847553-89-3

Usage

Uses

Used in Pharmaceutical Industry:
SHA 68 is used as a selective neuropeptide S antagonist for the development of novel therapeutic agents targeting the NPSR. Its high selectivity and affinity for the NPSR isoforms make it a valuable tool in the research and development of drugs for the treatment of neurological disorders and conditions related to the neuropeptide S system.
Used in Neuroscience Research:
SHA 68 is used as a research tool in neuroscience to study the role of neuropeptide S and its receptor in various physiological and pathological processes. Its ability to selectively antagonize the NPSR allows researchers to investigate the specific functions and mechanisms of the neuropeptide S system in the central nervous system.
Used in Drug Development for Neurological Disorders:
SHA 68 is used as a lead compound in the development of drugs targeting the NPSR for the treatment of neurological disorders. Its high selectivity and affinity for the NPSR make it a promising candidate for the development of drugs that can modulate the neuropeptide S system to alleviate symptoms and improve outcomes in patients with neurological conditions.
Used in Behavioral Studies:
SHA 68 is used in behavioral studies to investigate the effects of neuropeptide S and its receptor on various behaviors, such as horizontal activity, vertical rearing, and climbing in mice. Its ability to reduce NPS-induced behaviors makes it a valuable tool for understanding the role of the neuropeptide S system in modulating these behaviors.
Used in Addiction Research:
SHA 68 is used in addiction research to study the role of neuropeptide S and its receptor in the conditioned reinstatement of cocaine seeking in rats. Its ability to reduce conditioned reinstatement of cocaine seeking suggests that it may have potential as a therapeutic agent for the treatment of addiction and substance abuse disorders.

Upstream product

• 847553-76-8 3-oxo-1,1-diphenyltetrahydrooxazolo[3,4-a]pyrazine-7-carboxylic acid 9H-fluoren-9-ylmethyl ester 
• 132740-43-3 4-fluorobenzylisocyanate 
• 847555-93-5 1,1-diphenyltetrahydro-1H-oxazolo[3,4-α]pyrazin-3(5H)-one 
• 17532-22-8 (1,4-dibenzyl-piperazin-2-yl)-diphenyl-methanol 
• 17532-20-6 diphenyl(piperazin-2-yl)methanol 
• 591-51-5 phenyllithium 
• 1287264-28-1 3-oxo-4-(1-phenylethyl)piperazine-1-carboxylic acid tert-butyl ester 
• 944256-02-4 4-(1-phenylethyl)piperazine carboxylic acid tert-butyl ester 
• 1287264-37-2 (S)-1,1-diphenyl-7-((S)-1-phenylethyl)tetrahydro-1H-oxazolo[3,4-a]pyrazin-3(5H)-one 
• 1287264-39-4 3-oxo-1,1-diphenyltetrahydrooxazolo[ 3,4-a]pyrazine-7-carboxylic acid 9H-fluoren-9-ylmethyl ester 
• 1287264-25-8 {2-[(2-chloroacetyl)-(1-phenylethyl)amino]ethyl}carbamic acid tert-butyl ester 
• 1287264-33-8 3-oxo-1,1-diphenyltetrahydrooxazolo[ 3,4-a]pyrazine-7-carboxylic acid 9H-fluoren-9-ylmethyl ester 
• 1287264-32-7 (R)-1,1-diphenyl-7-((S)-1-phenylethyl)tetrahydro-1H-oxazolo[3,4-a]pyrazin-3(5H)-one 

Relevant academic research and scientific papers

Identification of neuropeptide s antagonists: Structure-Activity relationship studies, x-ray crystallography, and in vivo evaluation

Modulation of the neuropeptide S (NPS) system has been linked to a variety of CNS disorders such as panic disorder, anxiety, sleeping disorders, asthma, obesity, PTSD, and substance abuse. In this study, a series of diphenyltetrahydro-1H-oxazolo[3,4-α]pyr

Synthesis and separation of the enantiomers of the neuropeptide S receptor antagonist (9 R/S)-3-Oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4- a ]pyrazine-7-carboxylic Acid 4-fluoro-benzylamide (SHA 68)

This study reports the synthesis, chromatographic separation, and pharmacological evaluation of the two enantiomers of the neuropeptide S receptor (NPSR) antagonist (9R/S)-3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine- 7-carboxylic acid 4-fluoro-be

Identifying structural features on 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones critical for Neuropeptide S antagonist activity

A series of 7-substituted 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones were synthesized and tested for Neuropeptide S (NPS) antagonist activity. A concise synthetic route was developed, which features a DMAP catalyzed carbamate formation. 4-Fluorob

Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor

Neuropeptide S (NPS) has been shown to modulate arousal, sleep wakefulness, anxiety-like behavior, and feeding after central administration of the peptide agonist to mice or rats. We report here the chemical synthesis and pharmacological characterization of SHA 66 (3-oxo-1,1-diphenyl-tetrahydro- oxazolo[3,4-a]pyrazine-7-carboxylic acid benzylamide) and SHA 68 (3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide), two closely related bicyclic piperazines with antagonistic properties at the NPS receptor (NPSR). The compounds block NPS-induced Ca2+ mobilization, and SHA 68 shows displaceable binding to NPSR in the nanomolar range. The antagonistic activity of SHA 68 seems to be specific because it does not affect signaling at 14 unrelated G protein-coupled receptors. Analysis of pharmacokinetic parameters of SHA 68 demonstrates that the compound reaches pharmacologically relevant levels in plasma and brain after i.p. administration. Furthermore, peripheral administration of SHA 68 in mice (50 mg/kg i.p.) is able to antagonize NPS-induced horizontal and vertical activity as well as stereotypic behavior. Therefore, SHA 68 could be a useful tool to characterize physiological functions and pharmacological parameters of the NPS system in vitro and in vivo. Copyright

BICYCLIC PIPERAZINE COMPOUND AND USE THEREOF

The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.