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Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

ABSTRACT: The discovery and characterization of a novel chemical series of phosphorothioyl-containing imidazopyridines as potent neuropeptide S receptor antagonists is presented. The synthesis of analogues and their structure-activity relationship with respect to the Gq, Gs, and ERK pathways is detailed. The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addiction disorders.

SUBMITTER: Patnaik S 

PROVIDER: S-EPMC4877059 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature

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Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

Patnaik Samarjit S   Marugan Juan J JJ   Liu Ke K   Zheng Wei W   Southall Noel N   Dehdashti Seameen J SJ   Thorsell Annika A   Heilig Markus M   Bell Lauren L   Zook Michelle M   Eskay Bob B   Brimacombe Kyle R KR   Austin Christopher P CP  

Journal of medicinal chemistry 20131111 22

The discovery and characterization of a novel chemical series of phosphorothioyl-containing imidazopyridines as potent neuropeptide S receptor antagonists is presented. The synthesis of analogues and their structure-activity relationship with respect to the Gq, Gs, and ERK pathways is detailed. The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addict  ...[more]

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