4R and MC3R, respectively.
LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO
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Page 40, (2010/02/07)
Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts
Ligands of melanocortin receptors and compositions and methods related thereto
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, (2008/06/13)
Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein A, m, n, R1, R2, R3a, R3b, R4, R5, R6 W1, W2, W3, W4, Y1, Y2, Y3 and Y4 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
Phencyclidine and phencyclidine metabolites assay, tracers, immunogens and antibodies
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, (2008/06/13)
The present invention is directed to a fluorescence polarization assay for phencyclidine and phencyclidine derivatives, to the various components needed for preparing and carrying out such an assay, and to methods of making these components. Specifically, tracers, immunogens and antibodies are disclosed, as well as methods for making them. The tracers and the immunogens are made from substituted phencyclidine compounds. A fluorescein moiety is included in the tracer, while a poly(amino acid) forms a part of the immunogen. The assay is conducted by measuring the degree of polarization retention of plane polarized light that has been passed through a sample containing antiserum and tracer.
Phencyclidine and phencyclidine metabolites assay, tracers, immunogens, antibodies and reagent kit
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, (2008/06/13)
The present invention is directed to a fluorescence polarization assay for phencyclidine and phencyclidine derivatives, to the various components needed for preparting and carrying out such an assay, and to methods of making these components. Specifically, tracers, immunogens and antibodies are disclosed, as well as methods for making them, and a reagent kit containing them. The tracers and the immunogens are made from substituted phencyclidine compounds. A fluorescein moiety is included in the tracer, while a poly(amino acid) forms a part of the immunogen. The assay is conducted by measuring the degree of polarization retention of plane polarized light that has been passed through a sample containing antiserum and tracer.
