Pharmacology letter Accelerated communicationSR 142801, The first potent non-peptide antagonist of the tachykinin NK3 receptor
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Neurokinin receptors and their implications in various autoimmune diseases
2021, Current Research in ImmunologyScaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact
2019, Bioorganic and Medicinal ChemistryCitation Excerpt :The fused piperidine derivatives 4b–d were synthesized from a common substrate, 3-oxopiperidine derivative 7 (Scheme 1B). Reaction of ketone 7 with 1-azido-4-nitrobenzene provided 1,2,3-triazole 8.25 N1-arylation on triazole 8 proceeded by treatment of triazole 8 with 2-chloroquinoline in the presence of i-Pr2NEt to afford the desired 1-(quinolin-2-yl)triazole 9 after separation from a mixture of regioisomers.
Evidence for involvement of NK<inf>3</inf> receptors in the anxiogenic-like effect of SP6-11(C-terminal), a metabolite of substance P, in rats evaluated in the elevated plus-maze
2016, Behavioural Brain ResearchCitation Excerpt :Species differences in the pharmacological characteristics of NK3 receptor antagonists further complicate investigations in animal models. For instance, the NK3 antagonist used in the current study, SR142801, is a selective and potent non-peptide antagonist at the human NK3 receptor (pA2 = 9.15) [62], but shows some species differences in binding to NK3 receptors. Firstly, SR1421801 has the highest affinity for the guinea pig NK3 receptor with a Ki value of 0.11 nM as compared to the rat (15 nM), gerbil (0.42 nM) and human (0.21 nM) NK3 receptors [61].
Design and synthesis of potential dual NK<inf>1</inf>/NK<inf>3</inf> receptor antagonists
2014, Bioorganic and Medicinal Chemistry Letters