An article Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140) WOS:000460365600004 published article about AGONIST SALVINORIN; PROLACTIN; DYNORPHIN; LY2456302; DOPAMINE; STRESS; 2-METHYL-N-((2′-(PYRROLIDIN-1-YLSULFONYL)BIPHENYL-4-YL)METHYL)PROPAN-1-AMINE; EXPRESSION; DISCOVERY; BINDING in [Guerrero, Miguel; Urbano, Mariangela; Kim, Eun-Kyong; Gamo, Ana M.; Riley, Sean; Abgaryan, Lusine; Leaf, Nora; Brown, Steven J.; Rosen, Hugh; Roberts, Edward] Scripps Res Inst, Dept Mol Med, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA; [Van Orden, Lori Jean] BlackThorn Therapeut Inc, 780 Brannan St, San Francisco, CA 94103 USA; [Xie, Jennifer Y.; Porreca, Frank] Univ Arizona, Dept Pharmacol, Tucson, AZ 85724 USA; [Cameron, Michael D.] Scripps Res Inst, Dept Mol Med, Jupiter, FL 33458 USA; [Xie, Jennifer Y.] Arkansas State Univ, Coll Osteopath Med, New York Inst Technol, Dept Basic Sci, Jonesboro, AR 72446 USA in 2019, Cited 47. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. COA of Formula: C7H13NO2
kappa opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chemistry community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2 H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clinical trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiology.
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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem