Inooka, Hiroshi; Sakamoto, Kotaro; Shinohara, Tokuyuki; Masuda, Yasushi; Terada, Michiko; Kumano, Satoshi; Yokoyama, Kotaro; Noguchi, Jiro; Nishizawa, Naoki; Kamiguchi, Hidenori; Fujita, Hisashi; Asami, Taiji; Takekawa, Shiro; Ohtaki, Tetsuya published an article about the compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid( cas:156478-71-6,SMILESS:O=C(O)CN1CCN(C(OC(C)(C)C)=O)CC1 ).Related Products of 156478-71-6. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:156478-71-6) through the article.
Neuromedin U (NMU) is a neuropeptide known to regulate food intake and energy homeostasis that is widely distributed in the gastrointestinal tract, hypothalamus, and pituitary. A short form of NMU, porcine NMU-8 has potent agonist activity for the receptors NMUR1 and NMUR2; however, its short half-life precludes its effective use in vivo. To address this limitation, we designed and synthesized NMU-8 analogs modified by polyethylene glycol (PEG) with a mol. weight of 30 kDa (PEG30k) via a variety of linkers (i.e., ω-amino- and ω-imino-carboxylic acid linker). Integrated evaluation of NMUR1 and NMUR2 binding affinities in vitro and anorectic activity in mice revealed that the introduction of a linker with a rigid ring group, e.g., 2-(piperazin-1-yl)acetic acid (PipAc), yielded a highly potent anorectic peptide, PEG30k-PipAc-NMU-8 (14), possessing improved receptor binding affinity. Subsequent optimization of the mol. weight of the PEG moiety led to the discovery of a PEG20k conjugate (15), which exhibited significant anti-obesity effect upon once-daily s.c. administration in diet-induced obese mice with 10% and 22% body weight loss at doses of 10 and 30 nmol/kg, resp. In addition, 15 reduced the weights of the liver and adipose tissue in a dose-dependent manner and improved the plasma biochem. parameters, e.g., insulin, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase, and total cholesterol. Thus, our results suggest that 15 (NMU-0002), which showed potent and long-lasting biol. profiles in vivo, represents a candidate peptide for investigating the central and peripheral actions of NMU and its potential for clin. use.
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Reference:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem